Weight loss abstract
The present invention is directed to herbal compositions which
reduce weight, maintain weight loss over an extended period of time,
and act as an appetite suppressant. The composition consists of
St. John's Wort with or without caffeine or other appetite suppressants
known in the art, and also a composition comprising St. John's Wart
(hypericin) and Mahuang (Ephedra sinica or ephedrine). Another composition
disclosed comprises a combination of the above herbs with caffeine.
Weight loss claims
What is claimed is:
1. A composition comprising a dosage of a member selected from
the group consisting of St. John's Wort and hypericin and a member
selected from the group consisting of Mahuang extract, Ephedra sinica
and ephedrine in an amount effective for reducing weight and maintaining
the weight loss.
2. A composition comprising a dosage of a member selected from
the group consisting of St. John's Wort and hypericin and a member
selected from the group consisting of Mahuang extract Ephedra sinica
and ephedrine in an amount effective for suppressing appetite.
3. The composition of claim 1 wherein St. John's Wort is present
in an amount ranging from 10 mg to 2500 mg.
4. The composition of claim 1 wherein the amount of St. John's
Wort is 400 mg.
5. The composition of claim 1 wherein the amount of St. John's
Wort ranges from 10 mg to 2500 mg, and the dosage of Mahuang ranges
from 5 mg to 1500 mg.
6. The composition of claim 1 wherein St. John's Wort is present
in an amount of 500 mg per day and Mahuang is present in an amount
of 800 mg per dose.
7. The composition of claim 1 in sustained release form.
8. The composition of claim 1 in unit dosage form.
9. The composition of claim 1, further comprising an agent selected
from the group consisting of electrolytes, buffers, colorants, aromatic
agents, flavoring agents, emulsifying agents, compounding agents,
formulation agents, permeation enhancers and other weight reduction
agents and bulking agents.
10. A method for obtaining weight reduction in humans and animals
including taking a daily dosage of St. John's Wort in the range
of 10 mg to 2100 mg per day and a daily dosage of a member selected
from the group consisting of Mahuang extract, Ephedra sinica and
ephedrine in the range of 10 mg to 2500 mg.
11. A method for obtaining and maintaining weight reduction in
humans and animals including taking a composition comprising a daily
dosage of St. John's Wort in the range of 10 mg to 2100 mg per day
and a daily dosage of a member selected from the group consisting
of Mahuang extract, Ephedra sinica and ephedrine in the range of
10 mg to 2500 mg and administering to the subject, after a predetermined
weight is attained, a weight maintaining effective amount of the
Weight loss description
This application claims the benefit under 35 USC 119(e) of provisonal
application Ser. Nos.60/036,339, filed Jan. 22, 1997 and 60/038,128
filed Mar. 3, 1997.
FIELD OF THE INVENTION
The invention relates to compositions for reducing weight in humans
and/or animals and more particularly to herbal compositions for
achieving the desired result.
BACKGROUND OF THE INVENTION
This invention relates to herbal compositions for reducing weight,
maintaining weight loss over an extended period of time and suppressing
appetite in a human or a domestic animal.
Examples of known appetite reducing agents are ephedrine which
is an extract of the herb Mahuang (Ephedra sinica), phenylpropanolamine
(PPA), amphetamines and fenfluramine alone or in combination with
caffeine. Caffeine functions probably to reduce fatigue as caffeine
has stimulating properties. Phenylpropanolamine (PPA) is a popular
over-the-counter drug for appetite suppression and its side effects
are well documented.
Several herbal compositions have been developed for reducing weight
in humans or domestic animals. U.S. Pat. No. 5,422,352 discloses
a composition of ephedrine and caffeine in a ratio of about 1:12.
U.S. Pat. No. 5,019,594 discloses a method for decreasing appetite
by administering a composition containing ephedrine or other indirect
acting sympathomimetic drugs and tyrosine. U.S. Pat. No. 5,273,754
discloses an appetite suppressant composition comprising a heating
and a cooling carminative substance, which composition may also
include an amino acid and an anxiolytic substance. One of the anxiolytic
substances disclosed is St. Joh's Wort. U.S. Pat. No. 5,543,405
discloses a weight reduction composition comprising a sympathomimetic
agent and a mineral cation salt or chelate. Preferred is a composition
comprising ephedrine and chromium picolinate. U.S. Pat. No. 5,055,460
discloses a composition for reducing weight comprising ephedrine,
acetylsalicylic acid and caffeine.
However, none of the methods for weight reduction or appetite suppression
disclose a composition consisting of St. John's Wort (hypericin),
or a composition comprising St. John's Wort and Mahuang (Ephedra
sinica or ephedrine) which are disclosed in the present invention.
The synergistic effect of St. John's Wort and Mahuang have been
shown to be unexpectedly superior than the effect of the individual
SUMMARY OF THE INVENTION
The present invention discloses herbal compositions effective in
reducing weight, maintaining weight loss and suppressing appetite
comprising comprising St. John's Wort (hypericin) and Mahuang (Ephedra
sinica or ephedrine). When taken in combination, St. John's Wort
and Mahuang act synergistically to increase serotonin levels in
the brain to effect appetite suppression and caloric expenditure
increase in the body. These weight reduction and appetite suppressant
compositions are presented in a variety of formulations, with or
without other weight reduction active ingredients such as phenalpropanolamine
BRIEF DESCRIPTION OF THE INVENTION
It is a well established fact that overweight and obesity is an
unhealthy condition. It is therefore logical that substances aiding
or resulting in weight reduction would be beneficial to a society
where millions suffer from obesity, as long as the substance is
safe and effective when taken as directed. This condition may be
related to a genetic trait and/or to environmental factors. See,
generally, Ravussin, Lillioja, Knowler, Reduced Rate Of Energy Expenditure
As A Risk factor For Body Weight Gain, New Jr. Eng. of Med., 318,
p. 467, 1988.
Over-weight and obesity are chronic conditions which are highly
prevalent in industrialized society. These conditions are associated
not only with social stigma but are also associated with decreased
longevity and numerous medical problems such as diabetes, reproductive
disorders, dermatological disorders, varicose veins, arthritis,
heart disease, cancer, etc.
Over-weight and obesity is a condition characterized by the excessive
accumulation of fat in the body as a consequence of an energy intake
which is greater than energy expenditure. Over-weight is present
if the body weight exceeds a "desirable weight", whereas
obesity represents a condition where the weight is 20% or more above
the desirable weight. Desirable weight for humans is defined in
the Metropolitan Height And Weight tables as the midpoint of the
range of medium frame individuals. See, JAMA,260, 2547-48, 1988.
Existing therapies for over-weight and obesity basically include
a treatment to establish a negative energy balance. This may be
accomplished by reduction of energy intake, for example, a low calorie
diet; or an increase in energy expenditure, for example, by increased
physical exercise; or by ingestion of a sympathomimetic drug which
stimulates thermogenesis, i.e., increases the metabolic rate of
the body in humans and animals. Known thermogenic drugs are ephedrine,
phenylpropanolamine and caffeine. See, for example, Astrup, A.V.,
Treatment Of Obesity With Thermogenic Agents, Nutrition, 5, p. 70,
1989; Bray, Nutrition Reviews, 49, p. 33, 1991.
While energy expenditures may increase 10-fold during exercise,
the thermogenic effect of pharmacological agents is much more modest.
Sympathomimetic compounds and beta adregenic agonists can increase
resting energy expenditure by 10% to 15% and slightly potentiate
the effect of foods. Energy expenditure may be increased 5% to 10%
on a 24-hour basis. See, generally, Astrup, Breum, Tourbo, Pharmacological
And Clinical Studies Of Ephedrine And Other Thermogenic Agonists,
Obesity Research, 3, p. 537, 1995.
Drugs which are used for reducing weight or obesity suppress appetite
by acting the on noradrenergic neurotransmitter such as mazindol
and derivatives of phenethylamine, for example, phenylpropanolamine,
phentermine, amphetamine, methamphetamine. Also well known in the
art are the use of drugs which act on the serotonin neurotransmitter
such as fenfluramine, tryptophan, fluoxetine and sertraline. However,
all these drugs have side effects.
There is, therefore, a need for a drug which will reduce the weight
of overweight or obese persons without side-effects and which will
also help obese and overweight subjects maintain the reduced weight
OBJECTS OF THE INVENTION
It is therefore an object of the present invention to provide a
regimen that is useful in returning the body weight of overweight
or obese subjects to a lower and preferably normal body weight.
It is another object of the present invention to provide a therapy
for overweight or obesity that results in maintenance of the lowered
body weight over an extended period of time.
DETAILED DESCRIPTION OF THE INVENTION AND PREFERRED EMBODIMENTS
The present invention is directed to a composition of St. John's
Wort, and also to a composition comprising St. John's Wort (hypericin)
and Mahuang (Ephedra sinica, or its extract ephedrine).
St. John's Wort is a herb of the hypericaceae family which contains
the therapeutically active ingredient hypericin. St. John's Wort
has antidepressant properties for which it is widely used in Europe.
Numerous publications and meta-analysis strongly suggests the antidepressant
efficacy through seratonergic mechanisms. However, it was unexpectedly
found that St. John's Wort also functions to reduce weight and also
acts as an appetite suppressant, most likely by controlling serotonin
levels. See BMJ 1996; 313:253-8 St. John's Wort for Depression--An
Overview and Meta-analysis Of Randomized clinical Trials; K. Linde,
The dosage form of St. John's medication contains its extract at
a concentration of 0.3% Hypercum perforatum. For efficacy in providing
weight reduction, St. John's Wort should be present in an amount
ranging from 10 mg to 2500 mg per dose per day, preferably 100 mg
to 800 mg per dose per day or 500 mg per dose per day, Most preferably,
St John's Wort is present in amount of 400 mg per dose which is
to be taken two times per day. Other weight reduction compositions
such as caffeine may be taken with St. John's Wort.
Another composition which is effective in reducing weight and suppressing
appetite is a composition comprising St. John's Wort (hypericin)
and Mahuang (Ephedra sinica or ephedrine) Mahuang is also a naturally
occurring herb which aids in weight reduction through its active
ingredient the sympathomimetic compound Ephedra sinica or its extract
ephedrine. When used in combination with St. John's Wort, Mahuang
should be present in an amount ranging from 5 mg to 1500 mg per
dose per day, and most preferably at a concentration of two doses
of 250 mg each per day.
Both St. John's Wort and Mahuang are safe and effective when used
as directed and side effects are minor or none. High doses of Mahuang
are associated with sympathomimetic simulation and attendant side
effects. Accordingly, low doses are recommended in the medication
and subjects who have high blood pressure or cardiac arrhythmias
are not good candidates for this drug regimen.
If both St. John's Wort and Mahuang are taken, it is recommended
that Mahuang be taken separately in the morning and St. John's Wort
in the afternoon before dinner.
Good results were observed in a clinical study according to the
present invention by using a pharmaceutical tablet composition consisting
of a composition comprising St. John's Wort and Mahuang in overweight
or obese subjects. However, the results of the clinical studies
detailed below clearly demonstrate that the action exerted by the
combination of St. John's Wort and Mahuang is due to an unexpected
synergistic effect of the two drugs.
The herbal components (St. John's Wort and Mahuang) may be used
for weight reduction and appetite suppressant without being further
processed, or they may be used as extracts thereof. For example,
St. John's Wort herb may be dried, powdered and used in the powdered
form as the active ingredient in a oral dosage form such as a pill
or a capsule. Alternatively, hypericin, the active ingredient of
St. John's Wort may be extracted from the herb by soaking the crushed
herb in an alcohol/water solution and the extracted active ingredient
dried by spray drying or evaporation.
The composition according to the present invention may be formulated
for administration by any conventional route such as oral, rectal,
nasal, topical (dermal) or parenteral. Thus the composition may
be in the form of tablets, capsules, suspensions, emulsions, solutions,
suppositories, sprays or injectibles. Formulations for oral use
include tablets which contain the active ingredient in admixture
with pharmaceutically acceptable inert excipients. These excipients
may be, for example, inert diluents such as calcium carbonate, sodium
chloride, lactose, calcium phosphate, sodium phosphate, etc.; granulating
and disintegrating agents, for example, potato starch, alginic acid,
etc.; binding agents, for example, starch, gelatin or acacia, etc.;
and lubricating agents for example, magnesium stearate, stearic
acid or talc. Other pharmaceutically acceptable excipients can be
colorants, flavoring agents, plasticizers, humectants, etc. The
tablets may be uncoated or they may be coated by known techniques.
Alternatively, the active ingredients of the weight reduction formulation
may be delivered over an extended time period by delaying disintegration
and absorption in the gastrointestinal tract to provide a sustained
release effect. For example, a time delay material such as glyceral
monostearate or glycerol distearate may be employed. The active
ingredient may be placed in an extended release dosage form by techniques
which are well known in the art. See, for example, Baker, Richard,
Controlled Release Of Biologically Active Agents, John Wiley And
Sons, 1986. The inactive excipients in a tablet may include calcium
carbonate, dicalcium phosphate, microcrytalline cellulose, croscarmellose
sodium, stearic acid, silica, magnesium stearate and pharmaceutical
glaze. Alternatively, the active ingredient or extract thereof may
be delivered in a soft or hard gel capsule by mixing the active
ingredient with water or an oil medium such as peanut oil, liquid
paraffin, or olive oil and enclosing it within the capsule or gel
The dosage may also be administered as an oral liquid dosage form
by suspending the active ingredients or extracts thereof in an aqueous
solution in admixture with a dispersing or wetting agent, suspending
agent and one or more preservatives. Suitable dispersing or wetting
agents are, for example, naturally occurring phosphatides, for example,
lecithin, or condensation products of ethylene oxide, fatty acids,
long chain aliphatic acids, or a partial ester derived from fatty
acids and a hexitol or hexitol anhydrides, for example, polyoxyethylene
stearate, polyoxyethylene sorbitol monooleate, polyoxyethylene sorbitan
monooleate, etc. Suitable suspending agents are, for example, sodium
carboxymethylcellulose, methylcellulose, sodium alginate, etc.
The pharmaceutical formulation may also be delivered parenterally
in dosage forms containing conventional pharmaceutically acceptable
carriers and adjuvants. The formulation and preparation of such
compositions is well known to those skilled in the art. For example,
specific formulations can be found in the text Remington's Pharmaceutical
Sciences, Mack Publishing Co., Easton, Pa., 1995. The active ingredients
may be dissolved in vehicles such as water, isotonic sodium hydroxide
solutions, etc. The aqueous formulations may also contain a preservative
such as methyl, ethyl or n-propyl p-hydroxybenzoate.
For rectal applications, suitable dosage forms for a composition
according to the present invention include suppositories (emulsion
or suspension type), and rectal gelatin capsules (solution or suspensions).
In a typical suppository formulation, the active ingredients of
the two herbs are combined with an appropriate pharmaceutically
acceptable suppository base such as cocoa butter, esterified acids,
glycerinated gelatin, and various water soluble or dispersable bases
like polyethylene glycols and polyoxyethylene glycols and polyoxyethylene
sorbitan fatty acid esters.
To prepare the weight loss and appetite suppressant of the present
invention in a tablet form, the extract of the two herbs were combined
with excipients in an appropriate ratio and thereafter tableted
by methods which are well known in the art. See, for example, Remington's
Pharmaceutical Sciences, Mack Publishing Co., Easton, Pa., 1995.
Overweight and obese patients were placed on a low calorie diet
and a daily dosage of St. John's Wort effective to control appetite
and reduce weight and maintain the weight loss is 10 mg to 2100
mg per day, with and without caffeine. It was found that over a
two month period, over 90% of the subjects lost an average of 4
pounds per month, were able to maintain the weight loss, and reported
a decreased craving for food and a decreased appetite.
A dose response open-label study of the thermogenic effect of St.
John Wort in combination with Mahuang was conducted. The concentration
range over which Mahaung is effective to control appetite, reduce
weight and maintain the weight loss is from 10 mg to 2500 mg per
The aim of the study was to assess the effectiveness, tolerability
and safety of oral administration of St. John's Wort at a dosage
of 400 mg twice daily and a Mahuang dosage of 250 mg twice daily
over a 6 week period for the treatment of overweight and appetite
suppression. Changes in weight and body composition measurements
were primary effectiveness variables. The aim of the study was to
determine if fat is preferentially lost when the two herbs are combined
with the diet. Appetite suppression was a secondary effectiveness
The study was conducted in subjects with a body mass index of 27
to 32 kg/square meter. Fifteen overweight but otherwise healthy
subjects were selected at random for the study. The subjects were
supplied with two weeks supply of 28 caplets and one of three calorie
diet plans. The subjects were directed to swallow a caplet comprising
one 200 mg St. John's Wort and 125 mg of Mahuang 30 to 60 minutes
before breakfast and to repeat the same dosage before dinner with
a glass of water.
Specifically excluded from this study were subjects who required
or were currently taking any significant medication other than analgesics
on an occasional basis such as drugs containing sympathomimetics
amines, MAO inhibitors and other drugs indicated for weight reduction.
The subjects were instructed to visit the clinic every week to
weigh-in and pick up the necessary combined St. John's Wort and
Mahuang tablets. On each visit the subjects were also monitored
for blood pressure, temperature, body fat by bioimpendence analysis
and anthropometry, and circumference measurements of the chest,
waist and hips.
At the end of the six weeks study, the 12 subjects lost an average
of 8 pounds. The subjects also reported on the effects of the herbal
therapy as it related to appetite control, feeling of fullness and
snack cravings. 87% of the subjects reported a suppression of appetite;
81% reported satisfaction with less food during a meal, and 81%
reported that they were less inclined to snack between meals.
It will be apparent to one of ordinary skill in the art that many
changes and modifications can be made to the present disclosure
without departing from the spirit and scope of the invention as
set forth herein.
A latitude of modification, change and substitution is intended
in the foregoing disclosure, and in some instances, some features
of the invention will be employed without a corresponding use of
other features. Accordingly, it is appropriate that the appended
claims be construed broadly and in a manner consistent with the
spirit and scope of the invention herein described.