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Weight Loss Patent Abstract
Formulations and methods for enhancing lipolysis and the suppression
of appetite are presented. Currently the preferred embodiment has
these formulations as two separate compositions because of taste
considerations (the combined taste, currently, is disagreeable).
However, it is known that the two separate compositions can be combined
into a single delivery systems, such as a drink, bar, gel or other
nutritional delivery system known in the arts. The two separate
compositions are: 1. compositions comprising substances that enhance
oxygen uptake, and 2. a protein supplement composition comprising
substances that regulate blood sugar. The overall purpose of this
invention is to induce weight loss in as short of time as possible
with the least amount of discomfort.
Weight Loss Patent Claims
What is claimed is:
1. A composition for weight loss comprising: a) a first composition
comprising at least one substance that enhance oxygen uptake; and
b) a second composition comprising a protein supplement comprising
at least one protein source and at least one substance that regulates
blood sugar.
2. The composition according to claim 1 wherein at least one substance
that regulates blood sugar further comprise a long chain inulin
and at least one water soluble chromium compound.
3. The composition according to claim 2 wherein the at least one
water soluble chromium compound are chromium arginate and/or chromium
chelidamate.
4. The composition according to claim 2 further comprising additional
components comprising inulin, L-methionine, and/or a medium chain
triglyceride oil.
5. The composition according to claim 4 further comprising additional
components comprising inulin, L-methionine, and/or a medium chain
triglyceride oil.
6. The composition according to claim 1 wherein the first separate
composition further comprises at least one xanthine and/or at least
one ephedra based thermogenic composition.
7. The composition according to claim 6 wherein the at least one
xanthine and/or at least one ephedra based thermogenic composition
further comprises caffeine and at least one other member of the
xanthine family that is not caffeine.
8. The composition according to claim 7 wherein the ratio of the
weight of caffeine to the total weight of the other members of the
xanthine family within the composition typically ranges from about
1:3 to 3:1.
9. The composition according to claim 7 wherein the ratio of the
weight of caffeine to the total weight of the other members of the
xanthine family within the composition typically ranges from about
1:2 to 2:1.
10. The composition according to claim 6 further comprising at
least one cognitive cofactor.
11. The composition according to claim 7 wherein the at least one
cognitive cofactor comprise biosynthetic precursors to neurotransmitters
or neurosteroids, cerebral vasodilators, minerals, nootropic herbs,
or essential amino acids.
12. The composition according to claim 11 wherein the biosynthetic
precursors to neurotransmitters or neurosteroids, cerebral vasodilators,
minerals, nootropic herbs, or essential amino acids are comprised
of ginkgo biloba; niacin and derivatives containing the niacin nucleus;
acetyl-L-carnitine; dimethylaminoethanol (DMAE); choline including
esters and salts thereof; amino acids including salts and esters
thereof, such as L-phenylalanine, glutamic acid, glycine, and aspartic
acid; squalane; squalene; pregnenolone; dehydroepiandrosterone (DHEA);
or dehydroeplandrosterone-3-sulphate.
13. A composition for weight loss comprising: a) a first composition
comprising at least one substance that enhance oxygen uptake comprising
Ephedra E @ 8%, which ranges between 0.1-40% by weight of the composition,
Green Tea Extract @ 90% Theophylline, which ranges between 0.1-40%
by weight of the composition, Guarana Extract @ 90% Caffeine, which
ranges between 0.1-40% by weight of the composition, Coleus Forskholii
extract @ 10%, which ranges between 0.001-20% by weight of the composition,
L-Tyrosine, which ranges between 0.1-50% by weight of the composition,
Dimethylaminoethanol 50 mg 0.1-75% by weight of the composition,
Choline Citrate, which ranges between 0.1-75% by weight of the composition,
Huperzine-A, which ranges between 0.000001-5% by weight of the composition,
St. John's Wort @ 0.3% hypericum, which ranges between 0.1-50% by
weight of the composition, Passionflower Extract A, which ranges
between 0.1-50% by weight of the composition, Potassium Chloride,
which ranges between 0.1-20% by weight of the composition, Magnesium
Phosphate Dibasic, which ranges between 0.1-80% by weight of the
composition, Chromium Arginate, which ranges between 0.001-20% by
weight of the composition, White Willow Bark (Salicylic Acid), which
ranges between 0.01-75% by weight of the composition, and Excipients
as necessary; and b) a second composition comprising a protein supplement
comprising at least one protein source and at least one substance
that regulates blood sugar comprising: Soy Protein, which ranges
between 10-99% by weight of the composition, Inulin, which ranges
between 0.01-20% by weight of the composition, L-Methionine, which
ranges between 0.01-20% by weight of the composition, MCT oil, which
ranges between 0-10% by weight of the composition, Vanilla Flavoring,
which ranges between 0-10% by weight of the composition, Sucralose,
which ranges between 0-10% by weight of the composition, Carboxymethyl
Cellulose, which ranges between 0-20% by weight of the composition,
Carrageenan, which ranges between 0-20% by weight of the composition,
Magesium Phosphate, which ranges between 0-30% by weight of the
composition, Chromium Arginate, which ranges between 0-5% by weight
of the composition, Chromium Chelidamate, which ranges between 0-5%
by weight of the composition, Glycine, which ranges between 0.01-20%
by weight of the composition, Vanadyl Sulfate, which ranges between
0.001-10% by weight of the composition, Manganese gluconate, which
ranges between 0.001-10% by weight of the composition.
14. A composition for weight loss comprising: a) a first composition
comprising at least one substance that enhance oxygen uptake comprising
Gingko A at approximately 5.0 mg, Theophylline at approximately
25.0 mg, Caffeine at approximately 27.5 mg, Green Tea at approximately
84.0 mg, L-pyroglutamate at approximately 75.0 mg, Xanthinol nicotinate
at approximately 38.0 mg, N-Acetyl-L-carnitine at approximately
7.5 mg, Choline Bitartrate at approximately 122.0 mg, DMAE bitartrate
at approximately 60.0 mg, Magnesium glycinate at approximately 25.0
mg, L-phenylalanine at approximately 50.0 mg, and Chromium arginate
at approximately 200 mg, and b) a second composition comprising
a protein supplement comprising at least one protein source and
at least one substance that regulates blood sugar comprising: Soy
Protein, which ranges between 10-99% by weight of the composition,
Inulin, which ranges between 0.01-20% by weight of the composition,
L-Methionine, which ranges between 0.01-20% by weight of the composition,
MCT oil, which ranges between 0-10% by weight of the composition,
Vanilla Flavoring, which ranges between 0-10% by weight of the composition,
Sucralose, which ranges between 0-10% by weight of the composition,
Carboxymethyl Cellulose, which ranges between 0-20% by weight of
the composition, Carrageenan, which ranges between 0-20% by weight
of the composition, Magesium Phosphate, which ranges between 0-30%
by weight of the composition, Chromium Arginate, which ranges between
0-5% by weight of the composition, Chromium Chelidamate, which ranges
between 0-5% by weight of the composition, Glycine, which ranges
between 0.01-20% by weight of the composition, Vanadyl Sulfate,
which ranges between 0.001-10% by weight of the composition, Manganese
gluconate, which ranges between 0.001-10% by weight of the composition.
15. A composition for weight loss comprising: a) a first composition
comprising at least one substance that enhance oxygen uptake comprising
Caffeine, which ranges between 1-60% by weight of the composition,
Theophylline, which ranges between 1-60% by weight of the composition,
Gingko-A, which ranges between 0-50% by weight of the composition,
L-pyroglutamate, which ranges between 1-70% by weight of the composition,
Xanthinol nicotinate, which ranges between 1-70% by weight of the
composition, N-Acetyl-L-carnitine, which ranges between 0-50% by
weight of the composition, Choline Bitartrate, which ranges between
1-70% by weight of the composition, DMAE, which ranges between 1-70%
by weight of the composition, Magnesium glycinate, which ranges
between 0-50% by weight of the composition, Potassium aspartate
21%, which ranges between 0-50% by weight of the composition, Chromium
arginate, which ranges between 0-5% by weight of the composition,
and L-phenylalanine, which ranges between 1-70% by weight of the
composition, and b) a second composition comprising a protein supplement
comprising at least one protein source and at least one substance
that regulates blood sugar comprising: Soy Protein, which ranges
between 10-99% by weight of the composition, Inulin, which ranges
between 0.01-20% by weight of the composition, L-Methionine, which
ranges between 0.01-20% by weight of the composition, MCT oil, which
ranges between 0-10% by weight of the composition, Vanilla Flavoring,
which ranges between 0-10% by weight of the composition, Sucralose,
which ranges between 0-10% by weight of the composition, Carboxymethyl
Cellulose, which ranges between 0-20% by weight of the composition,
Carrageenan, which ranges between 0-20% by weight of the composition,
Magesium Phosphate, which ranges between 0-30% by weight of the
composition, Chromium Arginate, which ranges between 0-5% by weight
of the composition, Chromium Chelidamate, which ranges between 0-5%
by weight of the composition, Glycine, which ranges between 0.01-20%
by weight of the composition, Vanadyl Sulfate, which ranges between
0.001-10% by weight of the composition, Manganese gluconate, which
ranges between 0.001-10% by weight of the composition.
Weight Loss Patent Description
FIELD OF THE INVENTION
[0001] The present invention is generally directed to mood stabilization,
lipolysis, and appetite suppression, and compositions and methods
relating thereto. These compositions include components that increase
oxygen uptake and suppress appetite in conjunction with a modified
food source that comprises protein compositions and compositions
that regulate blood sugar.
BACKGROUND OF THE INVENTION
[0002] Obesity continues to be a problem approaching pandemic proportions
in this country. Unfortunately most weight loss approaches utilize
substances that are inherently tachyphylactic. Historically substances
that have induced weight loss have been amphetamines, their congeners,
substituted tertiary amines and the like, or their precursors, mahuang
cephedra and the like. Unfortunately, these substances promote anxiety
when used at therapeutic levels and with increased use their efficacy
proportionally diminishes. They also promote a secondary depression
upon withdrawal due to neural transmitter depletion.
[0003] Thermogenic substances that promote lipolysis include a
variety of different compounds and combinations that include, but
are not limited to, ephedrine, xanthine compounds such as caffeine,
theophylline, theobromine and alpha adrenergic stimulants. Yohimbine,
coleus forskholii and the like or beta adrenergicstimulants such
as clenbuterol.
[0004] However while these substances are thermogenic and lipolytic
they have no sustained effect on appetite suppression. Interestingly,
all the aforementioned, including amphetamines, affect oxygen transport
by increasing bronchial diameter. In effect they are bronchodilators
because they selectively affect relaxation of certain muscles in
the bronchial tree. The addition, therefore, of a substance that
selectively relaxes smooth muscle would further enhance this effect.
[0005] Surprisingly, alkaloids derived from coleus forskholii synergistically
enhance bronchial dilation when combined with any of the aforementioned
compounds, ephedra, xanthines and the like. This clearly enhances
oxygen transport and therefore lipolysis. Yohimbine and its alkaloids
can also effectively enhance bronchodilation in conjunction with
ephedra or xanthine compounds.
[0006] Effective appetite suppression requires that the neural
transmitters be in balance. This specifically includes the acetylcholine,
serotonin, norepinephrine and dopamine pathways. In addition to
increased appetites, imbalances in neural transmitters can also
cause the symptoms of both depression and anxiety. It has been found
that the vast majority of overeating occurs as a result of anxiety
and/or depression. Thus, regulating the neural transmitter levels
by appropriate supplementation will profoundly affect appetite and
therefore sustain weight loss.
[0007] Anxiolytic preparations that are particularly useful include
passion flower and magnesium containing compounds. Compounds that
up-regulate acetylcholine by reversibly inhibiting acetylcholine
breakdown are also effective in reducing anxiety. Physostigmine,
pyridostigmine and Huperzine A are effective because they are acetylcholinesterase
inhibitors and therefore they allow a build up of acetylcholine
in the system. At the axial-dendritic junction, adding choline containing
compounds such as dimethylaminoethanol (DMAE), phosphatidylcholine
and/or choline bitartrate will obviously intensify the anxiety reduction
effect because they provide the appropriate substrate precursors
that will allow the body to manufacture acetylcholine.
[0008] Finally, inclusion of additional substances that have anti-depressive
properties is useful to any composition that diminishes appetite.
St. Johns Wort (Hypericum), buproprion hydrochloride and S-adenosyl
methionine are useful examples of additional substances that affect
and up regulate mood.
[0009] In order to supplement the bodies' ability to synthesize
norepinephrine and dopamine, it is important to have the corresponding
precursor amino acids, such as tyrosine and/or phenylalanine. The
presence of these precursors will help prevent neural transmitter
depletion and secondary depression so commonly seen after the cessation
of ephedrine or xanthine compounds, said compounds cause global
cerebrocortical stimulation and hence increase the utilization of
the various neurotransmitters.
[0010] However, to truly and powerfully affect weight loss, the
combination of an appropriate protein substrate in conjunction with
the aforementioned substances that enhance oxygen uptake and prevent
the global depression associated with the cerebrocortical stimulant
effect would be most useful. In fact, the addition of a high protein,
low fat, low carbohydrate supplement to the diet in conjunction
with the aforementioned compositions, which will increase oxygen
uptake, will dramatically and surprisingly affect weight loss. It
will be clear that the combination of a substance that increases
oxygen uptake in conjunction with a high protein supplement that
regulates blood sugar is far more effective than either composition
alone in inducing weight loss.
SUMMARY OF THE INVENTION
[0011] The present invention provides an orally administered composition
for enhancing lipolysis and inducing appetite suppression and methods
provided thereto. Surprisingly it has been found that lipolysis
and bronchial dilation with the attendant increase in oxygen transport
are intimately related. Equally surprising it has been found that
the use of said composition in conjunction with a high protein nutritional
supplement that embodies an excess of methionine in conjunction
with blood sugar regulating compounds such as inulin and chromium,
dramatically enhances weight loss and thereby decreases fat in a
much shorter time then would otherwise be the case with simple diet
or the oxygen uptake enhancing composition alone. Of equal interest,
it is noted that the combination of the oxygen uptake enhancing
composition in conjunction with the high protein composition that
regulates blood sugar tends to markedly decrease the sensation of
hunger in those for that such obvious calorie restriction would
other wise cause a significant degree of hardship. In fact it was
determined by the use of the Hamilton Anxiety Scale that people
on this particular approach were less anxious that they would be
on either approach alone. As previously noted, anxiety and the attendant
depression constitute the primary reasons for over eating in humans.
[0012] The novel features that are considered characteristic of
the invention are set forth with particularity in the appended claims.
The invention itself, however, both as to its structure and its
operation together with the additional objects and advantages thereof
will best be understood from the following description of the preferred
embodiment of the present invention when read in conjunction with
the accompanying figures. Unless specifically noted, it is intended
that the words and phrases in the specification and claims be given
the ordinary and accustomed meaning to those of ordinary skill in
the applicable art or arts. If any other meaning is intended, the
specification will specifically state that a special meaning is
being applied to a word or phrase. Likewise, the use of the words
"function" or "means" in the Description of
Preferred Embodiments is not intended to indicate a desire to invoke
the special provision of 35 U.S.C. .sctn.112, paragraph 6 to define
the invention. To the contrary, if the provisions of 35 U.S.C. .sctn.112,
paragraph 6, are sought to be invoked to define the invention(s),
the claims will specifically state the phrases "means for"
or "step for" and a function, without also reciting in
such phrases any structure, material, or act in support of the function.
Even when the claims recite a "means for" or "step
for" performing a function, if they also recite any structure,
material or acts in support of that means of step, then the intention
is not to invoke the provisions of 35 U.S.C. .sctn.112, paragraph
6. Moreover, even if the provisions of 35 U.S.C. .sctn.112, paragraph
6, are invoked to define the inventions, it is intended that the
inventions not be limited only to the specific structure, material
or acts that are described in the preferred embodiments, but in
addition, include any and all structures, materials or acts that
perform the claimed function, along with any and all known or later-developed
equivalent structures, materials or acts for performing the claimed
function.
DESCRIPTION OF THE DRAWINGS
[0013] FIG. 1 Average weight lost/week with Xanthine composition
over 4 weeks.
[0014] FIG. 2 Average weight lost/week with Protein Supplement
composition containing compositions that regulate blood sugar over
4 weeks.
[0015] FIG. 3 Average weight lost/week with Xanthine composition
& protein supplement containing blood sugar regulating compositions
over 4 weeks.
[0016] FIG. 4 Average weight lost/week with Ephedra & Xanthine
& coleus forskholii over 4 weeks.
[0017] FIG. 5 Average weight lost/week with Ephedra and Xanthine
and coleus forskholii and protein supplement composition over 4
weeks.
[0018] FIG. 6 Weight loss totals over 4 weeks according to the
various compositions of FIGS. 1-5.
[0019] FIG. 7. Shows the results of the Hamilton Anxiety Test on
subjects using the composition according to the present invention.
DESCRIPTION OF THE PREFERRED EMBODIMENTS
[0020] The present invention is general directed toward compositions
and methods for enhancing lipolysis and the suppression of appetite.
Currently the preferred embodiment has these compositions as two
separate compositions because of taste considerations (the combined
taste, currently, is disagreeable). However, it is known that the
two separate, compositions can be combined into a single delivery
systems, such as a drink, bar, gel or other nutritional delivery
system known in the arts. The two separate compositions are: 1.
compositions comprising substances that enhance oxygen uptake, and
2. a protein supplement composition comprising substances that regulate
blood sugar. The overall purpose of this invention is to induce
weight loss in as short of time as possible with the least amount
of discomfort. Although many specific details associated with certain
aspects of the present invention are set forth below, those skilled
in the art of pharmacology and especially neuro-pharmacology and
nutrition will recognize that the present invention may have additional
embodiments or that the invention may be practiced without several
of the details disclosed herein.
[0021] Generally speaking, a diet is simply a reduction in caloric
intake. The body responds to the lower caloric intake by in turn
lowering metabolic rate in an attempt to conserve energy. Therefore,
one can deduce that the body decreases its uptake of oxygen so as
to decrease the amount of weight lost. At lower metabolic rates
the body burns fewer calories than under normal circumstances, hence
an individual gets disappointing weight loss results even though
the caloric intake is lower. This is true of virtually all diets
that last more than two to three weeks. If an individual wants to
lose weight, reduce body fat, and improve muscle tone, more than
diet is required. A total weight management and exercise program
increases the body's metabolism and enables it to burn calories
at a faster rate.
[0022] The components of the two separate compositions according
to the present invention are more specifically described below.
[0023] The present invention provides a first separate composition
that is an orally administered composition for enhancing oxygen
uptake. There is also a second separate composition that provides
is a nutritional protein supplement composition that regulates of
blood sugar.
[0024] Oxygen Uptake Enhancing Composition
[0025] Exercise helps to increase the rate at which the body burns
fat to thermogenicly/lipolytically produce heat. This is why exercise,
in addition to moderate daily caloric intake, has always been an
effective means for weight loss. Recently, the medical community
has discovered that herbal thermogens help boost the body's ability
to burn fat and curb an individuals appetite, thus making the addition
of herbal thermogens a great adjunct to exercise and diet programs.
[0026] Several products on the market contain the herb ephedra,
a versatile thermogenic/lipolytic herb. Ephedra contains ephedrine,
a stimulant naturally found in the plant. This herb promotes weight
loss because it has a thermogenic/lipolytic and fat-metabolizing
effect. Ephedrine is thought to activate both alpha and beta adrenoceptors,
which elevates metabolic rate, thereby increasing caloric expenditure
and resulting in weight loss. Ephedrine also exhibits appetite suppressant
properties by reducing one's desire for food. In other words, ephedrine
simultaneously speeds up metabolism and reduces caloric intake by
curbing the appetite.
[0027] It is important to remember that ephedra has been used for
relieving asthma and allergies for many individuals. It is quite
potent owing to the ephedrine and pseudoephedrine it naturally contains.
Both compounds excite the sympathetic nervous system causing vasoconstriction
of the nasal mucosa, dilation of the bronchioles, as well as cardiac
stimulation. While these natural substances produce benefits similar
to the body's adrenaline, they are not overly stimulating. This
is why ephedra is such a useful herbal plant. It is extremely effective
without being too strong in its actions when properly utilized.
[0028] The metabolic action of ephedra can be greatly enhanced
when it is used in combination with a source of caffeine and other
non-caffeine xanthines, such as when ephedra is combined with guarana
and green tea alone. Caffeine, methylxanthines, and ephedrine work
together to produce thermogenisis and to burn more fat than ephedrine
alone. The greatest synergistic effect occurs when ephedra, guarana
and green tea are combined with white willow bark (white willow
bark is a source of salicin, a natural relative of aspirin). Some
products designed to induce thermogenesis contain both ephedra and
guarana plus occasionally white willow, but the fast acting synergistic
combination of all four herbs yields the greatest results toward
the goal of long lasting weight loss.
[0029] Thus, in the first separate composition contains caffeine
in addition to at least one other member of the xanthine family
that is not caffeine. The composition may contain caffeine and xanthine,
caffeine and theophylline, caffeine and theobromine or caffeine,
theophylline and xanthine, to name a few representative possibilities.
In one embodiment, the composition contains caffeine and theophylline
as the only active ingredients from the xanthines as defined above.
The ratio of the weight of caffeine to the total weight of the other
members of the xanthine family within the composition typically
ranges from about 1:3 to 3:1, and preferably ranges from about 1:2
to 2:1.
[0030] The term "xanthine" as used herein refers to compounds
incorporating the xanthine nucleus as shown below, wherein R.sup.1,
R.sup.2, and R.sup.3 are independently selected from hydrogen and
lower (C1-C4) alkyl. 1
[0031] Exemplary xanthine compounds include xanthine, wherein R.sup.1,
R.sup.2, and R.sup.3 are hydrogen; caffeine, also known as trimethylxanthine,
where R.sup.1, R.sup.2, and R.sup.3 are each methyl; theophylline,
which is also known as 1,3-dimethylxanthine, wherein R1 is hydrogen
and R.sup.2 and R.sup.3 are methyl; and theobromine, also known
as 3,7-dimethyl xanthine, wherein R.sup.1 and R.sup.2 are methyl
and R.sup.3 is hydrogen. As used herein, the term "first xanthine
compound" means caffeine, and the term "second xanthine
compound" refers to xanthine compounds as defined above, excluding
caffeine. Pharmaceutically-acceptable salts, hydrates and solvates
of xanthines are also included within the term "xanthines"
as used herein. The salt may be an acid- or base- addition salt.
Such salts may have at least one negatively charged ion such as
chloride, bromide, sulfate, phosphate, C.sub.1-15carboxylate, methanesulfonate
and p-toluenesulfonate, where exemplary C.sub.1-15carboxylate ions
are acetate, glycolate, lactate, pyruvate, malonate, succinate,
glutarate, fumarate, malate, tartarate, citrate, ascorbate, maleate,
hydroxylmaleate, benzoate, hydroxybenzoate, phenylacetate, cinnamate,
salicylate and 2-phenoxybenzoate. The salt may have at least one
positively charged ion such as lithium, sodium, potassium, beryllium,
magnesium, calcium and quaternary ammonium ions, where exemplary
quaternary ammonium ions are tetraalkylammonium, and trialkylaralkyammonium
ions. A solvate or hydrate of the salt may include ethylenediamine.
[0032] Xanthines are commercially available in pure form, and as
such may be used in preparing compositions of the invention. For
example, caffeine and theophylline are each available in 99% purity
from Aldrich chemical Company (Milwaukee, Wis.), and may also be
obtained from Sigma Chemical Company (St. Louis, Mo.).
[0033] Both caffeine and theophylline are known to have desirable
effects on the mammalian body. Caffeine dilates coronary arteries
and bronchioles in the lungs. In time, it also induces cerebral
vasoconstriction and is a powerful neurostimulant. Theophylline
increases bronchial dilation significantly, thereby enhancing the
transportation of oxygen into cells and carbon dioxide out of the
body, and is a low-grade cortical neurostimulant. Caffeine, however,
is known to significantly enhance mental performance and to prolong
a wakeful state. Both caffeine and theophylline are known to enhance
physical performance.
[0034] The potentiating action of caffeine and salicin (found in
white willow bark) on ephedrine's action has been studied in numerous
weight loss studies in animals and humans. A report in the American
Journal of Clinical Nutrition showed that when ephedrine was used
alone with a group of animals, it resulted in losses of 14 percent
in body weight and 42 percent in body fat. When it was used in combination
with caffeine, however, there was a loss of 25 percent in body weight
and 75 percent in body fat. In contrast, when caffeine was used
alone there was no significant loss in body weight. The reason for
the increased loss of body weight is an increased metabolic rate
and fat cell breakdown promoted by ephedrine and potentiated by
caffeine.
[0035] Research reported by Dr. Dulloo and others in Nutrition
(5:7-9, 1989), has shown that when caffeine is combined with lose-dose
aspirin and ephedrine, an ephedra/kolaut/white willow bark mixture
has been shown to cause significant weight loss in overweight persons
who consume a reduced-calorie diet.
[0036] It has been known for some time that small airway obstructions
associated with clinical diseases such as asthma or emphysema have
an inflammatory component. Surprisingly, the use of a known anti-inflammatory
composition such as salicylic acid (naturally found in white willow
bark) in conjunction with bronchodilators also substantially increases
oxygen transport, and consequently increases calorie burning, of
course many other anti-inflammatory agents could be used to similar
results.
[0037] Acetylcholine is a neurotransmitter necessary for normal
conduction of nerve impulses between nerve endings. In addition,
the use of a reversible acetylcholinesterase inhibitor (a compound
that inhibits the enzyme acetylcholinesterase, which breaks down
acetylcholine and renders it ineffective at nerve junctions) further
enhances acetylcholine levels and prevents attendant breakdown of
this neurotransmitter level, in spite of chronic stimulant use.
Huperzine A, a derivative of Chinese moss, is a particularly effective
natural acetylcholinesterase inhibitor.
[0038] Research has also shown that the herb coleus forskhollii
also relaxes smooth muscle, thereby inducing or increasing bronchiodilation,
thereby increasing oxygen transport. This, in conjunction with the
ability of caffeine to increase free fatty acid release, will clearly
result in an increased tendency towards lipolysis (the breakdown
of fat).
[0039] It appears that the regular use of ephedra, caffeine, methylxanthines,
coleus forskhollii and salicin in is relatively safe for most people.
Ephedrine, especially in its herbal form, also appears relatively
innocuous for individuals not in a high risk group, such as individuals
with high blood pressure, heart disease, diabetes, those taking
antidepressants, or certain other prescription or over-the-counter
medications.
[0040] In order to produce optimal weight loss benefits, herbal
thermogenic/lipolytic products containing ephedra, guarana, green
tea and white willow bark must be properly combined in synergistic
formulations that include appropriate neurotransmitter precursors,
as discussed below.
[0041] Although some authors have questioned the value of caffeine,
Dr. Daniel Mowrey, in his book Fat Management! has proven caffeine
to be effective in supporting a continued supply of neurotransmitters.
Thus, the inclusion of caffeine acts not only to boost the stimulant
effect for of other components, but to help preserve the balance
of neurotransmitters necessary for total well being.
[0042] Caffeine is used in many cultures as a stimulant. Coffee
is rapidly becoming our culture's "herbal" stimulant of
choice. Studies show that most healthy people can safely consume
up to 200 mg of caffeine and related methylxanthines per day without
adverse reactions. Research shows that herbal thermogenic/lipolytic
formulas are effective at levels well below this threshold.
[0043] It is also known that when used in combination methylxanthines,
caffeine, and ephedrine, all of which will induce bronchodilation,
has the effect of increasing weight loss that is demonstrably better
than when the compounds are used alone.
[0044] One of the primary benefits of thermogenic/lipolytic formulas
seems to be their ability to promote fat breakdown while sparing
muscle tissue (since frequently low calorie diets also cause loss
of muscle tissue). In one study reported by Astrup and coworkers
in Metabolism (41:686-688, 1992), a combination of ephedrine (20
mg) and caffeine (200 mg), taken twice a day or a placebo for eight
weeks in 16 obese women showed no significant difference in weight
loss between groups. However, the ephedrine group lost on the average
4.5 kg more fat and 2.8 kg less muscle mass. While the total weight
loss did not differ, the ephedrine group increased lipolysis while
sparing muscle mass. Additionally, the ephedrine group had a higher
level of energy expenditure than did the placebo group--a definite
plus for dieting. The extra energy available for expenditure apparently
resulted from the fat breakdown.
[0045] In addition to caffeine and a second (non-caffeine) xanthine,
the first composition contains one or more cognitive cofactors.
As used herein, a cognitive cofactor ameliorates diffuse chronic
depolarization and subsequent cortical depression commonly associated
with stimulants. Exemplary cognitive cofactors include, without
limitation, biosynthetic precursors to neurotransmitters or neurosteroids,
cerebral vasodilators, minerals, nootropic herbs, and essential
amino acids.
[0046] The biosynthetic precursor of a neurotransmitter is a compound
which, upon ingestion by a subject, is converted in vivo into a
neurotransmitter, while a biosynthetic precursor of a neurosteroid
is a compound, which upon ingestion by the subject, is converted
in vivo into a neurosteroid. Biosynthetic precursors of both neurotransmitters
and neurosteroids are well known in the art.
[0047] The following are exemplary cognitive cofactors according
to the first composition: ginkgo biloba; niacin and derivatives
containing the niacin nucleus; acetyl-L-carnitine; dimethylaminoethanol
(DMAE); choline including esters and salts thereof, amino acids
including salts and esters thereof, such as L-phenylalanine, glutamic
acid, glycine, and aspartic acid; squalane; squalene; pregnenolone;
dehydroepiandrosterone (DHEA); and dehydroeplandrosterone-3-sulphate.
All of these biosynthetic precursors can be acquired from Sigma
Chemical Company (St. Louis, Mo.).
[0048] A description of the above precursors follows:
[0049] Ginkgo biloba is a nootropic herb. It has been found to
significantly increase cerebral circulation, enhance mental alertness,
and increase the production of ATP in the brain. It also improves
the ability of the brain to metabolize glucose. It is a powerful
antioxidant and cerebral vasodilator.
[0050] Niacin and derivatives thereof include compounds that contain
the niacin nucleus, which is shown below:
[0051] Niacin and derivatives thereof include, but are not limited
to niacin, xanthinol nicotinate, methyl nicotinate, tocopheral nicotinate,
and inositol hexanicotinate. Xanthinol nicotinate is a preferred
niacin derivative and a preferred cognitive cofactor according to
the invention. Xanthinol nicotinate is known to be a potent cerebral
vasodilator of significant specificity, has been used for many years
to lower serum cholesterol, and has been shown to dramatically enhance
cerebral blood flow. On the basis of in vivo testing, it is also
known that once inside brain cells, xanthinol nicotinate will increase
glucose metabolism and correspondingly increase ATP. Xanthinol nicotinate
does not generally cause flushing.
[0052] Acetyl-L-carnitine is related to choline compounds both
clinically and chemically. Acetyl-L-carnitine protects the brain
from the effects of aging. It has been definitively shown to decrease
the buildup of lipofuscin pigments that are found in the brains
of aged mammals. A buildup of these fatty deposits in nerve cells
is associated with reduction of cognitive powers and a decrease
in the rate of depolarization of nerve cells. Acetyl-L-carnitine
increases brain levels of choline-acetyl-transferase and acetylcholine,
a vital neurotransmitter.
[0053] Dimethylaminoethanol, or DMAE, is normally present in small
amounts in mammalian brains. DMAE is known for its ability to elevate
mood, enhance memory, increase intelligence, and increase the rate
at which learning is accomplished. DMAE may take some time to have
its effect noticed when taken alone. DMAE works by accelerating
the brain's synthesis of the neurotransmitter acetylcholine. In
the present composition, DMAE acts synergistically to dramatically
enhance the effects of the xanthine stimulants.
[0054] Choline esters and salts as presented in compositions of
the present invention are biosynthetic precursors to acetylcholine.
A preferred choline salt is choline bitartrate, which is a phospholipid
that is the immediate biosynthetic precursor of acetylcholine. Choline
is known for its ability to improve memory by increasing the amount
of acetylcholine in the brain. Choline bitartrate is a preferred
form of choline because of its water solubility, which makes it
more readily absorbable on the basis of oral administration.
[0055] Glutamic acid esters and salts, as used herein, includes
pyroglutamate and arginine pyroglutamate. Pyroglutamate is a glutamic
acid compound that is present in very large amouns in the human
brain, cerbral spinal fluid, and blood. Pyroglutamate is known to
have a number of remarkable cognitive enhancing effects. Studies
have shown that pyroglutamate will effectively treat alcohol-induced
memory deficits in humans. It has been shown that pyroglutamate
can be very effectively transformed in the brain into the neurotransmitter
glutamine. Arginine pyroglutamate has been found to not only enhance
cognition, but is also an excellent grown hormone releasing factor
because it is carried far more efficiently across the blood brain
barrier than arginine alone. Other glutamic acid compounds are also
efficacious as neurotransmitter precursors.
[0056] Aspartic acid and esters and salts thereof includes, without
limitation, the sodium and potassium salts of aspartic acid. Potassium
aspartate is a preferred aspartic acid salt, which may be used to
enhance the intracellular ionic balance in the central nervous system
that may otherwise be depleted by various stimulants.
[0057] Squalane and squalene are immediate biosynthetic precursors
of all steroid molecules, including neurosteroids, and can be converted
as needed to pregnenolone and/or other steroids. Pregnenolone is
a neurosteroid that is known to enhance memory function. It has
been conclusively shown to decrease GABA (gamma-amino-butyric acid)
activity and thereby enhance wakefulness. Dehydroepiandrosterone
and dehydroeplandrosterone-3-sulphate are related neurosteroids
that are known to stabilize cell membranes. In particular, they
are known to affect astrocytes and the splingomyelin sheath.
[0058] Specifically, the pathways for the neurotransmitters, acetylcholine,
norepinephrine, and dopamine are affected. In order to ameliorate
this problem, it is known that supplementation with neurotransmitter
precursors can be effective in maintaining physiological levels
of the neurotransmitters in the body.
[0059] The use of certain amino acids such as L-tyrosine and L-phenylalanine
has been found to be particularly important since these are precursors
to norepinephrine and dopamine. The use of various choline containing
compounds such as choline citrate, and dimethlyaminoethanol (DMAE),
etc. have proven effective in supporting the continued supply of
neurotransmitters.
[0060] Huperzine A works by a unique mechanism that has been scientifically
discovered and reported in many research journals. It acts as a
potent acetylcholinesterase inhibitor. As stated earlier, acetylcholine
is the neurotransmitter in the brain that is responsible for carrying
electrical impulses from one nerve to another. Acetylcholine is
produced in the end sections of nerve fibers and packaged into small
vesicles where it is stored until released by the nerve ending.
Once the nerve ending has secreted acetlycholine, it persists for
a few seconds. In a normal brain, the enzyme acetylcholinesterase
serves a housekeeping function by breaking down the acetylcholine
into an acetate molecule (from the "acetyl" part) and
choline. The choline (a member of the B-vitamin family) is then
transmitted back into the nerve ending to be used again to make
acetylcholine. Frequently when individuals take stimulant preparations,
the precursors for producing acetylcholine are decreased, leading
to a deficiency of acetylcholine available at the nerve junctions.
Even with this deficiency, the acetylcholine is still released by
the nerve endings. Huperzine A stops the acetylcholinesterase from
breaking down acetylcholine, thus preventing acetylcholine deficiency
and improving mental function.
[0061] Hypericum, the active ingredient in St. John's Wort, is
known to be an effective anti-depressant and anti-anxiety agent
(anxiolytic). Its effect is due to the inhibition of serotonin reuptake.
Serotonin is another neurotransmitter whose levels affect mood,
memory, anxiety and perceived energy levels. This, in conjunction
with enhanced acetylocholine levels, surprisingly inhibits anxiety
related to the use of any stimulant. Additionally, improvements
in even sub-clinical depression and anxiety decrease the excessive
appetite often seen with these conditions.
[0062] The amino acid L-tyrosine (normally present in dietary intake)
and/or L-phenylalanine are also important to controlling how the
brain functions. The brain can use L-tyrosine to synthesize the
neurotransmitters norepinephrine and dopamine, both of which are
critical to the feeling of alertness and stability. The addition
of L-tyrosine to the preparation assists the brain to stabilize
levels of norepinephrine and dopamine that would otherwise be depleted
by stimulant use.
[0063] Ephedrine, caffeine, and theophylline all have central nervous
system stimulant effects. As a result, it is well known that tachyphylaxis
is a side effect of these stimulants and that sub-threshold depression
may occur with sustained use or abrupt withdrawal. This is due to
generalized neurotransmitter depletion. Specifically, the acetylcholine,
norepinephrine, and dopamine pathways are affected. In order to
ameliorate this problem, it was found that supplementation of neurotransmitter
precursors was surprisingly effective. In addition, supplying an
acetylcholinesterase inhibitor was particularly effective.
[0064] The use of certain amino acids such as L-phenylalanine and/or
L-tyrosine was found to be particularly important since these are
precursors to norepinephrine and dopamine. The use of various choline
containing compounds including, but not limited to, phosphatidyl
choline, choline citrate, dimethylaminoethanol, and the like, as
proven effective. In addition, the use of a reversible acetylcholinesterase
inhibitor further enhances acetylcholine levels and prevents attendant
breakdown in spite of chronic stimulant use. Huperzine A, a derivative
of Chinese moss, is a particularly good acetylcholinesterase inhibitor,
although obviously other related pharmacological agents such as
physostigmine or pyrodostigmine would also prove functional.
[0065] Anxiety and depression are known to result in excessive
consumption of food beyond the body's nutritional requirements and
dietary norms. Oftentimes, these conditions are sub-threshold; i.e.,
not clinically apparent. It is now apparent that overeating can
be traced to deficiencies in certain neurotransmitters; i.e., norepinephrine
and/or serotonin. Logically, therefore, substances that decrease
and/or alleviate depression or anxiety will be useful in preventing
excessive dietary consumption. This in conjunction with enhanced
acetylcholine levels surprisingly inhibits appetite anxiety related
to the use of any stimulant. Anxiety can be decreased with use of
a variety of anxiolytic compounds. These include, but are not limited
to, benzodiazepines, Kava alkaloids, passionflower, valerian, and/or
chamomile extracts, and the like. Obviously, other antidepressants
could be used such as buproprion hydrochloride, fluoxetine, and
the like.
[0066] Several mineral compositions are useful supplements in the
formulation according to the present invention. They include magnesium
compounds such as magnesium phosphate or magnesium carbonate. It
is known that magnesium and potassium contribute to the relaxation
of smooth muscle.
[0067] A first example formulation of the oxygen uptake enhancing
composition according to the present invention, with ranges of ingredients
is noted below:
1 Ingredient mg/capsule Range % Ephedra E @ 8% 12 mg 0.1-40 Green
Tea Extract @ 90% 50 mg 0.1-40 Theophylline Guarana Extract @ 90%
Caffeine 40 mg 0.1-40 Coleus Forskholii extract @ 10% 2.5 mg 0.001-20
L-Tyrosine 65 mg 0.1-50 Dimethylaminoethanol 50 mg 0.1-75 Choline
Citrate 50 mg 0.1-75 Huperzine-A 0.009 mg 0.000001-5 St. John's
Wort @ 0.3% hypericum 25 mg 0.1-50 Passionflower Extract A 30 mg
0.1-50 Potassium Chloride 50 mg 0.1-20 Magnesium Phosphate Dibasic
100 mg 0.1-80 Chromium Arginate 0.1 mg 0.001-20 White Willow Bark
(Salicylic Acid) 30 mg 0.01-75 Excipients as necessary
[0068] The first four ingredients are thermogenic/lipolytic compositions
that effect smooth muscle relaxation in bronchioles. The second
four ingredients are neurotransmitter replacements that prevent
acetylcholine breakdown. St. John's Wort and Passionflower Extract
A are appetite suppressants (as their central effect), the potassium,
magnesium, and chromium salts are mineral replacements, and the
White Willow Bark acts as an anti-inflammatory agent.
[0069] If indeed, bronchodilation and its attendant increase in
oxygen transport are the cause for lipolysis, then relative increases
in FEV, will be directly related to weight loss. Surprisingly, this
is indeed the case. Therefore, thermogenesis and resultant increases
in metabolism are a direct consequence of increased oxygen delivery
and consumption in either the resting or active state. To effectively
demonstrate this principal, 10 individuals were given pulmonary
function tests that measured FEV.sub.1 and weight was measured and
recorded before administration of the composition above. The 10
individuals then regularly took the composition above. One month
later, FEV.sub.1 and weight were re-measured. Interestingly, those
with the largest positive increase in FEV.sub.1 (indicating the
greatest amount of bronchodilation) consistently lost the most weight.
[0070] In general, to achieve the beneficial results described
above, a person in need thereof may be administered active ingredients
of the first composition in an amount ranging from about 0.1 mg
per kg of body weight per day to about 100 mg/kg/day. For the average
person, a typical daily dosage is an amount ranging from 10 mg to
500 mg of caffeine in combination with a second xanthine compound
(not caffeine) in an amount ranging from 1 mg to 1000 mg. The cognitive
cofactor is present in a typical dosage in an amount ranging from
1 mg to 1000 mg. Preferred composition contains from 50 mg to 250
mg caffeine, from 10 to 500 mg of the second xanthine compound,
and from 10 mg to 500 mg f the cognitive cofactor.
[0071] The composition formulated for oral administration should
generally contain at lest about 4% of the active ingredients as
identified above, but that amount may be varied up to 100% of the
weight of the unit, if desired. The amount of the active ingredients
present in orally-administered composition is such tat a suitable
dosage will be obtained.
[0072] Preferred compositions and preparations according to the
present invention are prepared so that an oral dosage unit form
contains between 5.0-300 mg of the active ingredients as identified
herein.
[0073] A second example formulation of the oxygen uptake enhancing
composition according to the present invention, with ranges of ingredients
is noted below:
2 Ingredient mg/unit Range (%) 1. Gingko A 5.0 2. Theophylline
25.0 3. Caffeine 27.5 4. Green Tea 84.0 5. L-pyroglutamate 75.0
6. Xanthinol nicotinate 38.0 7. N-Acetyl-L-carnitine 7.5 8. Choline
Bitarirate 122.0 9. DMAE bitartrate 60.0 10. Magnesium glycinate
25.0 11. L-phenylalanine 50.0 12. Chromium arginate 200
[0074] An efficacy trial was performed according to the following
protocol: Three different groups of ten subjects were given a 240
calorie meal replacement. They were further given an additional
composition, in capsule form, depending upon in which group they
participated. The first group, Group A, was give a xanthine composition
containing caffeine, theophylline and a cognitive co-factor (See
the formulation below); the second group, Group B, was given the
same amount of caffeine and theophylline noted in the xanthine composition
given to Group A, but no cognitive cofactors; and the third group,
Group C, was given a placebo. The subjects were weighed weekly for
6 weeks and asked to note how long they were able to go after ingesting
the meal replacement and the capsules before feeling the need to
eat again.
[0075] A third example formulation of the oxygen uptake enhancing
composition according to the present invention, with ranges of ingredients
is noted below:
3 Weight Loss Effect Formula % Comp. Range % 1. Caffeine 220 mg
16.0% 1-60 2. Theophylline 110 mg 8.0% 1-60 3. Gingko-A 5 mg 0.36%
0-50 4. L-pyroglutamate 100 mg 7.3% 1-70 5. Xanthinol nicotinate
85 mg 6.2% 1-70 6. N-Acetyl-L-carnitine 7.5 mg 0.55% 0-50 7. Choline
Bitartrate 122 mg 8.9% 1-70 8. DMAE 200 mg 14.6% 1-70 9. Magnesium
glycinate 25 mg 1.8% 0-50 10. Potassium aspartate 21% 50 mg 3.6%
0-50 11. Chromium arginate 200 mg 14.6% 0-5 12. L-phenylalanine
250 mg 18.2% 1-70
[0076] The first composition provides, in one embodiment, a therapeutic
composition for oral administration that includes caffeine, a second
xanthine other than caffeine, and a cognitive cofactor as defined
above. Thus, the invention provides compositions for oral administration
that includes caffeine, a xanthine compound other than caffeine
and ginkgo biloba; caffeine, a xanthine compound other than caffeine,
and glutamic acid or ester or salt thereof; caffeine, a xanthine
compound other than caffeine, and niacin or derivative thereof;
caffeine, a xanthine compound other than caffeine and acetyl-L-carnitine;
caffeine, a xanthine compound other than caffeine and dimethylaminoethanol;
caffeine, a xanthine compound other than caffeine, and an amino
acid or ester or salt thereof; caffeine, a xanthine compound other
than caffeine, and L-phenylalanine; caffeine, a xanthine compound
other than caffeine, and choline or a salt thereof; caffeine, a
xanthine compound other than caffeine, and glycine or ester or salt
thereof; caffeine, a xanthine compound other than caffeine, and
aspartic acid or ester or salt thereof; caffeine, a xanthine compound
other than caffeine, and squalane; caffeine, a xanthine compound
other than caffeine, and squalene; caffeine, a xanthine compound
other than caffeine, and pregnenolone; caffeine, a xanthine compound
other than caffeine, and dehydroepiandrosterone; caffeine, a xanthine
compound other than caffeine, and dehydroepiandrosterone-3-sulfate.
In one embodiment, the xanthine compound other that caffeine is
theophylline. In another embodiment, the niacin or derivative thereof
is xanthinol nicotinate. In still another embodiment, the glutamic
acid or ester or salt thereof is pyroglutamate. In yet a further
embodiment of the invention, the afore-listed compositions contain
only the mentioned compounds as active ingredients.
[0077] Blood Sugar Regulation Composition
[0078] The second separate composition is a nutritional protein
supplement composition that includes long chain inulin and water
soluble chromium compound for the regulation of blood sugar. It
should be noted that water-soluble chromium containing compounds
are far more effective in regulating blood sugar than standard non-water
soluble chromium containing compounds, such as chromium picolinate.
The preferred chromium containing compositions used in the present
invention are chromium arginate and/or chromium chelidamate. The
two chromium compounds noted above have the unique property of being
water-soluble thereby making them considerable more bio-available
than other chromium preparations.
[0079] It should be noted that if the diet is supplemented with
a substance that enhances oxygen uptake, metabolic rate is not effectively
decreased. Therefore weight loss proceeds at a more rapid and sustained
pace than would otherwise be the case with either the oxygen containing
composition alone or diet alone. A protein supplement composition
with blood sugar regulating components is a novel addition to the
first separate composition comprising either a xanthine composition
or an ephedra based thermogenic compositions. It comprises a protein
source, such as soy protein, whey protein, egg albumin protein,
and the like. Preferably the protein supplement composition further
comprises additional components such as inulin, L-methionine, MCT
oil (a medium chain triglyceride oil, which is caprylic/caproic
acid). Such components are administered to warm-blooded animals
in need thereof in an amount sufficient to regulate blood sugar
level and/or stabilize the mood of the animal. The preferred inulin
used is a long chain derivative of chicory root with a molecular
weight exceeding ten thousand. Compositions with these ingredients
have been proven to be effective in regulating blood sugar in doses
of anywhere between one and five grams per serving.
[0080] The second composition comprises inulin in addition to the
source of protein. Inulin is a non-absorbable, non-nutritive carbohydrate
that may be derived from natural sources, such as dahlia tubers,
Jerusalem artichoke, or chicory root, or it may be synthesized.
Prior to the isolation and purification of insulin, inulin was historically
used by physicians and American Indians to regulate blood sugar
levels in diabetic patients. To achieve a modicum of therapeutic
regulation, a dosage of between 25 and 50 grams per day of inulin
was required. These exceedingly large dosages have effectively precluded
the usefulness of inulin administration for blood sugar regulation.
Since that time, because of its unique non-absorbability it has
been used to accurately determine renal clearance rates in normal
and pathological states. Inulin is a complex carbohydrate consisting
of beta-linked fructose subunits that may be represented by the
formula (C.sub.6H.sub.12O.sub.5).sub.n where n represents the number
of fructose subunits in the carbohydrate and is indicative of the
degree of polymerization. In the practice of the present invention,
inulin with a degree of polymerization between 8 and 65 is preferred.
In a more preferred embodiment, the inulin has a degree of polymerization
between 15 and 45. Inulin is present in the compositions of this
invention in an amount ranging from 10 to 99 percent by weight of
the total composition, and preferably from 30 to 99 percent by weight
of the total composition and the dosage range should be 200-800
mg.
[0081] Although not intending to be limited to the following theory,
inulin, as a component of the composition of the present invention,
serves to catalytically stimulate the 2,6, bisphosphate energy system.
This, in turn, enhances and modifies glycogenolysis. Specifically,
it is suspected that glycogen synthase a and glycogen phosphorylase
b, which are not phosphorylated, in the presence of sufficient inulin
behave as though they are phosphorylated. It is well known that
the phosphorylation process is an active confirmation process that
activates the catabolic enzymes that lead to glycogenolysis. Therefore,
in the presence of inulin, glycogen stores will be utilized more
efficiently. There is an interesting side effect that develops as
a result of this process, to a greater extent than normal, carbohydrates
are prevented from turning into storage fat.
[0082] The second compositions of the present invention, which
contain inulin and a protein source are effective in regulating
blood sugar levels at significantly lower dosages by virtue of the
apparent synergistic affect of the other non-inulin composition
components. These include certain metal complexes, as well as supplemental
methionine. In the practice of the present invention, the dosage
of inulin needed to effect blood sugar regulation ranges from about
50 micrograms (tg) to no more than about 10 grams of inulin per
subject per day, and preferably from abut 1 gram to about 5 grams
of inulin per subject per day.
[0083] As mentioned above, the inulin compositions of the present
invention may include one or more metal complexes. The metal complex
is present in the composition in an amount ranging from 0.01 to
20 percent by weight of the total composition, and preferably from
0.01 to 5 percent by weight of the total composition. These metal
complexes, in conjunction with inulin, effect blood sugar regulation.
Suitable metal complexes include metal complexes of chromium, manganese,
and vanadium. As used herein, the term "complex" refers
to any organic or inorganic ligated metal species.
[0084] While metal complexes alone generally have at least some
capacity to effect blood sugar levels and improve glucose tolerance,
the combination of inulin (in the amount disclosed above) and the
metal complexes provide a composition that effects blood sugar level
regulation significantly greater and at a much lower concentration
that administration of either inulin or the individual metal complexes
alone. Thus, the metal complexes are essential components of the
compositions of the present invention.
[0085] For example, chromium is known to have some effect on glucose
metabolism. These include, 1. Lowering blood levels of low density
lipoproteins, 2. Raising high density lipoproteins, 3. Ability to
modulate reactive hypoglycemia and 4. Modify exercise induced hypoglycemia.
All of these effects are adequately documented. The effect of chromium
on glucose metabolism was recognized as early as 1929 with the discovery
that yeast extracts potentiated the effect of insulin and it is
thought that a majority of the American public is chromium deficient.
Seemingly, chronic chromium deficiency may be associated with an
enhanced tendency towards atherosclerosis. In the presence of optimal
amounts of biologically active chromium, much lower amounts of insulin
are required. From an athletic point of view, this is a major advantage.
Exercise can thus be conducted at higher intensity levels for longer
periods of time before the induction of hypoglycemic fatigue. Several
U.S. patents have disclosed the ability of chromium picolinate to
influence blood sugar and insulin output (U.S. Pat. Nos. 5,164,384
and 4,315,927). In addition, it has been determined that the ability
of mammalian tissue to absorb chromium decreases with age (see.,
e.g., Schroeder, The Trace Elements and Man, Devin-Adair, pub.,
Old Greenwich, Conn., 1977), and may explain, in part, maturity
onset diabetes and its prevalence in humans after the age of 50.
[0086] Furthermore, some chromium complexes are known to have biological
activity, including chromium trichloride, chromium acetate, chromium
nicotinate (the active component of the metallovitamin, Glucose
Tolerance Factor, isolated from yeast), chromium picolinate, chromium
glycinate, chromium oxalate, chromium perchlorate, chromium salicylate,
and chromium-4-oxo-pyridine-2, 6-dicarboxylate. Chromium is also
a dietary requirement and chromium dietary requirements in humans
range from about 50 to 200 .mu.g per day.
[0087] Like chromium, manganese also improves glucose tolerance.
Historically, glucose intolerance resulting from manganese deficiency
was demonstrated in 1958. More recently, the importance of manganese
in the diets of humans was demonstrated by Schroeder in 1966 (Schroeder
et al., J. chronic Diseases 19:545-71, 1966). Although not formally
listed as a required nutrient, manganese requirements in humans
have been determined to be between 3 and 4 mg per day. Although
manganese is poorly absorbed, the ability to absorb manganese does
not decrease with age. The dietary dosage of manganese ranges from
2 to 100 mg per day.
[0088] Vanadium also effects blood sugar regulation and has recently
been classified as an essential trance mineral. Vanadium complexes
have been used in therapeutic applications including the treatment
of diabetes. Vanadium is poorly absorbed and dietary intake ranges
from about 2 to 15 mg per day. Because vanadium is poorly absorbed
and its numerous complexes are extremely toxic, few vanadium complexes
have been demonstrated to possess biological activity.
[0089] The chromium complexes of the present invention include
organic and inorganic chromium complexes such as chromium acetate,
chromium chloride, chromium potassium oxalate, and chromium potassium
sulfate. In a preferred embodiment, the chromium complex is chromium
picolinate. In a particularly preferred embodiment, the chromium
complex is chromium-4-oxo-pyridine-2,6-dicarboxylate.
[0090] The manganese complexes of the present invention include
manganese acetate, manganese chloride, manganese carbonate, potassium
permanganate, dimanganese trisulphate, manganese gluconate, manganese
glycinate and manganese citrate. In a preferred embodiment, the
manganese complex is manganese gluconate or manganese glycinate.
[0091] Like the chromium complexes, the vanadium complexes include
organic and inorganic vanadium complexes such as vanadium carbonyl,
vanadium pentoxide, vanadium trisulfate, vanadyl dichloride, and
vanadyl trichloride. Various organic vanadium complexes may also
be used in the composition of the present invention. Examples of
organic vanadium complexes include vanadyl glycinate, vanadyl gluconate,
and vanadyl citrate. In a preferred embodiment, the vanadium complex
is vanadyl sulfate (VSO.sub.5).
[0092] The second compositions of the present invention optionally
include medium chain triglycerides. As used therein, the term "medium
chain triglyceride" ("MCT") refers to a triester
of glycerol containing medium length chain carboxylic acids. Medium
length chain carboxylic acid chains are C.sub.6 to C.sub.12 carboxylic
acids. The three medium chain carboxylic acids that are attached
to the triglyceride backbone of the MCT may be, but need not be,
the same. The medium chain carboxylic acids can be either saturated
or unsaturated, but are preferably saturated. This unique fat in
many respects behaves like a carbohydrate. It is absorbed directly
into the splenic protal circulation where it is shuttled directly
to the liver as free fatty acids bound to albumin. These medium-sized
free fatty acids are preferentially oxidized to Acetyl-CoA, which
can immediately enter appropriate bio-energetic pathways, especially
the Krebs cycle. This is obviously advantageous in an energy depleted
or active exercise state. Further, there is evidence that MCT's
contributed to the stabilization of blood glucose during exercise.
This supports the premise that excess energy as MCT is not stored
with any degree of efficiency. In fact, a number of studies indicated
that long-term feeding of MCT's at fairly high doses will paradoxically
decrease plasma lipids and reduce fat deposition and body weight.
Medium chain triglycerides are GRAS and have been used for more
than 40 years in the feeding of premature infants both intravenously
and orally.
[0093] Examples of medium chain carboxylic acids of this invention
include C.sub.6 (capric acid), and C.sub.12 (lauric acid). As mentioned
above, the MCT may bear one or more different carboxylic acid chains.
In preferred embodiments, the MCTs comprise a mixture of from about
60% C.sub.8 and about 40% C.sub.10 to a mixture of abut 75% C.sub.8
and abut 25% C.sub.10. Odd numbered chains, such as C.sub.7, C.sub.9,
and C.sub.11 fatty acids, are less common, but are included within
the scope of this invention. Further, the MCTs of the present invention
may include minor amounts of short or long chain fatty acids. The
medium chain tridgycerides are used in the present invention to
reduce cravings for simple sugars that would otherwise increase
insulin secretion. The medium chain triglyceride is optionally present
in the composition in an amount ranging from 0 to 90 percent by
weight of the total composition, and preferably from 0 to 67 percent
by weight of the total composition.
[0094] In addition to the heating substances and protein, inulin,
mineral complexes and MCT oil, the second composition may further
include an amino acid selected from L-methionine, D-phenylalanine,
glycine, and mixtures thereof. Preferably, the amino acid is L-methionine,
a primary amine, and formed in high concentration in legumes. L-methionine
is believed to selectively affect the appetite control center in
the septal region of the hippocampus, resulting in a perception
by the brain of significant food intake, and thereby producing a
sensation of satiety. This presumably is due to the fact that methionine
is the scarcest of all of the essential amino acids in food. D-phenylalanine
is known to increase endorphin levels in the body and, since endorphins
are released after a large meal, it is believed to contribute to
a feeling of satiety. Glycine stimulates the release of glucagon,
which raises blood glucose levels that have fallen too low. This
aids in the prevention of overeating by those with hypoglycemia
(low blood sugar). Thus, the presence of one or more of these amino
acids in the composition imparts further advantages relating to
appetite suppression. Preferably, the amino acid is present in the
appetite suppressant composition in an amount ranging from 5 mg
to 2000 mg.
[0095] A first example formulation of the Protein Composition and
Blood Sugar Regulating Composition according to the present invention,
with ranges of ingredients is noted below:
4 Ingredient Wt. % Range (%) 1. Soy Protein 89 10-99 2. Inulin
4 0.01-20 3. L-Methionine 0.2 0.01-20 4. MCT oil 3.0 0-10 (medium
chain Triglyceride 5. Vanilla Flavoring 0.3 0-10 6. Sucralose 0.2
0-10 7. Carboxymethyl Cellulose 0.8 0-20 8. Carrageenan 0.4 0-20
9. Magesium Phosphate 1.198 0-30 10. Chromium Arginate 0.001 0-5
11. Chromium Chelidamate 0.001 0-5 12. Glycine 0.2 0.01-20 13. Vanadyl
Sulfate 0.2 0.001-10 14. Manganese gluconate 0.2 0.001-10
[0096] In addition to the above-identified ingredients, the composition
may contain optional ingredients. On optional ingredient is a stimulant,
which is not one of the above-mentioned ingredients. In general,
materials known to have a stimulatory effect are well known in the
art, and any of these materials may be present in the composition
of the invention. An exemplary stimulant is phenethylamine.
[0097] In another aspect of the present invention, a method for
regulating blood sugar levels is disclosed. The method provides
for the systemic administration of the compositions of the present
invention in a quantity sufficient to regulate blood sugar levels
in warm-blooded animals. In one embodiment, the inventive formulation
of the present invention are administered to a warm-blooded animal
in an oral form. When formulated as capsules, the inulin composition
is preferably administered one to three times a day. While the oral
dosage may contain from 100 mg to 6000 mg (e.g., total weight of
all active ingredients), a single tablet or capsule containing more
than about 1000 mg may be too large to easily swallow. Thus, the
inventive formulation may be administered in either multiple capsule,
multiple tablet form, powders, or a ready to drink beverage. In
addition, The total weight of all active ingredients will depend
on the form of ingredients used.
Test Results
[0098] During the course of the study reported herein, all individuals
had a morning and afternoon meals consisting of the high protein
blood sugar regulating composition and an orange or an apple. In
the evening they were instructed to eat a standard meal but to limit
their intake of refined carbohydrates such as bread and rice. Upon
arising and at 2:00 p.m. all participants took two capsules containing
either the ephedra based or non-ephedra based anorectic broncho-dilator
as noted by the formulas given above. In total, there were five
different formulations administered to the individuals: 1. A composition
containing a xanthine; 2. A composition containing the protein supplement
and blood sugar regulator; 3. Both a xanthine containing composition
and a protein supplement with blood sugar regulator; 4. A composition
containing Ephedra, xanthine, and coleus forskholii; and 5. A composition
containing Ephedra, xanthine, and coleus forskholii and the protein
supplement with blood sugar regulator.
[0099] For the purpose of all experiments reported herein, individuals
were given servings of two ounces of the protein composition in
water, two times per day. Obviously, one skilled in the art could
generate compositions that would be in solid forms such as bar or
gel form that would be equally effective. This does not alter the
spirit or the effect of the invention.
[0100] FIG. 1 shows the average weight lost (in pound) using a
xanthine containing composition. This composition showed an initial
3 pound weight loss in the first week, that tapered down at about
2.15 pounds lost at the fourth week.
[0101] FIG. 2 shows the average weight lost (in pounds) using a
protein supplement composition containing a blood sugar regulator.
This formulation also showed an initial weight loss of 3 pounds
in the first week, with the average tapering down to about 2.25
pounds by the fourth week.
[0102] FIG. 3 shows the average weight lost (in pounds) using a
xanthine containing composition and a protein supplement composition
containing a blood sugar regulator. As can be seen from the figure,
the initial weight lost in the first week was double that of the
separate compositions individually, at 6 pounds. Further, this weight
loss tapered down to about 4.25 pounds, still greater than that
of the initial weight loss of the separate compositions and approximately
twice that at the fourth week. This surprising and unexpected result
supports the utility of the present invention.
[0103] FIG. 4 shows the average weight lost (in pounds) using a
composition containing Ephedra, Xanthine, and coleus forskholii.
This composition performed better than the xanthine containing composition
and protein supplement compositions, but not as well as the combination
of the two. This formulation showed an initial weight loss of 3.5
pounds in the first week, which tapered off to about 2.5 pounds
in the fourth week.
[0104] FIG. 5 shows the average weight lost (in pounds) using a
composition containing ephedra, xanthine, and coleus forskholli
and a protein supplement composition with a blood sugar regulator.
This formulation showed the best results. There was a 7 pound initial
weight loss that tapered of to about 4.5 pounds in the fourth week.
[0105] These figures clearly illustrate that the combination of
a xanthine containing composition and a protein supplement composition
containing a blood sugar regulator show surprising and unexpectedly
superior results in weight loss experienced by the using individuals.
Further, these figure clearly show that while coleus forskholii
clearly improves the performance of the xanthine containing composition,
it affects a greater improvement on the ephedra-xanthine formulations.
[0106] More importantly, FIG. 6 shows the average total weight
loss of the five formulations. This figure clearly illustrates that
total weight loss is benefited by combining a xanthine containing
composition, according to the present invention, and the protein
supplement with blood sugar regulator, according to the present
invention. In both formulations using the combination, there was
approximately a doubled weight loss experience than that experienced
using any formulation that did not have the combination. Weight
loss totals when the ephedra and protein where used together exceeded
twenty pounds in the space of four weeks. The xanthine composition
and protein exceeded nineteen pounds in four weeks. This is a very
substantial weight loss in a very short period of time. This is
important and exciting since it was wholly unexpected and surprising.
[0107] It is obvious in reviewing the data that this approach to
weight loss is extremely novel especially as regards the anxiety
commonly associated with weight loss. It could therefore be assumed
that such an approach would have a more successful long term result
since compliance would be so much greater. An individual that is
not anxious while losing weight with a calorie deprivation approach
is far more likely to continue on such a program.
[0108] Additionally, while the FEV average in 10 subjects before
and after using a xanthine containing composition showed an increase
in FEV (before=3.51 l; after=4.21 l; as 17% increase in FEV); the
FEV average in 10 subjects before and after using a composition
containing ephedrea, xanthine, and alpha adrenergic stimulants showed
a greater increase (before=3.35 l; after=4.3 l; a 22% increase in
FEV). The FEV measurement were performed using standard spirometry
techniques as noted in Diagnosis of Diseases of the Chest by Fraser
and Pare', vol. 1, p. 319-332. Measurements were done before and
1.5 hours after administration of the compositions.
[0109] What is equally interesting, is the patients where given
the Hamilton Anxiety Scale test prior to and following the four
weeks test of this composition, see FIG. 7. In each case there was
no difference noted statistically between the scores in patients
prior to the diet as contrasted with after the diet. As previously
noted, anxiety and depression result in excessive appetite. The
fact that people were not anxious when on this approach indicates
that it would be useful on long-term bases for those that required
it. Rapid weight loss due to any condition produces a certain degree
of discomfort and therefore anxiety. Generally speaking it is well
known in the art that all anorectic agents that increase sympathetic
zone; i.e. are broncho-dilators will inherently induce anxiety.
Likewise, weight loss associated with calorie deprivation will invariably
induce anxiety.
[0110] The Hamilton anxiety rating scale examination was administered
at the beginning of the study and weekly thereafter for 4 weeks.
The scores were averaged among the 20 individuals and the results
were surprising and unexpected. To this end twenty five individuals
were examined by a board certified psychiatrist and given the Hamilton
Anxiety Rating Scale (see e.g. Comprehensive Textbook of Psychiatry,
Kaplan, Freedman, and Sadock, ed. Williams & Wilkins, pub.,
Baltimore, Md.) In the Hamilton Anxiety Rating, a score of 0-10
is within normal limits, 10-20 indicates a potential need for counseling
or other intervention, while a score greater than 20 indicates a
potential need for pharmaceutical intervention. Five of the individuals
were removed from the study because of a pre-existing psychiatric
condition. The remaining 20 were divided into 2 groups of 10 each.
Ten were put into the group that did the high protein blood sugar
regulating composition and the ephedra based anorectic broncho-dilating
agent. The other 10 were placed on the high protein blood sugar
regulating composition in conjunction with an anorectic broncho-dilator
that was not ephedra based.
[0111] As can be seen from FIG. 7, the performance of the high
protein blood sugar regulating composition in conjunction with an
anorectic broncho-dilator that was not ephedra based showed little
overall reduction in anxiety until the last week of the test. The
performance of the high protein blood sugar regulating composition
and the ephedra based anorectic broncho-dilating agent, on the there
hand, showed a demonstrable decrease in anxiety during use, with
the most marked decrease during the last week of the test. This,
however, was attributed to gratification due to the substantial
amount of weight lost with minimal effort. At no time was there
a significant increase in anxiety among any of the subjects that
would require counseling or pharmaceutical intervention. In no case
was an exercise program of any sort recommended to the study participants.
[0112] The active ingredients in the inventive compositions can
be administered as a mixture thereof, or in combination with one
or more pharmaceutically acceptable inert materials, binders, carriers
or excipients, collectively referred to as adjuvants. Thus, the
composition may contain binders such as microcrystalline cellulose,
gum tragacanth or gelatin; excipients such as starch or lactose;
carriers such as sucrose, kaolin, glycerin, starch dextrins, sodium
alginate, carboxymethylcellulose and ethyl cellulose; disintegrating
agents such as alginic acid, Primogel, corn starch and the like;
lubricants such as magnesium stearate or Sterotex; and glidants
such as colloidal silicon dioxide. When the dosage unit form is
a capsule, it may contain, in addition to materials of the above
type, a liquid carrier such as polyethylene glycol or a fatty oil.
Other dosage unit forms may contain other various materials that
modify the physical form of ht dosage unit, for example, as coatings.
Thus, tablets or ills may be coated with sugar, shellac, or other
enteric coating agents. Materials used in preparing these various
compositions should be pharmaceutically pure and non-toxic in the
amounts used.
[0113] The inventive formulation of the present invention may be
administered systemically. Accordingly, the inventive formulation
may be formulated for oral as well as injectable administration.
In the case of oral administration, the inventive formulation of
this invention may be manufactured by combining all ingredients
in a form suitable for oral administration, and preferably as a
pill, capsule or tablet. For example, the inventive formulation
of the present invention may be encapsulated (such as in a coating
of hard gelatin) for oral administration. The inventive formulation
may be in the form of a wafer of chewing gum. Such techniques are
well known in the art (see, e.g., Baker, Richard, Controlled Release
of Biologically Active Agents, John Wiley & Sons, 1986). Inert
fillers may also be present in the oral (e.g., tablet or capsule)
form, in which case a powdered form may be preferred. Suitable inert
fillers include magnesium stearate and silicon dioxide. The inert
fillers may be present in the inventive formulation of the invention
up to less than 3 percent by weight of the total composition.
[0114] Alternatively, the inventive formulation may first be combined
with one or more suitable carriers or diluents to yield a pharmaceutical
preparation suitable for oral or parenteral application. Such diluents
or carriers, however, should not interact with the mood stabilizing
composition to significantly reduce the effectiveness thereof. Suitable
carriers for parenteral application (such as intravenous, subcutaneous
or intramuscular injection) include sterile water, physiological
saline, bacteriostatic saline (saline containing 0.9 mg/ml benzyl
alcohol) and phosphate-buffered saline.
[0115] The inventive formulation may be a liquid, such as an elixer,
suspension or syrup. In any case, the inventive formulation may
be formulated to have a pleasant taste, or it may be coated so that
it has essentially no taste. For example, sweetening agents such
as sucrose or saccharin may be added or a flavoring agent such as
peppermint, methyl salicylate or orange flavoring. Coloring agents,
e.g., dyes may also be present.
[0116] The inventive formulation may be administered to achieve
a variety of beneficial effects. Thus, the inventive formulation
may serve as a stimulant, to increase cerebral cortical activity,
to elevate mood, to enhance short-term memory, to provide increases
in musculature relative to adipose tissue and enhance athletic performance,
and decreases in appetite. These beneficial effects are discussed
further below.
[0117] It has been surprisingly found that the inventive formulation
provide a sustained and noticeable stimulant effect far beyond that
typically observed upon ingestion of an equivalent amount of caffeine
or second xanthine compound alone. The inventive formulation is
therefore also directed to a method of employing the inventive formulation
of the invention to enhance cerebral cortical activity and thereby
provide a stimulatory effect. Thus, the invention provides a method
for enhancing cerebral cortical activity in a subject in need thereof.
A "subject in need thereof" may be a warm-blooded animal
who has been diagnosed to have attention deficiency disease. According
to the method, an effective amount of the inventive formulation
as described above is administered to a subject in need of enhanced
cerebral cortical activity. Furthermore, the inventive formulation
affords this stimulant effect with an amelioration of the diffuse
chronic depolarization and subsequent cortical depression commonly
associated with stimulants alone. Accordingly, methods for enhancing
cerebral cortical activity while ameliorating the diffuse chronic
depolarization and subsequent cortical depression commonly associated
with stimulants alone is provided by the present invention.
[0118] It has also been surprisingly found that the inventive formulation
may afford substantial enhancements in short term memory as compared
with caffeine alone. The invention is therefore also directed to
a method of employing the inventive formulation to aid short term
memory recall. Thus, the invention provides a method for enhancing
the short term memory of a subject in need thereof, comprising oral
administration to the subject of an effective amount of a composition
of the invention as described above. This is particularly important
in preserving functionality while individuals are experiencing calorie
deprivation.
[0119] In a preferred embodiment, the inventive formulation contains
a biosynthetic precursor to a neurosteroid. When the inventive formulation
contains a biosynthetic precursor to a neurosteroid, it is particularly
preferred to administer such a composition to a subject in need
of increased in muscular development and athletic performance, and/or
decreased in appetite.
[0120] It has also been surprisingly found that the inventive formulation
causes a significant reduction in the appetite of an overweight
person who consumes the composition. Overweight person who consume
the inventive composition experience weight loss because their caloric
consumption decreases as their interest in food is reduced. The
inventive formulation is therefore useful for weight reduction and
long-term weight management. Thus, the invention provides a method
for achieving weight reduction comprising administering to a subject
in need thereof an effective amount of the inventive formulation
as described above.
[0121] In a further aspect of this invention, a method for stabilizing
mood is disclosed. This method provides for the systemic administration
of the compositions of the present invention in a quantity sufficient
to stabilize mood in warm-blooded animals. In one embodiment, the
compositions are orally administered to warm-blooded animals. The
oral administration of a composition of the present invention for
mood stabilization is described in more detail above.
[0122] The term "effective amount" refers to an amount
that is effective, upon single or multiple dose administration to
the subject, in providing one or more effects as described herein.
In determining the effective amount or dose, a number of factors
are considered by the attending diagnostician, including, but not
limited to: the species of mammal; its size, age, and general health;
the specific goal desired; the severity of the problem being experienced
by the subject; the responsiveness of the individual subject or
the treatment; the particular composition administered; the bioavailability
characteristics of the preparation administered; the dose regimen
selected; the use of concomitant medication; and other relevant
circumstances.
[0123] The preferred embodiment of the invention is described above
in the Figures and Description of Preferred Embodiments. While these
descriptions directly describe the above embodiments, it is understood
that those skilled in the art may conceive modifications and/or
variations to the specific embodiments shown and described herein.
Any such modifications or variations that fall within the purview
of this description are intended to be included therein as well.
Unless specifically noted, it is the intention of the inventor that
the words and phrases in the specification and claims be given the
ordinary and accustomed meanings to those of ordinary skill in the
applicable art(s). The foregoing description of a preferred embodiment
and best mode of the invention known to the applicant at the time
of filing the application has been presented and is intended for
the purposes of illustration and description. It is not intended
to be exhaustive or to limit the invention to the precise form disclosed,
and many modifications and variations are possible in the light
of the above teachings. The embodiment was chosen and described
in order to best explain the principles of the invention and its
practical application and to enable others skilled in the art to
best utilize the invention in various embodiments and with various
modifications as are suited to the particular use contemplated.
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