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Weight Loss Patent Abstract
A method for promoting weight loss and/or lowering blood glucose
comprises an active material which may be cinnamon, an extract of
cinnamon, or a derivative of a cinnamon extract. The active material
may be utilized in combination with further active ingredients.
Weight Loss Patent Claims
1. A method for promoting weight loss in an animal, said method
comprising: orally administering to said animal a composition comprising
a member selected from the group of: cinnamon, an extract of cinnamon,
a derivative of an extract of cinnamon, and combinations thereof.
2. The method of claim 1, wherein said composition comprises an
extract of cinnamon.
3. The method of claim 2, wherein said extract of cinnamon is prepared
by extracting cinnamon with an aqueous solvent.
4. The method of claim 2, wherein said extract of cinnamon is prepared
by extracting cinnamon with an acidified organic solvent.
5. The method of claim 4, wherein said acidified solvent is acidified
ethanol.
6. The method of claim 2, wherein said extract is a polyphenol.
7. The method of claim 6, wherein said polyphenol is a type A polyphenol.
8. The method of claim 2, wherein said extract is methyl hydroxy
chalcone polymer.
9. The method of claim 1, wherein said composition comprises Cinnulin.
10. The method of claim 1, wherein the step of administering said
composition comprises administering between 1 and 10,000 mg of said
composition.
11. The method of claim 1, wherein said step of administering said
composition comprises administering between 100 and 500 mg of said
composition.
12. The method of claim 1, wherein said composition further includes
a material selected from the group consisting of: chromium picolinate,
green tea extract, gymnema sylvestre, alpha-lipoic acid, green coffee
extract, 7-keto DHEA, evodiamine, oolong tea, caffeine, yohimbine,
hoodia gordonii, glucomannan, magnolia officianalis, phosphatidyl
serine, a carbohydrate blocking agent, and combinations thereof.
13. The method of claim 1, wherein said animal is a mammal.
14. The method of claim 1, wherein said animal is a human.
15. The method of claim 1, wherein said composition is disposed
in a food product.
16. The method of claim 1, wherein said composition is disposed
in a nutritional supplement.
Weight Loss Patent Description
RELATED APPLICATION
[0001] This application claims priority of U.S. Provisional Patent
Application Ser. No. 60/521,885 filed Jul. 16, 2004, entitled "Dietary
Supplements Containing Extracts of Cinnamon and Methods of Using
Same to Promote Weight Loss," which is incorporated herein
by reference.
FIELD OF THE INVENTION
[0002] The present invention is directed to dietary supplements
comprising cinnamon, or extracts thereof or derivatives of the extracts
thereof, and to methods of using these dietary supplements to promote
weight loss, both in humans and animals.
BACKGROUND
[0003] Obesity and Type II diabetes are quickly becoming an epidemic
in the United States. The increased incidence of these conditions
has been attributed to diets characterized by high fat intake and
repeated ingestion of refined foods and sugars, coupled with low
fiber and vegetable intake. Diet, along with the natural aging process,
causes deterioration in the way in which the body metabolizes blood
glucose. When the body cannot properly metabolize blood glucose,
a tendency to store glucose as fat typically occurs. This is one
reason levels of body fat increase with age. There is also a known
link with these conditions to a variety of ailments including heart
disease and hypertension. Similarly, there is a known link between
insulin resistance and increased visceral adiposity. Therefore,
when glucose regulation is out of balance, a greater propensity
for adiposity exists.
[0004] It has long been known that natural and/or synthetic substances
may aid in controlling blood glucose. Such substances act by a variety
of mechanisms. For example, some substances act by mimicking the
effects of endogenous insulin and are therefore capable of replacing
endogenous insulin. Such substances include synthetic insulin injections
such as those which are routinely prescribed to individuals with
Type I diabetes. Other commonly prescribed substances known to mimic
the effects of insulin include the naturally occurring compounds
taurine, 4-hydroxyisoleucine, arginine, and vanadium. Although these
compounds have been shown to work as insulin mimetics by acting
in the body to decrease serum blood glucose levels, they have not
been successfully developed into viable treatments for disorders
of glucose metabolism.
[0005] Still other substances act directly to increase what is
termed insulin sensitivity or glucose tolerance. Glucose intolerance
forces the body to generate additional insulin in an effort to lower
blood glucose. This causes stress on the beta-cells of the pancreas
and is thought to be a key contributor to Type II diabetes. In a
state of glucose intolerance, the body mechanism for disposing of
blood glucose is not functioning at its optimum level and therefore
the system is inefficient. Substances which increase insulin sensitivity
or glucose tolerance by assisting the body in returning to optimal
levels of blood glucose include alpha-lipoic acid, pinitol and myo-inositol.
These substances cannot entirely replace the function of endogenous
insulin, but work at the receptor level alongside endogenous insulin
to increase insulin sensitivity or glucose tolerance. Here, the
action is exerted directly on the Glut-4 receptor of the cell to
trigger the cascade normally caused by insulin that allows for the
reduction in blood sugar via the transport of nutrients into the
cell.
[0006] In the past, chromium was thought to aid in weight loss
by controlling blood glucose and preventing the deposition of fatty
acids. However, its actions were greatly limited and its claims
never came to fruition. Cinnamon, known for its high concentration
of chromium, has also been used for the control of blood glucose.
However, researchers have demonstrated that cinnamon's effects are
not from chromium, but rather from a different class of compounds.
One study by Kahn et al. compared the chromium levels of foods and
spices including cinnamon, and failed to find a correlation between
chromium level and the level of insulin potentiation. (Biological
Trace Element Research, 1990; 24:183-188). A meta-analysis by Althuis
et al. showed no association between chromium and glucose or insulin
concentrations. (Am. J. Clin. Nutr., 2002; 76:148-55). A study by
Broadhurst et al. has demonstrated that cinnamon is a strong potentiator
of insulin in comparison to various other herbs and spices. (J.
Agric. Food Chem., 2000; 48:849-852).
[0007] One particular extract of cinnamon, methyl hydroxy chalcone
polymer (MHCP), shows promising data in the area of glucose control.
A recent study compared the effect of MHCP in 3T3-L1 adipocytes
to that of insulin. (Jarvill-Taylor et al., J. Am. College Nutr.,
2001; 20:327-336). The results from that study support the theory
that MHCP triggers the insulin cascade and subsequent transport
of nutrients. The study also demonstrated that MHCP treatment stimulated
glucose uptake and glycogen synthesis to a similar level as insulin.
The study further demonstrated that treatment with endogenous insulin
and MRCP resulted in a synergistic effect. Due to these conclusions
it is suggested that MHCP may prove to be a very valuable tool in
the fight against diabetes, where insulin is present.
[0008] In addition to benefiting Type II diabetics, cinnamon may
benefit individuals with impaired glucose tolerance (i.e., pre-diabetics).
Further, cinnamon has been shown to possess antioxidant activities
related to lipid peroxidation. (Mancini-Filho et al., Bollettino
Chimico Farmaceutico, 1998; 37:443-47). Cinnamon can be used as
a food antioxidant and to enhance food palatability.
[0009] There exists a need in the art for a safe, effective and
viable method promoting weight loss. Further, there exists a need
in the art for a material which can be incorporated into a pharmaceutical
formulation, a dietary supplement or a food product, whose administration
at normal physiological concentrations would promote weight loss.
BRIEF DESCRIPTION OF THE INVENTION
[0010] Disclosed herein is: (a) a dietary supplement comprising
cinnamon, or an extract thereof or a derivative of the extract thereof
and (b) methods of losing weight and reducing body fat comprising
administration of said dietary supplement.
DETAILED DESCRIPTION
[0011] The body fat reduction and weight loss dietary supplements
of the invention comprise cinnamon, or an extract thereof or a derivative
of the extract thereof. The materials of the present invention are
effective when administered orally; however, intravenous, intramuscular
or transdermal delivery of these materials may also be employed.
The active materials of the present invention may be incorporated
into pharmaceutical preparations. They may also be used in dietary
supplements, and may also be added directly to food products.
[0012] Cinnamon is one of the world's most popular spices. Cinnamon
contains over one hundred different chalcones within it. Chalcones
are a type of polyphenol or flavonoid. These chalcones or polymers
may be extracted from cinnamon and isolated, and, optionally, derivatized.
One class of polyphenols which can be extracted from cinnamon is
the phytochemical Type A polyphenols. In a specific embodiment of
the invention, the dietary supplement includes Type A Polyphenols.
One particular cinnamon derived material having utility in this
invention is methyl hydroxy chalcone polymer (MCHP).
[0013] The isolation of phytochemicals from cinnamon according
to one method having utility in this invention follows the general
process of aqueous extraction followed by centrifugation to remove
non-soluble compounds. In one preparation method, Type A polyphenols
are extracted from cinnamon using the following process: 5 g cinnamon
and 100 ml 0.1 N acetic acid are combined and autoclaved for 15
minutes. The resultant mixture is cooled, then centrifuged and the
precipitate discarded. Four volumes of ethanol/0.1 N acetic acid
are added to the supernatant and the mixture is stored overnight
at 4 C.degree.. The mixture is screened through a filter and then
introduced onto an LH-20 column and washed with 600 ml ethanol/0.1
N acetic acid. The desired fraction is then eluted with a 1:1 mixture
of acetonitrile and 0.2 N acetic acid. The eluant is then concentrated
and introduced onto a HPLC column at 275 nm.
[0014] Another method for producing an extract which may be used
in the practice of the present invention is as follows: [0015] 1.
Choose clean cinnamon bark about 50 g (from Indonesia), grind into
small particles or powder. Regulate the temperature of the grinder.
[0016] 2. Weigh about 20 g ground cinnamon powder into a suitable
flask, mix with 1000 mL distilled water. Leave at room temperature
for about 0.5 hour. The amount of water added to the raw material
for extraction is in a weight ratio of about 1:50. In general, the
range can be from 1 to 1:200. If the ratio is too low (1:20), the
extraction liquid will be very thick, not easy to filter, and the
extraction efficiency is also lower. If the ratio is too high (1:200),
the volume of extraction solution will be much greater resulting
in an increase of drying time. [0017] 3. Heat and stir the cinnamon
liquid on a magnetic heat stirrer. The bioactive polymers in the
cinnamon are relatively heat sensitive. The temperature and extraction
time is crucial to the concentration of the bioactive polymers.
The extraction process should be no longer than one hour. As outlined
below: [0018] a) 15-20 minutes bring to boil while stirring constantly.
[0019] b) 20 minutes boiling and stir constantly. [0020] c) 20-30
minutes simmer stirring constantly after turning down the heat (temperature
is about 80-95.degree. C.). [0021] It is better to control the boiling
time about 20-25 minutes. Move the flask from the heater; after
it cools down, store at 4.degree. C. for overnight. [0022] 4. Filter
the solution through a filter paper to remove any solid debris.
If the solution is too thick to go through the filter paper, centrifuge
can be used for separation. The supernatant can be separated first
with a pipette, then filter the rest of the solution with the medium
speed filter paper. Usually the debris settles to the bottom of
the flask. It is not necessary to filter this debris. [0023] 5.
If the raw material and the water ratio are low, a second extraction
is needed. Add 200 mL distilled water into the residual debris,
mix and heat the solution for 30 minutes at 90.degree. C. Filter
it and mix the first and second extraction solutions together. Note:
The sample and water ratio, heat time, volume of water in second
extraction may vary depending on the amount of the raw material
used for extraction. [0024] 6. Pour the extraction solution into
a nonstick tray, and dry it in an oven at 80-90.degree. C. Do not
overheat or boil the solution. If vacuum spray dry equipment is
available, it is acceptable to use. [0025] 7. Collect the dry cinnamon
powder, weigh it. Calculate the extraction ratio. %=w/20.times.100%
[0026] w: the weight of the cinnamon extract powder.
[0027] In one experimental series, an extract was prepared according
to the foregoing procedure. Weigh 100 mg extract powder into 100
mL volumetric flask, dilute with water to 100 m, sonicate the solution
for 30-45 minutes. Filter the solution through 0.45 um PTFE syringe,
determine the polymers according to the INI procedure. The concentration
of the sample was approximately 5.17 mg/ml. It is also very important
to note that the concentrations of the polymers change with the
temperature and extraction time.
[0028] Samples were extracted at 50-60.degree. C. for about one
hour, polymers eluting at 17 and 21 minutes seemed to have reasonable
concentrations. After increasing the temperature to 75-82.degree.
C. for one hour, the peaks eluting at 17 and 21 minutes decreased
by about 2-3%. There are an additional two relatively small peaks
that seemed to surface during this extraction. They eluted at 28.5
minutes and 33.5 minutes, respectively. After increasing the heat
to 85-90.degree. C. for an additional hour, the peaks eluting at
17 and 21 minutes decreased about 7-9%. The peaks at 28.5 and 33.5
minutes increase significantly. Finally, the temperature was increased
to 95-100.degree. C. for 20 minutes, and heat was then reduced to
85-95.degree. C. for an additional 40 minutes. The results in peaks
eluting 17 and 21 minutes seemed to decrease about 15-20%. The peaks
eluting at 28.5 and 33.5 minutes increase more than double from
the previous. According to these results, the polyphenols at 17
and 21 minutes are believed to convert to isomers at 28.5 and 33.5
minutes respectively. These results suggest that the extraction
at 100.degree. C. seemed to yield the highest concentration of polymers.
[0029] An additional experiment was conducted on the extract at
100.degree. C. to verify stability. Samples were extracted at 95-100.degree.
C. for about one hour, polymers eluting at 17 and 21 minutes seemed
to have reasonable concentrations. The peaks eluting at 17 and 21
minutes decrease as the temperature increases in the first 2-3 hours.
After 3 hours, the peaks eluting at 17 and 21 minutes did not change
significantly. The peak area at 28.5 and 33.5 minutes increased
temperature in the first 2-3 hours. After 3 hours the peaks eluting
at 28.5 and 33.5 minutes did not change significantly. These results
suggest after 3 hours, these polymers seem to stabilize.
[0030] Not only is it important to note that the time and temperature
play a key factor in sustaining higher concentrations of these key
actives, additionally the species of choice can have a dramatic
impact on the levels of these Type-A polymers. The following species
appear to provide the highest level of active Type-A polymers: Cinnamomum
Burmmannii (Nees) Blume--Microbial Identification I (MIDI) class;
Korintji Cassia. Concentrations of the bioactive polymers appear
to be much higher in Indonesian cinnamon versus several other samples.
[0031] U.S. Pat. No. 6,200,569 discloses the preparation of particular
botanical extracts having utility in the treatment of diabetes and
similar conditions. Specifically disclosed therein are some specific
methods for preparing cinnamon extracts and derivatives of the type
having utility in the practice of the present invention. The entire
disclosure of the U.S. Pat. No. 6,200,569 is incorporated by reference
herein. One of skill in the art could, by reference to the incorporated
patent, prepare cinnamon-based materials having utility in the present
invention.
[0032] Typical formulations used in the practice of the present
invention for promoting weight loss and/or reduction of body fat
generally include 1-10,000 mg of the cinnamon material. In specific
embodiments, levels of cinnamon derived materials in the range of
100-500 mg are utilized. The foregoing dosages are based upon the
weights of the raw extract powder. The active Type-A polymer fraction
of such powders is approximately 1%, so dosages based solely on
the active material will be in the approximate range of 100 mcg
to 1000 mcg.
[0033] Formulations of the present invention may simply comprise
a pharmaceutical preparation of a liquid, encapsulated liquid, or
solid form of the material. In some instances, the active ingredient
of the present invention may be disposed in a food product such
as a biscuit, energy bar, or the like. However, in particular instances,
the active cinnamon-based material of the present invention is included
as a part of a dietary supplement or nutraceutical which may include
further active ingredients, as well as inactive ingredients such
as flavoring agents, coloring agents, carriers, fillers, and the
like. In specific formulations, the active, cinnamon-based material
is utilized at a level of approximately 100-500 mg, and this dosage
is typically consumed on a daily basis.
[0034] One specific formulation for promoting glucose control based
weight loss includes a cinnamon-based extract of the type disclosed
in the U.S. Pat. No. 6,200,569, said extract being referred to herein
as Cinnulin PF. This specific formulation comprises: TABLE-US-00001
Cinnulin PF: 250 mg Chromium picolinate: 100 mcg Green tea 45% EGCG:
250 mg Gymnema sylvestre: 100 mg Alpha-lipoic acid (r): 100 mg Green
coffee (chlorogenic acid): 100 mg
[0035] Another formulation in accord with the present invention
for thermogenic based glucose and/or weight control comprises: TABLE-US-00002
7-keto DHEA: 00 mg Cinnulin PF: 250 mg Evodiamine: 25 mg Oolong
tea: 100 mg Green tea 45% EGCG: 300 mg Caffeine anhydrous: 200 mg
Yohimbine: 3 mg
[0036] A formulation of the present invention for control of weight
and/or glucose which functions as an appetite control agent comprises:
TABLE-US-00003 Hoodia gordonii: 100 mg Cinnulin PF: 250 mg Glucommanan
(konjac): 500 mg Chromium picolinate: 100 mcg
[0037] A formulation which promotes weight loss and/or moderates
glucose and further operates to lower cortisol comprises: TABLE-US-00004
Magnolia officianalis: 100 mg Phosphatidyl serine: 300 mg Cinnulin
PF: 250 mg
[0038] Yet another formulation of the present invention which further
operates to block carbohydrates includes Cinnulin PF in an amount
of typically 250 mg together with a carbohydrate blocking material
such as Phase 2 or a starch blocking substance in the amount of
500 mg.
[0039] The efficacy and safety of the method of the present invention
was evaluated in a twelve-week, double-blind, placebo-controlled,
randomized group study conducted by the Ohio Research Group in Wadsworth,
Ohio. Subjects were randomized and received either the Cinnulin
PF paste composition or a placebo supplement for a twelve-week period.
Minimal steps were taken to influence subjects' lifestyle changes
with regard to diet or exercise. The subjects comprised 24 persons
having fasting glucose levels between 100 mg/dl and 139 mg/dl, and
ranging in age between 23 and 64 years. The subjects' weight, percent
body fat, fat mass, fasting glucose, fructosamine, blood pressure
and pulse were measured at zero days, six weeks and twelve weeks
post-randomization. The study showed that subjects receiving the
Cinnulin PF treatment experienced on the average 2.1% reduction
in body fat, compared to the placebo group of subjects who gained
0.9% body fat. In addition, the subjects receiving the Cinnulin
treatment experienced an average 9.18 mg/dl reduction in blood glucose
compared with a 1.1 mg/dl increase in blood glucose for the placebo
group. There were no significant differences observed in the two
groups with respect to diastolic blood pressure, pulse, or the occurrence
of any adverse event. Based upon the twelve-week trial, it was demonstrated
that the subjects consuming the Cinnulin PF supplement experienced
a significant reduction in body fat percentage without an increase
in blood pressure, pulse or the rate of any adverse events. These
benefits were achieved in the absence of any major lifestyle treatment
to change dietary or exercise behavior.
[0040] In a typical regimen, the foregoing materials are taken
orally between one and three times daily; although, other routes
of administration may be utilized as noted above. In other embodiments,
the various ingredients listed above may be utilized in other combinations
and/or at other dosage levels. Also, it should be noted that the
extracts of the present invention may be utilized in the form of
derivatives. For example, the extracts may be bonded, chemically
or physically, to other species and moieties such as synthetic polymers,
liposomes, small organic molecules, chitin, chitosan, other biopolymers
and the like. In view of the teaching presented herein, still further
combinations will be readily apparent to those of skill in the art.
[0041] The foregoing discussion and description is illustrative
of specific embodiments of the present invention, but is not meant
to be a limitation upon the practice thereof. Further modifications
and variations of the invention will be readily apparent to those
of skill in the art. It is the following claims, including all equivalents,
which define the scope of the invention.
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