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Weight Loss Patent Abstract
This invention discloses a new and unique combination of Dahurian
Angelica Root extract, Polygonum multiflorum extract, Theobroma
cocoa extract, Yerba mate extract, Oolong tea extract, Kohki Tea
extract, Horse Chesnut extract, and Ligustrum Lucidum extract useful
as a dietary supplement for increasing weight loss in humans.
Weight Loss Patent Claims
5. A weight loss method comprising administering a composition of
matter comprising Angelica Dahurica (Fisch ex Hoffm.) Benth et.
Hook f. and Polygonum cuspidatum Sieb. et Zucc. in amounts effective
to promote weight loss.
6. The composition according to claim 5, which further comprises
Theobroma Cacao L., llex Paraguayensis, Camellia sinensis (L.) Kuntze
or Engelhardtia chrysolepis.
7. The composition according to claim 5, which further comprises
Aesculus Hippocastanum L. or Ligustrum Lucidum.
8. A weight loss method comprising administering a composition
of matter comprising imperatorin and emodin in amounts effective
to promote weight loss.
9. The composition according to claim 8, which further comprises
theobromine, caffeine, mate saponin, caffeic acid, polyphenols,
catechins, astibilin or taxifolin.
10. The composition according to claim 8, which further comprises
escins or oleanic acid.
Weight Loss Patent Description
BACKGROUND OF INVENTION
[0001] Over recent years obesity has reached epidemic proportions.
Obesity contributes to 400,000 deaths each year and according to
federal guidelines, half the population is overweight and a third
is obese. Obesity is defined as an excess proportion of total body
fat correlating with a body weight greater than 20 percent of ideal
body weight (IBW). Body Mass Index (BMI) is another method to determine
whether or not an individual is obese. BMI is calculated with an
equation consisting of weight and height measurements in order to
determine total body fat. A BMI between 25-29.9 indicates an individual
is overweight. Causes for obesity include genetic, environmental,
economic, emotional, and physiological factors. These factors can
then lead to the over consumption of total calories. The amount
of total calories consumed versus the amount of total calories burned
determines the amount of fat stored for energy reserves. Calories
or Kcals (kilocalories) are defined as the amount of heat necessary
to raise the temperature of 1 gram of water 1 degree Celsius. The
amount of total calories burned is defined as the calories utilized
by exercise plus basal metabolic rate (BMR) or resting metabolic
rate (RMR). BMR represents the amount of calories needed to maintain
IBW at rest. Increasing BMR results in fewer calories stored as
fat and can promote weight loss if the amount calories burned is
greater than the amount of calories ingested. One of the main factors
that controls BMR is the percentage of lean body weight.
[0002] Standard medical therapy for obesity includes oral prescription
medications. Most of these medications are designed to regulate
appetite by releasing serotonin or catecholamine. For instance Sanorex,
Mazanor, Adipex-P, and Meridia are common appetite suppressant medications.
However most of these medications can only be used on a short-term
basis and are scheduled as controlled substances due to the fact
that they can become addictive. Other side effects include increased
heart rate, blood pressure, constipation and insomnia. Merida is
the only appetite suppressant that has been approved for long-term
use. Another long-term pharmaceutical approach to weight loss is
the fat absorption inhibitor Xenical. Xenical works by blocking
about 30 percent of dietary fat from being absorbed. Enzymes in
the digestive system, called lipases, assist in the digestion of
dietary fats. Xenical attaches to the lipases and inhibits the digestion
of dietary fat as triglycerides into absorbable free fatty acids
and monoglycerides, which are then excreted in the bowel. Xenical
literature recommends not ingesting more than 30 percent of total
calories from dietary fat per day due to concerns regarding loose
bowels. It appears that a common and unpleasant side effect of Xenical
includes flatulence and loose bowels when consumed with a high fat
diet.
[0003] U.S. Pat. No. 5,422,352 to Arne Astrup relates a method
for a slimming pharmaceutical composition. This invention represents
an improvement in standard pharmaceutical weight loss medications
due to its non-addictive properties. The use of ephedrine and caffeine
has been documented as an effective weight loss preparation. Ephedrine
and caffeine produce a thermogenic response and decrease appetite
by stimulating the release of catecholamines. Ephedrine is categorized
as a sympatomimetic compound, which utilizes the adrenergic alpha
and beta-receptors, involved in the release of the catecholamines.
Since ephedrine is not a selective beta agonist it stimulates all
of the main beta receptors (beta1, beta2, and beta3) resulting in
the stimulation of metabolic rate, blood pressure, and heart rate.
Although this increase in blood pressure and heart rate is less
than ideal in number of individuals.
[0004] U.S. Pat. No. 6,316,499 to Dennis Jones relates a method
for increasing muscle mass of a human with materials derived from
citrus varieties. This invention represents an improvement in standard
pharmaceutical and dietary supplement weight loss products due its
natural origin and non-addictive properties. Citrus Aurantium contains
several alkaloids including hordenine, octopamine, tyramine and
N-methyltyraminesynephrine and synephrine as the principal alkaloid.
These alkaloids are thought to be beta selective and only stimulate
the beta 3 receptor, which is responsible for metabolic rate. This
represents an improvement in weight loss therapies. However, depending
upon the dose, these alkaloids can stimulate the alpha receptors,
which are partly responsible for blood pressure. According to this
patent citrus varieties containing these alkaloids can also be used
to promote muscle mass in humans when combined with a high protein
diet and weight training program. Although while this may be an
improvement in standard pharmaceutical weight loss therapy it is
still less than desirable due to the possible increase in blood
pressure.
[0005] U.S. Pat. No. 5,804,596 to Muhammed Majeed et al. relates
a method of preparing forskohlin composition from forskohlin extract
and use of forskohlin for promoting lean body mass and treating
mood disorders. This invention represents a further improvement
in standard pharmaceutical and dietary supplement weight loss products
due to the fact that it is naturally derived, non-addictive, and
a non-stimulant. Forskohlin extract is derived from the Coleus Forskoli
plant and a method for this extraction is described. Forskohlin
stimulates noradrenaline production, which in turn stimulates the
beta adrenergic receptors to produce adenyl cyclase. Adenyl cyclase
is responsible for the promotion cAMP (cyclic adenosine monophosphate),
which in turn activates protein kinase to phosphorylate HSL (hormone
sensitive lipase) for the release of fatty acids from adipose tissue.
The increase in cAMP is thought to correspond to enhancing the thermogenic
response to food thus improve absorption of nutrients and their
incorporation into lean body mass. The increased release of fatty
acids and the increase in lean body mass contribute to shifting
of the lean body mass/adipose tissue ratio in favor lean body mass
for the regulation body weight. Forskohlin also restores the level
of monoamines for presynaptic availability, which has known anti-depressant
action and which may contribute better eating habits. However, these
actions can be easily blunted by an insulin response generated from
a meal.
[0006] U.S. Pat. No. 6,531,162 to William Llewellyn relates to
a non-stimulant composition and formulation for decreasing body
weight. The combination of octopamine, yohimbine, bergenin, and
decaffeinated green tea extract increases lipolysis, thermogenesis,
and weight loss, and is safe and much less apt to cause the side
effects normally associated with stimulant-based weight loss products.
Octopamine is a naturally occurring catecholamine structurally related
to norephinephrine, and has been proven in in-vitro studies to be
a potent selective beta-3 agonist. Yohimbine is an extremely potent
naturally occurring alpha-2 receptor antagonist. Adrenergic lipolysis
in human adipose tissue is regulated in a dual nature by adrenoceptors.
Studies with Green Tea extract with standardized amounts of EGCG
have suggested it exerts a direct effect on thermogenesis by increasing
the respiration rate of brown fat cells, and furthermore that it
can strongly enhance the lipolytic action of other chemicals or
agents acting on this system. Bergenin has been shown to have an
action in the body that augments the lipolytic action of norepinephrine.
However, while this may be an improvement in weight loss formulations
it is not a truly non-stimulant formula. Octopamine is not a selective
beta 3 agonist but actually an alpha-Adrenergic sympathomimetic
amine, biosynthesized from tyramine in the central nervous system
and platelets and also in invertebrate nervous systems. Yohimbine
is also known to increase blood pressure so when combined with octopamine
it can result in strong stimulant activity.
SUMMARY OF INVENTION
[0007] This invention discloses a new and unique combination consisting
of Dahurian Angelica Root extract, Polygonum multiflorum extract,
Theobroma cocoa extract, Yerba mate extract, Oolong tea extract,
Kohki Tea extract, Horse Chesnut extract, and Ligustrum Lucidum
extract useful as a dietary supplement for increasing weight loss.
The problem of the present invention is to provide a composition
that decreases body weight with out any of the previously mentioned
negative side effects associated with pharmaceutical or nutraceutical
compositions. According to the invention these problems are solved
by the use of a carefully blended composition containing Dahurian
Angelica Root extract, Polygonum multiflorum extract, Theobroma
cocoa extract, Yerba mate extract, Oolong tea extract, Kohki Tea
extract, Horse Chesnut extract, and Ligustrum Lucidum extract. Prior
art also discloses these eight compounds of interest to this inventor,
but which heretofore had not been combined to create a new and useful
weight loss product.
DETAILED DESCRIPTION
[0008] This invention discloses the formula sets that embody the
invention of the supplement composition for increasing weight loss
in humans. The combination of Dahurian Angelica Root extract, Polygonum
multiflorum extract, Theobroma cocoa extract, Yerba mate extract,
Oolong tea extract, Kohki Tea extract, Horse Chesnut extract, and
Ligustrum Lucidum extract possess the ability to act as oxidative
uncouplers, nitric oxide, fatty acid synthase and anti-lipolytic
hormone inhibitors.
[0009] The first unique and novel combination is that of Dahurian
Angelica Root extract and Polygonum multiflorum extract. Dahurian
Angelica Root contains natural coumarins or more specifically furanocoumarins
such as imperatorin and psoralen. Furanocoumarins dramatically promote
and initiate lipolysis or fat burning. For instance Yoshiyuki et
al. Planta Med 1982 July 45:3 183-7 has demonstrated the ability
of furanocoumarins to activate the actions of lipolytic hormones
and selectively inhibit the effects of anti-lipolytic hormones such
as insulin. Furanocoumarins have been shown to activate adrenaline
induced lipolysis while at the same time selectively inhibiting
the anti-lipolytic hormone insulin.
[0010] A vital function of furanocoumarins is there ability to
act as oxidative uncouplers. Olorunsogo et al. Chem Biol Interact
1990; 74(3): 263-74 has demonstrated the ability of chalepin, imperatorin
and marmesin to act as oxidative uncouplers. Oxidative phosphorylation
is the formation of adenosine diphosphate to adenosine triphosphate,
which is the primary energy source for many physiological functions.
When uncoupling of this reaction occurs, free energy or heat is
released resulting in a thermogenic response and caloric expenditure.
[0011] Furanocoumarins are inhibitors of the enzyme cAMP phosphodiesterase.
This enzyme is responsible for inhibiting lipolysis or fat burning.
Sadari et al. Pharmazie 1999 Jul. 54(7):554-6 has demonstrated the
ability of furanocoumarins to inhibit cAMP phosphodiesterase and
thus enhance lipolysis.
[0012] Another interesting function of furanocoumarins is their
ability to inhibit nitric oxide production. The inhibition nitric
oxide production has been associated with weight loss in animals.
Interestingly the nitric oxide biosynthetic pathway is thought to
contribute to the regulation of feeding. Inhibition of nitric oxide
causes a decrease in appetite and slows gastric emptying. Wang C
C et al. Cancer Lett 1999 Oct. 18; 145(1-2):151-7 has demonstrated
the ability of furanocoumarins to act as potent nitric oxide inhibitors.
Morely, et al. Life Sci 1992; 51(16): 1285-9, Morely et al. Pharmacol
Biochem Behav 1995 March; 50(3): 369-73, and Plourde V et al. Eur
J Pharmacol 1994 Apr. 21; 256(2): 125-9 clearly demonstrates the
role of the nitric oxide inhibition and weight loss. The use of
furanocoumarins for weight regulation is somewhat of a new application
that has been clearly overlooked for a number of years.
[0013] Polygonum multiflorum contains various hydroxy anthraquinones
and can be standardized specifically for Emodin (3-methyl-1,6,8-trihydroxy-anthraquinone).
Hydroxy anthraquinones are oxidative uncouplers as described by
Betina V et al. Chem Biol Interact 1987; 62:1 79-89. Oxidative uncouplers
inhibit oxidative phosphorylation or the formation of ATP. This
inhibition results heat production and calories burned at rest.
Emodin is a hydroxy anthraquinone that acts as an oxidative uncoupler
and fatty acid synthase inhibitor. The fatty acid synthase enzyme
is involved in the biosynthesis of fat. Emodin has been shown to
inhibit or slow down its activity and thus reduce body fat. According
to Zhang Chongben et al. Chin Med J 2002; 115(7): 1035-1038 emodin
has an inhibition effect on fatty acid synthase, which is dose dependent.
The inhibition of differentiation of 3T3-L1 by emodin might be related
to the blockage of fatty acid synthase activity, because lipid synthesis
is a very important biochemical event that causes the differentiation
of preadipocyte into adipocyte. Emodin has an effect on the differentiation
and proliferation of preadipocyte, as well as on lipid metabolism.
Prior art also discloses these two compounds of interest to this
inventor, but which heretofore had not been combined to create a
new and useful weight loss combination.
[0014] The next combination consists of Theobroma cocoa extract
and Yerba mate extract. This combination functions as a lipolysis
potentiator and gastric emptying inhibitor. Theobroma coca can be
standardized to contain methylxanthines such as theobromine, while
Yerba mate can be standardized to contain caffeine and theobromine
in addition to glycosides and mate saponins. Methylxanthines promote
fat burning via a direct thermogenic response and inhibit the phosphodiesterase
enzyme, which mediates the anti-lipolytic action of insulin. The
amount of methylxanthine found in this invention is minimal and
therefore overcomes the limitations of previous inventions.
[0015] Yerba mate formulations have been shown to decrease body
weight and gastric emptying resulting in fat loss and appetite suppression.
Andersen, T et al. J Hum Nutr Diet. 2001 June; 14(3): 243-50 discloses
a herbal preparation containing yerba mate, that significantly delayed
gastric emptying, reduced the time to perceived gastric fullness
and induced significant weight loss over 45 days in overweight patients
treated in a primary health care context.
[0016] The next unique and novel combination consists of Oolong
tea extract and Kohki tea extract. According to traditional Chinese
belief oolong tea is effective in controlling body weight. Rumpler,
W. et al. J Nutr 2001 November 131:2848-52 has demonstrated the
ability of oolong tea to increase 24 hour energy expenditure in
humans. Oolong tea extract can be standardized to contain polyphenols,
catechins, and caffeine.
[0017] Kohki tea is produced from the leaves of Engelhardtia chrysolepis
(Chinese name, huang-qui) and can be standardized to contain the
dihydroflavonol taxifolin and its glycoside astilbin. Han L K. et
al. J. Nat. Prod. Vol 61 August 1998, P1006-1011, (REF 25) and Motoyashiki,
T. et al. Biol Pharm Bull 1998 May; 21(5): 517-9 show that these
standardized extracts stimulate adrenocorticotrophic hormone induced
lipolysis and inhibit insulin induced lipogenesis from glucose.
Prior art also discloses these two compounds of interest to this
inventor, but which heretofore had not been combined to create a
new and useful weight loss combination.
[0018] The final unique and novel combination consists of Horse
chestnut extract and Ligustrum licidum extract. This combination
delays gastric emptying and glucose absorption and thus results
in appetite suppression and less plasma insulin secretion. Horse
chestnut extract can be standardized to contain escins and Ligustrum
licidum extract can be standardized to contain oleanic acid. Matsuda,
H et al. Eur J Pharmacol 1999 Mar. 5; 368(2-3): 237-43 has demonstrated
the inhibitory effects of the saponin fraction and its principal
constituents, escins Ia, Ib, IIa, and IIb, from horse chestnuts
on gastric emptying. Delaying gastric emptying causes a meal to
leave the stomach and enter the small intestine over a longer period
of time thus increasing satiety. It also slows the digestion of
carbohydrate to glucose resulting in less lipogenic insulin release.
Matsuda, H et al. Chem Pharm Bull (Tokyo). 1998 September; 46(9):
1399-403 has demonstrated the ability of oleanic acid to suppress
the transfer of glucose from the stomach to the small intestine
and by inhibiting glucose transport at the brush border of the small
intestine. Prior art also discloses these two compounds of interest
to this inventor, but which heretofore had not been combined to
create a new and useful weight loss combination.
[0019] It is now believed that one skilled in the art can, using
the following descriptions, can utilize the present invention to
its fullest extent. The following examples illustrate a weight loss
combination and formulation that is safe and that does not cause
any of the previously mentioned negative side effects. The following
examples should not be considered as limitations of the present
invention.
EXAMPLE 1
Weight Loss Combination and Formulation
[0020] 3 capsules contain: [0021] 150 mg Angelica dahurica var.
pai-chih extract (Standardized for 5% imperatorin) [0022] 150 mg
Polygonum multiflorum extract (Standardized for 75% Emodin) [0023]
150 mg Theobroma cocoa extract (standardized for 10% theobromine)
[0024] 150 mg Yerba mate (standardized for 20% caffeine, 7% theobromine,
7% Glycosides, 2% Mate saponin) [0025] 150 mg Oolong Tea extract
(standardized for 40% polyphenol, 20% catechin, and 9% caffeine)
[0026] 150 mg Kokhi tea extract (standardized for 10% astilbin and
taxifolin) [0027] 550 mg Horse Chesnut (standardized for 20% escins)
[0028] 550 mg Ligustrum lucidum (standardized for 98% Oleanolic
Acid) [0029] Excipients include dicalcium phosphate and magnesium
stearate for suitable encapsulation
EXAMPLE 2
Weight Loss Combination and Formulation
[0030] 3 capsules contain: [0031] 300 mg Angelica dahurica var.
pai-chih extract (Standardized for 5% imperatorin) [0032] 300 mg
Polygonum multiflorum extract (Standardized for 75% Emodin) [0033]
150 mg Theobroma cocoa extract (standardized for 10% theobromine)
[0034] 150 mg Yerba mate (standardized for 20% caffeine, 7% theobromine,
7% Glycosides, 2% Mate saponin) [0035] 150 mg Oolong Tea extract
(standardized for 40% polyphenol, 20% catechin, and 9% caffeine)
[0036] 150 mg Kokhi tea extract (standardized for 10% astilbin and
taxifolin) [0037] Excipients include dicalcium phosphate and magnesium
stearate for suitable encapsulation
EXAMPLE 3
Weight Loss Combination and Formulation
[0038] 2 capsules contain: [0039] 300 mg Angelica dahurica var.
pai-chih extract (Standardized for 5% imperatorin) [0040] 300 mg
Polygonum multiflorum extract (Standardized for 75% Emodin) [0041]
150 mg Theobroma cocoa extract (standardized for 10% theobromine)
[0042] 150 mg Yerba mate (standardized for 20% caffeine, 7% theobromine,
7% Glycosides, 2% Mate saponin) [0043] Excipients include dicalcium
phosphate and magnesium stearate for suitable encapsulation
EXAMPLE 4
Weight Loss Combination and Formulation
[0044] 2 capsules contain: [0045] 500 mg Angelica dahurica var.
pai-chih extract (Standardized for 5% imperatorin) [0046] 500 mg
Polygonum multiflorum extract (Standardized for 75% Emodin) [0047]
Excipients include dicalcium phosphate and magnesium stearate for
suitable encapsulation
[0048] The foregoing descriptions of the invention are for illustration
only. Modifications not included in the description, which are obvious
to those skilled in the art, are intended to be included in the
scope of the following claims.
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