Title of Invention


Abstract A pharmaceuitical composition suitable for regulating body weight, especially for promoting body weight loss comprising of the herb or a plant Zizyphus mauritiana Lamk or extracts of its bark or leaves for reducing body weight.
Full Text FORM-2
THE PATENTS ACT. 1970 (39 of 1970)
COMPLETE SPECIFICATION (Section 10, rule 13)
"A Composition and method for body weight loss"
Dr. Kishori Ganpat Apte and Ms. Vaishali Vasant Potnis, both residing at Survey No. 36/1/1, MN 199, Wadgaon Khurd, Sinhagad Road, Pune 411 041, Maharashtra, India.
Both Indian nationals
The following specification particularly describes the nature of the invention and the manner in which it is to be performed: -

Dated this 19th December, 2006

The invention relates to a composition for regulating body weight.
Particularly, the invention relates to compositions and methods for regulating body weight, especially for promoting body weight loss.
More particularly, the invention concerns the use of extracts of bark of Zizyphus mauritiana Lamk for regulating body weight and for promoting body weight loss.
Body weight and body composition is determined by the competing balance of food intake and energy expenditure. Although both genetic and environmental factors can contribute to obesity, the most common cause of weight gain and an overweight body composition is excessively high caloric intake accompanied by a lack of physical activity. The resulting accumulation of surplus fat places overweight or obese individuals at
increased risk of illness from hypertension, lipid disorders, type 2 diabetes, coronary heart disease, stroke, gallbladder disease, osteoarthritis, sleep apnea and respiratory problems, certain cancers, and a wide variety of other diseases and undesired physiological conditions, as well as overall mortality. Obesity is a cause of concern all over the world, including India. According to a study, the proportion of overweight

individuals in the United States increased from 25% in 1980 to 33% in 1991. (Third National Health and Nutrition Examination Survey, 1991). In 1998 the National Institutes of Health reported that over 55 percent of the U.S. population are now considered overweight or obese. (Obesity Clinical Guidelines: NIH Statement Jun. 3, 1998, press release).
Obesity may become partially reversed or prevented by employing diet or nutrition and behavior modification programs or by using pharmaceutical intervention. Among the most widely administered drugs are: orlistat, which reduces the amount of dietary fat that is absorbed from the intestine; sibutramine, which suppresses appetite by inhibiting the re-uptake of norepinephrine and serotonin; fenfluramine and d-fenfluramine, which suppress appetite by both releasing serotonin and then inhibiting its re-uptake; and phentermine, which suppresses the appetite by stimulating the release of norepinephrine.
Most weight reduction drugs typically achieve only a 5-10% decrease in body weight. (National Task Force on the Prevention and Treatment of Obesity: Long-term pharmacotherapy in the Management of Obesity, JAMA 276:1907-15, 1996). In addition, most drugs have mild to serious side effects. For example, the once popular appetite suppressant drug "Fen-Phen" (the combination of fenfluramine and phentermine), which gave a 15-20% reduction in body weight, was clinically determined to have significantly increased the risk of heart valve damage. (F. Brenot et al., Appetite Suppressant Drugs and the Risk of Primary Pulmonary Hypertension, N. Engl. J. Med., 335:609-16, 1996).

Consequently, after a number of confirmed "Fen-Phen"—related patient deaths, most of the drugs containing fenfluramine have been recalled and withdrawn. (Connolly H. M. et. al., N. Eng. J. Med. 337:581-88, 1997). In 1999 the FDA removed fenfluramine from the market. Other common side effects include dizziness, headaches, rapid pulse, palpitations, sleeplessness, hypertension, diarrhea, and intestinal cramping.
In addition to adverse side effects, current weight loss drugs may be habit forming, as exemplified by drugs containing amphetamines, and the initial weight reducing effect of many drugs wears off over time, requiring increased dosages to maintain weight reduction. The most serious problem, however, is that the lost weight is frequently regained after the drug is discontinued and the fairly limited utility of these drugs is more than offset by the side effects and other drawbacks inherent in their use.
The following table provides a synopsis of some of the characteristics of the most popular weight loss drugs and notes some of the impediments to wide-scale use:
Generic Name and Mechanism Brand Name Comments Amphetamine + Adderall Not commonly used Dextroamphetamine therapeutically for obesity, sympathomimetic amine High abuse potential, appetite suppressants Benzphetamine sympatho- Didrex; Not commonly used mimetic amine appetite Benzfetamine therapeutically. High abuse suppressant potential. Bromocriptine stimulates Ergoset; Not approved in US for dopamine type-2 receptors Parlodel obesity. Used "off label", and antagonizes type-1 receptors in brain Dexfenfluramine Redux Approved 04/96 in US with appetite

suppressant via no limit on duration of use. serotonin release and Voluntarily withdrawn in serotonin reuptake block; US 09/15/97 due to heart the d isomer of fenflu- valve damage, ramine; thought to be less addicting than most others Dextroamphetamine Dexedrine Not approved in US for sympathomimetic amine obesity. Used "off label", appetite suppressant Highly abused. Diethylpropion sympatho- Amfepramone; Possible link to primary mimetic amine appetite Tenuate; pulmonary hypertension suppressant Tenuate Dospan Fenfluramine racemic Pondimin; One component of "fen/ mixture dexfenfluramine Ponderal phen"; Approved in US in and L-fenfluramine; 1973. Voluntarily with- mechanism like dexfenflu- drawn in US due to heart ramine (see above), except valve damage 09/15/97 also affects dopamine availability Fluoxetine selective Prozac Not approved in US for serotonin reuptake inhibitor obesity. FDA application (SSRI) was withdrawn by manufacturer. Used "off label". Mazindol sympathomimetic Mazanor; Approved in US in 1973. amine appetite suppressant Sanorex Rarely used. High abuse potential. Methamphetamine Desoxyn; Rarely used for obesity, sympathomimetic amine Methampex High abuse potential, appetite suppressant Orlistat Xenical Recommended for approval not a CNS-active drug; in US 05/15/97; FDA panel decreases the amount of fat reconsidered and split 5-5 absorbed from the diet by on 03/16/98; due to possi- 30%. ble link to breast cancer Phendimetrazine sympatho-Adipost; Approved in US in 1961. mimetic amine appetite Anorex; Rarely used, suppressant Bontril; Parzine; Phendiet; Plegine; Wehless Phentermine sympatho-Adipex-P; Approved as "resin mimetic amine appetite Fastin; complex" in 1959. suppressant lonamin; Approved as hydrochloride Oby-Cap; in 1973. The other Phentamine; component of "fen/phen". T-Diet; Zantryl Phenylpropanolamine Acutrim;

Available "over the sympathomimetic amine Dexatrim; counter", appetite suppressant
Phenoxine; Phenyldrine; Propagest; Rhindecon Sibutramine Meridia Approved in US, 11/97 inhibits reuptake of dopamine, norepinephrine, and serotonin in brain
Various natural herbal weight reduction formulas have been suggested as safer alternatives to both prescription and over-the-counter weight loss compounds. Generally, herbal weight loss formulas have fewer side effects when properly formulated and
administered. Despite the fact that herbs are natural substances, however, some herbal formulas can still be abused. For example, improper administration of herbal weight loss formulas based primarily on ma huang (ephedra) and high caffeine-containing herbs, such as guanrana and kola nut, may result in diminished energy and a depleted body.
New compounds for treatment of humans are often tested in animal models to insure their safety and efficacy. A number of rat models have been used to study the effect of drugs on obesity. Diet-related obesity can be created in the Osbom-Mendel, Wistar and Sprague-Dawley rats by altering their diets to increase caloric consumption. This is usually accomplished by increasing the percentage of fat in a carefully controlled diet and measuring a series of physiologic parameters that indicate changes in energy metabolism, weight gain, weight loss, body composition, and other indicia of overall health and the balance between food intake and energy expenditure. These rats experience the increased weight and fat deposition characteristically seen in obese humans. Using these models, compounds that are candidates for agents to control body weight and composition are tested for safety and efficacy. Typically, drugs that prevent

weight gain or cause weight loss in rat models are also effective In humans, albeit at a
slightly lower level of efficacy. Given the serious problems associated with obesity, and the significant drawbacks associates with many weight loss compounds, a need exists for a safe and effective composition that reduces weight gain, causes weight loss, and improves body composition.
A United States Patent No. 7,074,440 claims, "An herbal composition comprising: green tea, ginseng, 25 500 mg of konjac extract comprising 90% glucomannan, and seaweed, wherein each ingredient is present in an amount effective to promote body weight loss, or maintain or control body weight.
A United States Patent No. 7,150,889 claims, "A method of inhibiting obesity, which comprises administering or ingesting a composition comprising: (1) a biologically effective amount of an extract of a plant of the genus Eucalyptus as an the active ingredient, wherein the extract is obtained by grinding raw material of a Eucalyptus plant; and extracting the active ingredient from the ground raw material using a mixture of water and ethanol to obtain a resultant extract, and (2) a biologically acceptable carrier or diluent."
A United States Patent No. 7,144,865 claims, "A method of reducing body weight in an overweight or obese mammal, said method comprising: administering at least once daily

to the overweight or obese mammal a pharmaceutical composition; wherein said pharmaceutical composition comprises: a zinc cation and an anion, and cyclo-Hispro wherein said zinc cation is administered to the mammal in an amount from about 0.01 to about 1.4 mg/kg/day; and wherein the cyclo-Hispro is administered to the mammal in an amount from about 0.007 to about 1.4 mg/kg/day.
A United States Patent No. 7,138,107 claims, "A method of reducing food intake of a subject, comprising intranasal administration of a pharmaceutical composition comprising an effective amount of diltiazem to a subject in need of such treatment.
A United States Patent No. 7,135,199 claims, "an extract of mixed herb medicine, and a pharmaceutical composition for the prevention and treatment of obesity containing the extract as an effective ingredient or health food containing the same, more precisely, an extract of mixed herb medicine extracted from the mixture of cassia seeds (Cassia obtusifoliaa L.), green tea (Thea sinensis L.), eucommia bark (Eucommia ulmoides Oliver), garlic (Allium sativum var. pekinense), hawthorn (Crataegus Pinnatifida Bungea), fresh pine needle (Pinus densiflora Siebold et Zuccarini) and wormwood (Artemisia capillaris Thunberg) using water or aqueous alcohol solution, a pharmaceutical composition for the prevention and treatment oaf obesity containing the above extract and a fermented extract extracted after adding rice, malt and yeast to the above mixture, or health food containing the same. The extract of the present invention can be effectively

used for the prevention and the treatment of obesity by inhibiting weight gain by high-fat diet, lowering blood cholesterol and decreasing neutral fat (triglyceride).
A United States Patent No. 7,129,237 claims, "A compound of Formula I or a pharmaceutically acceptable salt thereof: ##STR00008## wherein R.sup.l is hydrogen, alkyl of 1 to 6 carbon atoms, alkanoyl of 2 to 6 carbon atoms, or carboarylalkoxy of 7 to 11 carbon atoms; R.sup.2 and R.sup.3 are each, independently, hydrogen, hydroxy, alkyl of 1 6 carbon atoms, alkoxy of 1 6 carbon atoms, halogen, carboxamido, carboalkoxy of two to six carbon atoms, perfluoroalkyl of 1 6 carbon atoms, cyano, alkanesulfonamido of 1 6 carbon atoms, alkanesulfonyl of 1 6 carbon atoms, alkanamido of 1 6 carbon
atoms, amino, alkylamino of 1 6 carbon atoms, dialkylamino of 1 6 carbon atoms per alkyl moiety, perfluoroalkoxy of 1 6 carbon atoms, alkanoyloxy of 2 to 6 carbon atoms, alkanoyl of 2 to 6 carbon atoms, aroyl of 6 to 8 carbon atoms, aryl of 5 to 7 carbon atoms, a C.sub.6 to C.sub.13 alkylaryl group having 5 to 7 carbon atoms in the aryl moiety, a 5 to 7 membered heteroaryl group, or a 6 to 13 membered alkylheteroaryl group having 5 to 7 members in the heteroaryl moiety, wherein any R.sup.2 or R.sup.3 substituent having an aryl or heteroaryl moiety may optionally be substituted on the aryl or heteroaryl moiety with 1 to 3 substituents independently selected from a halogen atom, a C.sub.l C.sub.6 alkyl group, or a C.sub.l C.sub.6 alkoxy group; R.sup.4 and R.sup.5 are taken together with the carbons to which they are attached, to form a cyclic moiety selected from a cycloalkane of 4 to 8 carbon atoms, cycloalkene of 4 to 8 carbon atoms, bridged bicyclic alkane of 5 to 10 carbon atoms, bridged bicyclic alkene of 5 to 10 carbon atoms, pyran or thiopyran in which the sulfur atom is optionally oxidized to the sulfoxide or sulfone, wherein the cyclic moiety formed by R.sup.4 and R.sup.5 may optionally be

substituted with 1 to 3 substituents independently selected from a halogen atom, a C.sub.l C.sub.6 alkyl group, or a C.sub.l C.sub.6 alkoxy group; R.sup.6 and R.sup.7 are each, independently, hydrogen or alkyl of 1 to 6 carbon atoms; n is 1; and a dotted line represents an optional double bond.
A United States Patent No. 6,780,440 claims, "An oral herbal composition for the
treatment of diabetes and weight loss management in patients consisting of 0.01 to 4.0 grams of Ferula hermonis, wherein Ferula hermonis consists of the sesquiterpenes: 8,9-epoxy jaeschkeanadiol benzoate (epoxy ferutinol benzoate, (3)): jaeschkeandiol vanillate (ferutinol vanillate, (4)); jaeschkeanadiol p-hydroxybenzoate (ferutinin, (1)); jaeschkeanadiol benzoate (Teferdin, (2)); jaeschkeanadiol (ferutinol, (5)) 8,9-epoxy jaeschjeanadiol (12); 14-(14'-hydroxybenzoyloxy) dauc-4,8-diene (6); 14-(14'-hydroxy-3'-methoxy-benzoyloxy) dauc-4,8-diene (7); 14-benzoyloxy-dauc-4,8-diene (10); 8,9-epoxy jaeschkeanadiol p-hydroxybenzoate (Tenuferidin (11)); and jaeschkeanadiol p-methoxybenzoate (8); 8,9-epoxy jaeschkeanadiol m,p-dihydroxybenzoate (9), with one or more of selected herbs, and mixture thereof.
An ideal and acceptable weight should provide the following advantages: minimized side effects, increased ease of administration, weight loss without causing other diseases, and improved weight loss. In recent years, considerable attention has been directed to the development of implantable, intrauterine, cervical or vaginal fertility control delivery systems to provide a prolonged and controlled administration of steroidal

hormones to the body for achieving fertility control. However, none of the delivery systems developed so far can be considered ideal and free of side effects.
The objective of the present invention is to provide compositions and methods for inducing antifertility conditions in the females. The invention is based on a known
naturally occurring botanical, which offers a new category of antifertility agents to be used by women.
The present invention relates to the identification of a naturally occurring species from botanical family Rhamnaceae and preferably from the genus zizyphus. These naturally occurring botanical sources have been traditionally utilized for variety of treatments however it had not been not disclosed that extracts of stem bark and leaves and compositions described herein would offer remarkable potential for the induction of body weight loss.
Specifically, the botanical plant employed in the present invention is belonging to the genus zizyphus. Some species of it are as follows, zizyphus sativa, zizyphus numularia, Zyziphus oenoplia, Zizyphus jujuba, Zizyphus rugosa, Zizyphus mauritiana, Zizyphus xylocarpus, Zizyphus trinervia, Zizyphus fumiculosa, Zizyphus oxyphylla, Zizyphus vulgaris, Zizyphus glabrata, Zizyphus laccifera, Zizyphus hutchinsonii, Zizyphus mucronata, Zizyphus lotus, Zizyphus napeca, Zizyphus mistol, Zizyphus

hysodrica, Zizyphus juazero etc. In the preferred embodiment the invention comprises of extracts of bark and decoction of bark, which includes at least one of the species of zizyphus listed above.
The present invention utilizes the inner stem bark and leaves of zizyphus genus. This plant is widely grown in India, South Asia in dry areas with moderate temperature conditions. In the preferred embodiment of the present invention the bark and leaves used are from the variety in Maharashtra. It is known as Zizyphus mauritiana Lamk and differs from other varieties in habit of tree, shape of leaf, size, colour and keeping quality of fruit and fruiting season. This tree acts as a host tree for growth of insects which produce lacca.
The compositions for oral use disclosed in the present invention have shown promising potential for reduction of body weight in animals models such as mice , rats without affecting much their food intake. The doses of the extract and the decoctions used have found to be safe. An acute oral toxicity study with a single dose of 5000mg/kg has not shown any adverse effects.
The herbal preparations can be prepared by number of formulations varying from consuming the aqueous extract powder or decoction drink with water of the bark or leaves for weight reduction. The extracts can be prepared with water using Soxhlet extraction method. The liquid extracts so obtained can be concentrated under reduced pressure. The decoction of the bark can be prepared by using freshly obtained, dried and coarsely powdered inner bark and adding 16 times its weight water to it. These

ingredients can be boiled till about 1/8 of original volume of liquid is left which is then filtered.
The decoction of leaves can be prepared in water by using freshly collected and washed leaves and equal quantity of water by weight (1:1). These ingredients are boiled till half the initial volume of liquid is left which is then filtered. The oral compositions can also be administered in a pharmaceutical dosage form suitable for enteral administration to humans such as flavoured syrup, suspension or emulsion.

1. A method of inhibiting obesity, which comprises administering or ingesting a composition comprising a pharmaceutically and biologically effective amount of an extract of a plant of the genus from plant Zizyphus mauritiana Lamk as an the active ingredient, wherein the extract is obtained by grinding raw material from the plant Zizyphus mauritiana Lamk plant
2. A composition of claim 1, wherein the said composition is obtained from the bark
or leaves of plant Zizyphus mauritiana Lamk.
3. A composition and method of claim 1, wherein the said composition is administered orally.
4. A composition and method of claim 3, wherein the oral composition can be administered in a pharmaceutical dosage form suitable for internal administering humans such as flavored syrup, suspension or emulsion with edible vegetable oil.

Dated this 19th December, 2006

A pharmaceutical composition suitable for regulating body weight, especially for promoting body weight loss comprising of the herb or a plant Zizyphus mauritiana Lamk or extracts of its bark or leaves for reducing body weight.






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Patent Number 242722
Indian Patent Application Number 2159/MUM/2006
PG Journal Number 37/2010
Publication Date 10-Sep-2010
Grant Date 07-Sep-2010
Date of Filing 29-Dec-2006
Name of Patentee Dr. Kishori Ganpat Apte
Applicant Address Survey No. 36/1/1, MN 199, Wadgaon Khurd, Sinhagad Road, Pune 411 041,
# Inventor's Name Inventor's Address
1 Dr. Kishori Ganpat Apte Survey No. 36/1/1, MN 199, Wadgaon Khurd, Sinhagad Road, Pune 411 041,
2 Dr. Vaishali Vasant Potnis Survey No. 36/1/1, MN 199, Wadgaon Khurd, Sinhagad Road, Pune 411 041, Maharashtra, India
PCT International Classification Number A61K35/00, A23L1/09
PCT International Application Number N/A
PCT International Filing date
PCT Conventions:
# PCT Application Number Date of Convention Priority Country
1 NA