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Weight Loss Patent Abstract
A therapeutically effective dose of polymethoxylated flavones, for
example in the form of citrus peel extract, is provided for reducing
the typical rise in cortisol levels in a mammal undergoing weight
loss. The polymethoxylated flavones may include one or more of tangeretin,
nobiletin, and sinensetin. The polymethoxylated flavones may be
administered in any of a variety of known modes of administrations
such as oral and topical.
Weight Loss Patent Claims
1. A composition of matter, comprising:an effective dose of citrus
peel extract for inhibiting weight gain or promoting weight loss
in a mammal.
2. The composition of matter of claim 1, wherein the citrus peel
extract comprises from about 100 mg to about 500 mg of a citrus
peel extract.
3. The composition of matter of claim 1, wherein the citrus peel
extract comprises at least about 10 mg polymethoxylated flavones
(PMFs).
4. A composition of matter as defined in claim 1, wherein the citrus
peel extract comprises at least about 80 mg PMFs.
5. A composition of matter as defined in claim 1, wherein the citrus
peel extract comprises at least one of tangeretin, nobiletin, and
sinensetin.
6. A composition of matter as defined in claim 1, wherein the citrus
peel extract comprises:from about 5 mg to about 20 mg tangeretin;from
about 5 mg to about 20 mg nobiletin, andfrom about 2 mg to about
10 mg sinensetin.
7. A topical supplement, comprising:the composition of claim 1;
anda topical cream blended with the composition of claim 1, the
topical cream being configured for facilitating transdermal absorption
of the citrus peel extract.
8. A dietary supplement, comprising:a dietary acceptable carrier
prepared in a dosage form selected from the group consisting of
a liquid, a tablet, a capsule, a powder, a confectionary, and a
supplemented food; anda composition as defined in claim 1.
9. The dietary supplement of claim 8, further comprising one or
more additives selected from the group consisting of: ginseng, caffeine,
guarana, green tea extract, chromium, vanadium, and CLA.
10. A method for promoting weight loss in a mammal, the method
comprising:administering to a mammal participating in a weight loss
exercise routine a diet consisting of a caloric intake that is insufficient
to maintain the mammal's weight; andadministering to the mammal
a composition of matter as defined as in claim 1, the citrus peel
extract comprising a sufficient amount to either reduce cortisol
levels in the mammal or reduce the amount of cortisol increase in
the mammal.
11. A method for promoting weight reduction in a mammal, the method
comprising administering to a mammal undergoing loss of body fat
an effective dose of citrus peel extract for reducing cortisol levels
or inhibiting cortisol level increases in the mammal.
12. The method of claim 11, wherein the mammal comprises a human.
13. The method of claim 11, further comprising administering to
the mammal the effective dose at least once daily for a plurality
of days.
14. The method of claim 11, wherein the citrus peel extract comprising
at least one of tangeretin, nobiletin, and sinensetin.
15. The method of claim 11, wherein the citrus peel extract is
administered to the human subject as part of a regular regime of
dose administrations and the timing and the amount of each dosage
is determined with respect the cumulative effects of the regime.
16. The method of claim 15, wherein the effective dose is defined
as sufficient to reduce cortisol levels by at least 5% during the
regime relative to a cortisol level that would result in the absence
of the administration of the citrus peel extract.
17. The method of claim 11, wherein the citrus peel extract is
in a oral form selected from the group consisting of a beverage,
a tablet, a capsule, a powder, a confectionary, and a supplemented
food.
18. The method of claim 11, wherein the citrus peel extract is
blended with a topical cream for topical administration and administering
the effective dose of citrus peel extract comprises topically administering
the citrus peel extract.
19. A method for preventing or treating conditions enhanced by
the presence of excess glucocorticoids in a mammal, the method comprising:administering
to a mammal in need thereof a therapeutically effective dose of
citrus peel extract for reducing excess glucocorticoids, the citrus
peel extract comprising at least about 10 mg of polymethoxylated
flavones (PMFs).
20. The method of claim 19, wherein the therapeutically effective
dose of citrus peel extract comprises from about 100 mg to about
500 mg.
Weight Loss Patent Description
CROSS-REFERENCE TO RELATED APPLICATIONS
[0001]This application claims the benefit of Provisional Application
No. 60/785,158, filed Mar. 23, 2006, entitled "Weight Loss
With Citrus Flavonoids," which is incorporated by reference
herein in its entirety.
BACKGROUND OF THE INVENTION
[0002]1. The Field of the Invention
[0003]The present invention relates to the fields of food compositions
and dietary supplements. More particularly, the invention provides
compositions and methods for promoting weight reduction in a human
subject by administering an effective dose of citrus peel extract
to a human subject undergoing weight loss to reduce cortisol levels.
[0004]2. The Relevant Technology
[0005]Obesity, diabetes, and metabolic syndrome ("Syndrome
X"--encompassing insulin resistance, type 2 diabetes, dyslipidemia,
hypertension, and abdominal obesity) are reaching epidemic proportions
in the United States and around the world. Excess glucocorticoids
such as cortisol (a primary stress hormone) have been theorized
to contribute high levels of abdominal fat and diabetes. The negative
effects of cortisol have been theorized in part due to an increased
appetite that has been reported in persons with elevated cortisol
levels. Further, high levels of urinary cortisol excretion has been
noted in persons exercising high dietary restraint. The high levels
of cortisol excretion suggest a harmful cycle in which attempts
to lose weight by eating less are countered by the body releasing
cortisol in response to the stress, which in turn increases appetite
and thus heightens the chances of a failed weight loss attempt.
[0006]Accordingly, methods of reducing the harmful affects of cortisol
would represent an advance in the art of dietary supplements
BRIEF SUMMARY OF THE INVENTION
[0007]According the invention, conditions enhanced by the presence
of excess glucocorticoids such as cortisol can be reduced by using
citrus peel extract, including polymethoxylated flavones (PMFs),
to reduce the increase in cortisol levels typically resulting from
body fat and with weight loss. The citrus peel extractor PMFs may
be administered in any of a variety of known modes of administrations
such as oral and topical.
[0008]Accordingly, a first example embodiment of the invention
is a composition of matter including an effective dose of citrus
peel extract for inhibiting weight gain or promoting weight loss
in a mammal. An effective dose of the citrus peel extract may be
from about 1 mg to about 1000 mg, for example, or more preferably
the effective dose may be from about 100 mg to about 500 mg of a
citrus peel extract. Regardless, the citrus peel extract comprises
at least about 10 mg PMFs in the citrus peel extract. The PMFs preferably
include at least one of tangeretin, nobiletin, and sinensetin.
[0009]Example compositions of the present invention may be formulated
for administration through various known routes of administration,
such as oral, parenteral, and transdermal routes. Examples of oral
dosage formulations include without limitation, tablets, capsules,
liquids, suspensions, gels, powders, effervescent beverages, lozenges,
chewing gum, candy, supplemented food, etc. Examples of transdermal
routes of administration include without limitation, topical formulations,
such as lotions, creams, gels, and pastes, and transdermal patches,
such as liquid reservoir patches, plasters, and adhesive matrix
patches. Suitable ingredients required to produce a particular formulation,
such as specific carriers, excipients, binders, penetration enhancers,
etc., will be readily recognized by those of ordinary skill in the
art and are not discussed in detail herein to avoid obscuring the
invention. In preferred embodiments one or more weight loss enhancing
additives such as ginseng, caffeine, guarana, green tea extract,
chromium, vanadium, and CLA are added.
[0010]Another example embodiment of the invention is a method for
promoting weight loss in a mammal. The method generally includes:
administering to a mammal participating in a weight loss exercise
routine a diet consisting of a caloric intake that is insufficient
to maintain the mammal's weight; and administering to the mammal
a an effective dose of citrus peel extract to either reduce cortisol
levels in the mammal or reduce the amount of cortisol increase in
the mammal.
[0011]In another example embodiment of the invention the citrus
peel extract is administered to the human subject as part of a regular
regime of dose administrations and the timing and the amount of
each dosage is determined with respect the cumulative effects of
the regime. In this example the effective dose may optionally be
defined as the amount sufficient to reduce cortisol levels by at
least 5% during the regime relative to a cortisol level that would
result in the absence of the administration of the citrus peel extract.
[0012]These and other objects and features of the present invention
will become more fully apparent from the following description and
appended claims, or may be learned by the practice of the invention
as set forth hereinafter.
DETAILED DESCRIPTION OF THE PREFERRED EMBODIMENTS
[0013]In the following description, numerous specific details are
set forth in order to provide a thorough understanding of the present
invention. It will be obvious, however, to one skilled in the art
that the present invention may be practiced without these specific
details. In other instances, well-known aspects of citrus peel extract,
polymethoxylated flavones (PMFs), and various oral and topical dosage
forms have not been described in particular detail in order to avoid
unnecessarily obscuring the present invention.
[0014]Polymethoxylated Flavones (PMFs), particularly tangeretin,
sinensetin, and nobilitin, have known health benefits in reducing
cholesterol and promoting cardiovascular health. According to the
invention it has been determined that PMFs also assist in weight
loss or the reduction in weight gain (weight loss and the reduction
in weight gain will sometimes be referred to collectively as "weight
loss" herein for simplicity). Although all embodiments of the
application are not necessarily tied to any particular theory, it
is believed that the PMFs reduce cortisol levels, or at least decrease
cortisol level gains, during periods of stress to facilitate the
weight loss. Since cortisol is a stress hormone, higher levels of
which have been tied to weight gain, the reduction in cortisol leads
to the weight loss.
[0015]Accordingly, the present invention provides compositions
and methods using PMFs for the prevention and treatment of diabetes
and obesity. Individuals at high risk of developing or having diabetes
or desiring to prevent weight gain or promote weight loss may be
treated with an effective dose of citrus polymethoxylated flavones
(PMFs). More particularly, the present invention relates to the
discovery and use of PMFs to reduce systemic and local cortisol
concentrations (liver and adipose tissue), and promote blood sugar
control and weight loss. The current invention therefore represents
an important and innovative treatment for obesity, diabetes, and
related metabolic diseases by promoting weight loss and controlling
blood sugar levels.
[0016]According to one embodiment of the invention, a mammalian
subject can be administered once a day a composition of matter having
from about 1 mg to about 1,000 mg of a citrus peel extract. In a
more preferred embodiment the composition of matter has from about
100 mg to about 500 mg of a citrus peel extract. In a still more
preferred embodiment the composition of matter at least about 300
mg of the citrus peel extract. In each of the foregoing examples,
the citrus peel extract preferably has at least about 10 mg PMFs,
more preferably at least about 80 mg PMFs. The amount of citrus
peel extract may increase or decrease depending on the concentration
of the citrus peel extract.
[0017]Alternatively, in another embodiment of the invention a mammalian
subject can be administered once a day a composition of matter having
one or more of tangeretin, nobiletin, and sinensetin. By way of
example only, the dosage may have one or more of from about 1 mg
to about 50 mg of tangeretin, from about 1 mg to about 50 mg of
nobiletin, and from about 1 mg to about 20 mg of sinensetin. The
levels of each in a particular dosage may increase or decrease depending
on the respective concentrations in the citrus peel extract as well
as the overall concentration of the citrus peel extract. In a more
preferred embodiment the composition of matter has from about 5
mg to about 20 mg of tangeretin, from about 5 mg to about 20 mg
of nobiletin, and from about 2 mg to about 10 mg of sinensetin.
[0018]One embodiment of the invention is a composition of matter
having an effective dose of citrus peel extract for preventing weight
gain or promoting weight loss in a mammal. As used herein the term
"an effective dose" indicates an amount sufficient to
create a desirable result. For example, in one embodiment an effective
dose is the amount necessary to obtain a measurable change in cortisol
levels. An effective dose will therefore preferably reduce cortisol
levels by at least about 5 percent as compared to a cortisol level
that would result in the absence of the administered dose(s). Still
more preferably, an effective dose will reduce cortisol levels by
at least about 10 percent as compared to a cortisol level that would
result in the absence of the administered dose(s). Alternatively,
an effective dose can be the amount necessary to promote a relative
weight reduction, wherein a relative weight loss is defined by a
human obtaining a lower weight than the human user would have obtained
without receiving the effective dosage. The precise parameters of
an effective dose may of course vary with a number of factors, including
by way of example only, weight, gender, age, and desired result.
[0019]The compositions of the present invention may be formulated
for administration through various known routes of administration,
such as oral, parenteral, and transdermal routes. Examples of oral
dosage formulations include without limitation, tablets, capsules,
liquids, suspensions, gels, powders, effervescent beverages, lozenges,
chewing gum, candy, supplemented food, etc. Examples of transdermal
routes of administration include without limitation, topical formulations,
such as lotions, creams, gels, and pastes, and transdermal patches,
such as liquid reservoir patches, plasters, and adhesive matrix
patches. Suitable ingredients required to produce a particular formulation,
such as specific carriers, excipients, binders, penetration enhancers,
etc., will be readily recognized by those of ordinary skill in the
art and are not discussed in detail herein to avoid obscuring the
invention.
[0020]For example, one preferred administration route is as a diet
shake. The diet shake can be provided to a user in either liquid
form or as a powder having suitable ingredients for the user to
form a shake upon mixture with a liquid. In addition, a supplemented
food such as a nutritional bar or dessert is also preferred.
[0021]The citrus peel extract can be preferably combined in the
foregoing administration forms with a variety of other supplements,
vitamins, stabilizers, and the like as are known in the art to create
a desirable administration form. By way of example only, such additives
can include other forms of ginseng, caffeine, guarana, green tea
extract, chromium, vanadium, CLA, and the like.
[0022]Where the dosage form is oral, a flavoring such as a citrus
flavoring can be added to improve the taste as well as to enhance
the user's perception of consuming the citrus peel extract. Where
the dosage form is topical, a scent such as a citrus aroma can be
added to not only improve the scent of the topical cream or ointment,
but also to enhance the user's awareness of using the citrus peel
extract.
[0023]Other conventional additives such as stabilizers, pH adjusters,
excipients, carriers and diluents and the like may be added as desired
or necessary as is known in the art provided they do not interfere
with the activity of citrus peel extract.
[0024]The compositions of the invention can be formulated so as
to provide quick, sustained or delayed release of the citrus peel
extract after administration employing procedures and formulations
known in the art.
[0025]The following example is shown by way of illustration only.
EXAMPLES
Example 1
[0026]A group of fifty moderately overweight human subjects, self-described
as "stress-eaters," participated in an eight week study.
The subjects had an average age of 44, an average starting weight
of 78.5 kg, an average starting body fat percent of 32.4%, and an
average starting waist circumference of 86.7 cm. During the eight
week study, the subjects followed a program that included: daily
supplements including citrus peel extract, a moderate calorie-restricted
diet based on resting metabolic rate (RMR), a moderate exercise
program on five days each week, and daily stress management techniques.
More particularly, polymethoxylated Flavones (PMFs) were administered
to the test subjects in the form of 300 mg of citrus peel extract/day
containing 81 mg of PMFs comprising a minimum of 12 mg tangeretin,
12 mg nobiletin, and 5 mg sinensetin.
[0027]At the conclusion of the study the human subjects were again
tested and found to have a mean reduced body weight by 0.6 kg, mean
reduced body fat by 5.0%, mean reduced fat mass by 1.9 kg, mean
increased lean mass by 1.3 kg, and mean reduced waist circumference
by 1.3 cm.
[0028]In addition, the subjects were tested before and after the
eight week study for salivary cortisol levels by salivary enzyme
immunoassay. A mean 18.7% reduction in salivary cortisol levels
for the subjects was observed suggesting a reduction in stress.
[0029]In addition, before and after participation the subjects
each completed a 65 question Profile of Mood States (POMS) questionnaire.
The Profile of Mood States (POMS) is a well known test that measures
present mood state (disturbance) by a list of adjectives. In the
test, respondents rate 65 adjectives on a 5-point intensity scale
in terms of how they have been feeling in the past week (O=not at
all and 4=extremely). Except for vigor, the higher the score, the
greater the mood disturbance/more distress. For analysis, the questions
of the POMS are divided into six categories: tension, fatigue, confusion,
vigor, depression, and anger and a score calculated for each. A
Global Mood State score is also derived from the sum of all negative
categories minus the score for vigor. For further details on the
POMS test, see McNair D M, Lorr M, and Droppleman L F., Profile
of Mood States Manual, San Diego, Calif.: Educational and Industrial
Testing Services (1971). As noted in Table 1 below, the respondents
had mean improvements of from 14% to 41% in all categories suggesting
a strong reduction in stress as a result of the study.
TABLE-US-00001 TABLE 1 Test Percent Change Global Mood State -19.7%
Tension -19% Fatigue -41% Confusion -14% Vigor +29% Depression -40%
Anger -41%
[0030]The present invention may be embodied in other specific forms
without departing from its spirit or essential characteristics.
The described embodiments are to be considered in all respects only
as illustrative and not restrictive. The scope of the invention
is, therefore, indicated by the appended claims rather than by the
foregoing description. All changes which come within the meaning
and range of equivalency of the claims are to be embraced within
their scope. |