Title of Invention	" A COMPOSITION FOR CONTROL OF FERTILITY IN FEMALES"
Abstract	A pharmaceutical composition suitable for inducing anti fertility or preventing conception in females comprising of a specific botanical plant wherein a composition for both oral use and topical use in vagina comprising the herb or a plant Zizyphus mauritiana Lamk or extract of its bark or leaves in inducing anti fertility is used in females.

Full Text

FORM-2 THE PATENTS ACT, 1970 (39 of 1970) COMPLETE SPECIFICATION (Section 10, Rule 13) "A Composition and Method for control of fertility in females" I, Ms. Vaishali Vasant Potnis H-14, Yashomangal Apartments Pimpri Chinchwad Link Road Near Chinchwad Pumping Station Chinchwad - 411033, Maharashtra State, India The following specification particularly describes the nature of the invention and the manner in which it is to be performed: - 1 A Composition and Method for control of fertility in females Field of the invention: The invention relates to a composition for preventing conception in females. Particularly, the invention relates to compositions and methods for controlling fertility in adult women. More particularly, the invention concerns the use of extracts of bark of Zizyphus mauritiana Lamk for preventing conception in women. Background of the invention: Population control is a major concern worldwide, in particular for developing nations like India and China. India's population has already crossed the one billion mark and is growing at a steady fast rate. Scientists and economists believe that high rate of population growth is one of the major causes deterring the economic development of the country. As per the recent survey and studies conducted, around 50% of the country's population is in sexually active age group. Various socioeconomic causes, lack of sex education and lack of easy access to various birth control means are the main reasons for causing the uncontrolled population explosion. 2 There have been various endeavours and measures for preventing pregnancy in females. They include mechanical as well as medicated products to be used by females and males. Some of them are used prophylactically for prevention of unwanted pregnancies while some are available to terminate the pregnancies. The female anti fertility agents that prevent ovulation and/or fertilization of ovum are referred to as contraceptive agents. Those agents act after the implantation of the fertilized egg are called as antiimplantation agents or abortificients. Latter can further be subdivided into emmenogogues (menstruation stimulators) or echolics(uterine contractors). The term interceptive has been used to refer to compounds that act after the occurrence of fertilization but prevent implantation of fertilizes egg. By this definition, the compounds interfering with the secretion of proper amounts of steroids needed during this time period whether acting directly on the ovaries or indirectly by inhibiting gonadotropin or prolactin secretion can be referred to as interceptive. Drugs altering the ova transport (vide supra) can also be considered as interceptive like others, which destroy the fertilized ova or blastocysts, trophoblastsor act on uterus to prevent implantation. Additionally, various intra uterine and intra vaginal devices either non-medicated or medicated like copper- T, progestasert have found most acceptable status as female antifertility devices. The female condoms, vaginal diaphragms cervical caps, vaginal rings, vaulta caps and vaginal pessaries also constitute antifertility devices. 3 However, the most widely used contraceptives are oral hormonal preparations such as combined estrogen-progesterone pills or progesterone only pills, monophasic, biphasic, triphasic pills. Some injectable contraceptives include once a month injections of combined estrogen/progesterone biodegradable microcapsules and subcutaneous implants. Some pills are also recommended for emergency contraception in case unprotected sexual contact. They are to be consumed within 72 hours. The products for termination of pregnancy include abortificients such as prostaglandin, PGE2 and PGF2 alpha, intra-amniotic injections of hypertonic saline or 40% urea solution. Prostaglandin can also be given as extra-amniotic solution or gel through the cervical canal into the extra-amniotic space. Substantially continuous attention is focused on the development of improved contraceptive methods. One widely exploited technology is the use of spermicides, essentially a chemical barrier that prevents penetration of sperm to the uterus or egg, or inhibits the activity thereof, thereby precluding fertilization. One of the most widely used spermicides is a detergent, Nonoxynol-9. Reports indicate an increased incidence of urogenital infections and cervicovaginal inflammation in women employing this detergent spermicide. McGroarty et al, Journal of Urology, 152(3):831 833 (1994). However, at present, all commercially available spermicidal contraceptives have detergent ingredients that disrupt cell membranes. These include the neutral surfactants isononyl-phenyl-polyoxyethylene (9) ether or nonoxynol-9 (N-9), p-menthanyl-phenyl-polyoxyethylene (8,8) ether or menfegol, and isooctyl-phenyl-polyoxyethylene (9) ether 4 or octoxynol-9 (0-9) (Digenis G A, et al., Pharm Dev Technol, 1999;4:421-30; Furuse K, et al., J Pharmacobiodyn, 1983;6:359-72.) The detergent-type vaginal spermicide, N-9, available without a prescription, is the most commonly used spermicidal contraceptive in the UK and USA (OTC Panel, Federal Register, 1980;45:82014-49; Chantler E., Brit Fam Plann, 1992;17:118-9.) Worldwide, the cationic surfactant benzalkonium chloride and the anionic detergent sodium docusate (dioctyl sodium sulphosuccinate) are also used as vaginal spermicides (Mendez F, et al., Contraception, 1986;34:353-62.) N-9, sodium oxychlorosene, and benzalkonium chloride, have been used as gels, suppositories, ovules, sponges, or film. N-9 has been in use for more than 30 years in creams, gels, foams and condom lubricants. Typically, combinations of synthetic estrogen and synthetic progestin have been used in the past in orally administered dosage forms to control fertility. If a natural estrogen (17 beta estradiol) and progestin (progesterone) combination is to be used in the oral contraceptive pills, very large doses of these two hormones will be needed because of very extensive hepatic first-pass metabolism of the two hormones in the liver. The resulting metabolic products often cause undesired side effects. Therefore, a combination of synthetic progestin and estrogen are used to overcome the deficiencies. Although the combination of synthetic progestin and estrogen is very effective in suppressing ovulation, certain undesirable side effects are still prevalent with this type of oral contraceptive. The incidence of thromboembolic and related vascular disorders, including stroke and myocardial infarction, is higher in women using oral contraceptives; 5 the relative risk may be eleven times greater in users as compared to a control population. Further, the risk increases sharply in women over 35 years of age. Contraceptive use has also been associated with increased evidence of benign liver tumors and an increased risk of gallbladder disease. Additionally, fetal abnormalities may result if the mother continues to take the pill after becoming pregnant. Finally, some possible, but unproven complications of contraceptive use include breast cancer, and cancer of the uterus, cervix and vagina. In addition to the use of these modern pharmaceutical therapies various traditional remedies (traditional Ayurved medicines or traditional Chinese medicines) have been used by folklore or people living in countryside. Most of these traditional preparations make use of natural products including those derived from plants, animals and minerals. Many texts on Ayurved medicine describe various plants or their preparations as anti fertility agents. Some of them are prescribed exclusively for females and some are recommended for males and some are for both. In recent years much interest has been aroused in potential antifertility agents that are present in plants. Brief summary of the invention: Prior Art: A United States Patent No. 7,094,547 claims, "invention related to sperm specific surface proteins, nucleic acid sequences encoding those proteins and antibodies raised 6 against those proteins. Compositions comprising the sperm specific proteins or inhibitors of said proteins can be used in contraceptive applications. A United States Patent No. 7,067,162 claims, "a method for altering blood flow to the vagina of a female individual, comprising: administering to the female by inhalation of an odorant composition comprising a suprathreshold but not irritant concentration of a mixture of odorants effective to alter blood flow to the vagina, said concentration of the odorants being greater than an average normal threshold concentration of the odorants at about 25 55 decismel units; wherein the mixture of odorants is selected from the group consisting of a mixture of licorice-based and banana nut bread odorants, a mixture of licorice-based and cucumber odorants, a mixture of lavender and pumpkin pie odorants, and a mixture of baby powder and chocolate odorants; and the odorant composition is administered from a delivery device selected from the group consisting of a blister pack, a scratch-and-sniff odor patch, a scented cloth, and a spray device". A United States Patent No. 7,052,700 claims, "a composition comprising Ramulus Cinnamomi, Poria, Cortex Moutan, Radix Paeoniae Alba and Semen Persicae, wherein the composition is obtained by a method comprising steps of: a) obtaining, pruning, washing and cutting the plant parts: stem of Cinnamornum cassia Presl (Fam. Lauraceae), fungus of Poria cocos (Schw.) Wolf (Fam. Polyporaceae), root skin of Paeonia suffruticosa Andr. (Fam. Ranunculaceae), root of Paeonia lactiflora pall. (Fam. Ranunculaceae) and seed fruit of Prunus persica (L.) Batsch or Prunus davidiana (Carr.) 7 Franch. (Fam. Rosacese) b) drying the said plant parts to form 5 medicinal materials named, respectively: Ramulus Cinnamomi, Poria, Cortex Moutan, Radix Paeoniae Alba and Semen Persicae; c) Smashing Ramulus Cinnamomi, Semen Persicae and Cortex Moutan into coarse powders and chopping Radix Paeoniae Alba into slices; d) Sterilizing the Poria before granulating 50% of its formula weight into fine powder and filtering the powder; e) putting the powder of Cortex Moutan through a process of hot reflux in water and collecting its distillate, saving both the residue and fluid; f) filtering and vacuum-drying said distillate to obtain crude Paeonol; g) dissolving the crude Paeonol into 95% alcohol to form solution A; Slowly adding solution A into a saturated water solution of .beta.-cyclodextrin while agitating it at temperature of about 80.degree. C. to form mixture A; h) filtering mixture A and washing the residue with anhydrous alcohol and letting the washed residue dry to obtain clathrate A; i) distilling Ramulus Cinnamomi in water for four hours and collecting its volatile matter, saving both residue and fluid; j) dissolving the volatile matter into 95% alcohol to form a solution B; slowly adding the solution B into saturated water solution of .beta.-cyclodextrin while agitating it at temperature of about 45.degree. C. to form a mixture B; k) filtering mixture B and washing the residue with anhydrous alcohol and letting the washed residue dry to obtain clathrate B; 1) mixing residues frow step (e) and (i) with Radix Paeoniae Alba, Semen Persicae, 50% formula weight of Poria and 90% alcohol; extracting the mixture, filtering the extract and recovering alcohol from the filtered extract and saving the residue; m) adding water into the residue from step (1) distilling it and filtering the water extract; n) mixing the water extract from step (m), alcohol extract from step (1), fluid from step (e) and step (i); enriching the mixture to form a cream extract; o) mixing the cream extract 8 from step (n) with Poria powder from step (d), grinding the mixture into a fine powder after vacuum-drying it to form a granule; p) mixing the fine powder with an appropriate amount of 60% alcohol and starch sum and granulating the powder to 30 meshes to form a granule A; q) mixing an appropriate amount of silicon dioxide with clathrate A from step (h) and clathrate B from step (k); and r) mixing the mixture from step (g) with granule A from step (p) to obtain a final granule B~the composition. A United States Patent No. 7,045,145 claims, "A transdermal contraceptive delivery system (TCDS) for fertility control in women comprises a backing layer, an adjoining layer of a solid absorption adhesive polymer matrix in which effective daily doses of an estrogen and a progestin are dispersed and released for transdermal absorption. Presently preferred is the use of the synthetic estrogen, ethinyl estradiol, and the synthetic progestin, levonorgestrel. Along with these two steroidal contraceptive agents, a combination of several chemical skin permeation enhancing agents, including capric acid, blended at specific weight ratios, ranging from 2:1:1:0.8 to 6:1:1:0.8, are homogeneously dispersed in the adhesive polymer matrix. The invention also provides a method of fertility control utilizing the transdermal contraceptive delivery system. A United States Patent No. 6,995,251 claims, "a Ovary-specific proteins O1-180, 01-184 and 01-23 6, polynucleotides encoding them, antibodies which are immunoreactive with them and vectors and host cells containing O1-180, 01-184 or 01-236 are provided. 9 Also provided are methods for detecting cell proliferative or degenerative disorders of ovarian origin and which are associated with 01-180, 01-184 or 01-236. Further provided are methods for the evaluation of potential contraceptives using the proteins of the invention, as well as methods for the screening for genetic mutations in signaling pathways that are associated with some forms of human infertility or gynecological cancers, also using the proteins/mRNAs/genes of the invention. The proteins/mRN As/genes of the invention may also be used as markers for identifying primary and metastatic neoplasms of ovarian origin and as indicators of developmental anomalies in prenatal screening procedures. Furthermore, assays of the proteins/mRNAs/genes of the invention can be used in diagnostic assays for detecting forms of infertility and other diseases, including germ cell tumors and polycystic ovary syndrome. The proteins of the invention may be useful targets for in vitro fertilization procedures or in enhancing the number of eggs that can be retrieved from the human donor, e.g., in enhancing the success rate. An ideal and patient-acceptable fertility control system should provide the following advantages: minimized side effects, increased ease of administration, rapid termination of treatment, and improved patient compliance. 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. 10 The objective of the present invention is to provide compositions and methods for inducing antifertility conditions in the females. The potential benefit is reduction of the side effects of continually using the typical pharmaceutical therapies and safe plant product that can be taken on a regular basis. The invention is based on a known naturally occurring botanical, which offers a new category of antifertility agents to be used by women. Accordingly, there is provided a composition comprising a herbal source such as bark of Zizyphus mauritiana Lamk. Besides the crude extracts of the bark of this plant a decoction of bark along with a natural resin lacca derived from an insect Laccifer lacca has also been found to be safe when tested on various animal models for its antifertility potential. Detailed description of the invention: The present invention relates to the identification of a naturally occurring species from botanical family Rhamnaceae and preferably from the genus zizyphus which when consumed during the days of menses can induce antifertility in females. Although these naturally occurring botanical sources have been traditionally utilized for variety of treatments, it had not been previously disclosed that the various extracts of stem bark as well as a herbal composition described herein would offer remarkable potential for the prevention of the conception in females. 11 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. More particularly, the present invention utilizes the inner stem bark of the plant Zizyphus genus. The 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 used is from the variety in Maharashtra. The plant species is known as Indian jujube, Chinese jujube etc. This variety differs in habit of the tree, shape of leaf, fruit size, color, flavor, keeping quality and fruiting season. The wood of this plant is used for making agriculture weapons, as timber and for producing good quality charcoal. The tree acts as a host plant for lacca producing insects. The decoction of bark is used to control diarrhoea and dysentery and to relieve gingivitis. The composition for oral use disclosed in the present invention has shown a promising antifertility potential in various animal models such as female mice, rats and 12 rabbits. The doses of various organic and aqueous extracts have been found to be safe. In fact an acute toxicity test was conducted in mice at single dose of 5000mg/kg and the product was found to be safe. The herbal preparation can be prepared by number of formulations varying from consuming the individual extract powders alone or in a decoction drink with water or applied vaginally as cream, gel or pessary for prevention of conception. The extracts can be prepared using various organic solvents like chloroform, ethyl acetate, and alcohol or as aqueous extract with water by Soxhlet extraction method. The liquid extracts so obtained can then be concentrated under reduced pressure. The decoction can be prepared in water by using freshly obtained and dried inner bark of stem and equal parts of lacca granules. The ratio of water used is 16 times by weight of the weight of the ingredients. The decoction is prepared by boiling these ingredients in water until approximately 1/8 of original volume of liquid is left. The decoction should be consumed with a sufficient volume of an edible vegetable oil preferably the sesame oil during first three days of menstruation. The oral composition can be administered in a pharmaceutical dosage form suitable for enteral administering humans such as flavored syrup, suspension or emulsion with edible vegetable oil. 13 Furthermore a vaginal gel can be prepared using pharmacologically suitable amount of aqueous extract powder of bark in a synthetic carbomer base suitable for vaginal use. The extract powder can be dissolved in water and the other cosolvents such as polyethylene glycol, propylene glycol, ethanol etc. The solution so obtained can be gradually added to the gel base, formed by dispersing the carbopol in water with continuous stirring. The vaginal application of gel in pharmacologically effective doses can be used prophylactically for modifying the vaginal environment making it non favorable for conception. The various organic extracts such as chloroform, alcohol when given to mature female mice orally at different doses , 250mg/kg and 500mg/kg for 7 consecutive days prior to mating with male and for 14 consecutive days during co-habitation with the male mice of proven fertility could prevent the conception between 85-100%. The aqueous extract at 500mg/kg could prevent the conception in mature female mice almost 100%. The decoction made by boiling the bark of Zizyphus mauritiana and lacca granules in water when given orally in doses of 0.5ml/animal could 100% prevent conception in mature female mice. When tested for estrogen potential at 500mg/kg in female mice the aqueous extract showed no estrogenic activity. Thus it can be considered safe for prolonged duration also. The vaginal gels containing different concentrations of aqueous extract which were tested in mature female rats over a period of 15 consecutive days. The vaginal 14 environment indicated presence of leucocytes, cell types which do not favor the estrus phase. 15 I Claim, 1. A composition and method for inducing anti fertility or preventing conception in females comprising administering of an effective dose of an active agent selected from plant Zizyphus mauritiana Lamk. 2. A composition of claim 1, wherein the said composition is obtained from the bark 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 Abstract A pharmaceutical composition suitable for inducing anti fertility or preventing conception in females comprising of a specific botanical plant wherein a composition for both for oral use and topical use in vagina comprising the herb or a plant Zizyphus mauritiana Lamk or extracts of its bark or leaves in inducing anti fertility is used in females.

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