Title of Invention	"A PROCESS FOR THE PREPARATION OF A SPERMICIDAL SUBSTANCE"
Abstract	A process for the preparation of spermicidal substance comprising mixing a spermicidal agent of neem as herein described with a herbal agent as herein described in the ratio of 1:1 to 5:1, a vehicle alongwith hydroxy carboxylic acids and sodium or potassium bicarbonate present in the amount of 5 to 20% by weight, being added to said mixture to get said preparation.

Full Text

F1ELD OF INVENTIQN. This invention relates to a process for the preparation of a spermicidal substance. In particular, this invention relates to a spermicidal preparation in the form of an effervescence vaginal tablet. PRIOR ART. It is generally known that antifertility activity can be effected by three methods. One such method is that of a spermicidal agent Sperms from the male organism are killed or prevented from reaching the uterus of a female organism as to prevent any fertilization. Yet another method is that the sperms are allowed to reach the uterus of a female organism. Such sperms fertilize the ovum and the fertilized ovum starts developing, and that the developing embryo travels to the wall of the uterus of a female organism and gets implanted. In such a method the implantation is prevented. The third method is to allow the implantation and the uterine milieu is altered and embryo separated and aborted. The present invention relates to a spermicidal preparation so as to prevent a fertilization- Neem seed extractives such as neem oil is known to have antifertility activity but its shelf life is short-Thus, it is known to subject neem oil to the step of steam distillation to obtain a spermicidal agent. However a disadvantage associated with such a spermicidal preparation, and as described hereinabove, is that certain of the neem oil residue* required for other biological activities such as anti-implementation pesiticidal activity etc, are destroyed- OBJECTS OF THE INVENTION An object of this invention is to propose a process for the preparation of a vaginal spermicidal tablet containing neem. Another object of this invention is to propose a process for the preparation of a vaginal spermicidal tablet containing neem which is efficient. Still another object of this invention is to propose a process for the preparation of a vaginal spermicidal tablet containing neem, which has no side effects. Yet another object of this invention is to propose a process for the preparation of a vaginal spermicidal tablet containing neem which enables a faster dissolution of the preparation when in contact with vaginal fluids. BRIEF DESCRIPTION OF INVENTION. According to this invention there is provided a process for the preparation of spermicidal substance comprising mixing a spermicidal agent of neem as herein described with a herbal agent as herein described in the ratio of 1:1 to 5:1, a vehicle alongwith hydroxy carboxylic acids and sodium or potassium bicarbonate present in the amount of 5 to 20% by weight, being added to said mixture to get said preparation. In accordance with this invention, the spermicidal preparation is in the form of a tablet. The spermicidal preparation comprises an active spermicidal agent prepared from neem oil and/or neem seed extractives. The spermicidal agent may be prepared by a process as described for example in copending patent application nos.1272/Del/93 and 1713/Del/94. Patent application N0.1272/Del/93-A process for the preparation of a spermicidal agent from neem oil and/or known extractive obtained from neem seeds comprising in the steps of subjecting neem oil and/or said extractives to the step of solvent partition in the presence of an aliphatic hydrocarbon solvent such as n-hexane in the ratio of 0.5:1 to 3:1 to obtain a precipitate containing essentially of bitter constituents and a miscible solution containing odoriferous constituents, subjecting the miscible solution to the step of enrichment in the presence of an aqueous alcohol solvent to obtain a fraction comprising of said solvent and said odoriferous constituents, distilling the aqueous alcoholic solvent to obtain a concentrated extract enriched with spermicidal agent. Patent application No.l713/Del/94 -A process for the preparation of spermicidal agent from neem oil and/or neem seed extractive comprising mixing neem seed extractive and/or neem oil with an aliphatic hydrocarbon solvent in the ratio of 0.5:1 to 3:1, for removal of bitter constituents by precipitation, subjecting the decanted solution to the step of distillation for removal of said solvent, charging the residue containing spermicidal constituents to the step of steam/hydro distillation to obtain a fraction enriched spermicidal agent. The spermicidal preparation further comprises a herbal agent selected from essential oils, such as oil of citronella, lemon grass, mint, geranium or palma rosa. Such a herbal agent masks the odour and potentiates the activity and imparts stability to the active component. The active neem component and herbal agent is present in the spermicidal preparation in the ratio of 1:1 to 5:1, and preferably 1:1 to3:1. The spermicidal preparation further comprises a vehicle, which may be selected from a single polymer. Thus, and as by way of example, the vehicle may comprise a polyethylene glycol having a molecular weight of 4000-8000. The vehicle may also for example comprises carboxy methyl cellulose, polyvinyl pyrrolidine or glyco gelatin. The spermicidal preparation further comprises a disaccharide such as maltose, sucrose etc., sodium or potassium bicarbonate, hydroxy carboxylic acids such as citric acid and tartaric acid and present in the amount of 5 to 20% of total weight of tablet. The additives comprising the disaccharide are as an energy supplement to the vaginal flora. The additives comprising hydroxy carboxylic acid and sodium bicarbonate enable a faster dissolution of the pessary tablet when in contact with the vaginal fluid. Further objects and advantages of this invention will be more apparent from the ensuing examples. The spermicidal preparation of the present invention is produced due to synergistic effects among the ingredients thereof. The preparation is novel and useful and no chemical reaction exists. EXAMPLE 1 0.500gms of Polyethylene glycol is melted and .100 gms of active neem component and 0.50 gms of lemon grass and cooled to solidify. The waxy solid is broken to granules and mixed with the granules of effervescent mixture of 0.210 gms of lactose, 0-340 gms of sodium bicarbonate, 0.120 gms of citric acid and 0.180 gms of tartaric acid- Such a mixture is compressed to tablet of 1.5 gm each. EVALUATIONS: Physical Parameters: HARDNESS: The hardness of the tablets were tested using stokes Hardness Tester. The average hardness of the 2 tablets tested was found tobe 2kg/cm . The hardness requirements of the conventional tablets is about 4kg/cm2 . Since these tablets contain PEG 6000, only softer tablets can be manufactured. The requirement of 4kg/cm2 of hardness does not apply here. FRIABILITY: The friability of the tablets were tested using Friability Testing Apparatus U.S.P. The loss .in weight was found tobe less than XX which is within the limits. DISSOLUTION: A Vaginal tablet was taken and placed between two wire meshes of sieve Wo. 9. This was Kept in a static water bath containing the buffer solution of pH 4.4 (corresponding to vaginal pH). The time taken for the two meshes to join together was noted as the time taken for complete dissolution. The average time taken for the completion of dissolution was found tobe 4 minutes. BIOLOGICAL ACTIVITY: The spermicidal activity of the tablets was carried out by the modified method of Sander & Coamer. One tablet was dissolved in 25 ml buffer solution of pH 4.4 and lOOmc from this solution was transferred to lOOmc of semen, mi?ted and examined under microscope for motile sperms. All the sperms were found immotile within 8 seconds, AGEING STUDIES: The tablets were repeatedly exposed to refrigeration temperature (4°C) and body temperature (37°C), 12 hours each, for a period of 1 week. The tablets were evaluated for the biological activity. No significant difference in activity was observed from these tablets, proving that the tablets were stable. We Claims :- 1. A process for the preparation of spermicidal substance comprising mixing a spermicidal agent of steem as herein described with a herbal agent as herein described in the ratio of 1:1 to 5:3, a vehicle alongwith hydroxy carboxylic acids and sodium or potassium bicarbonate present in the amount of 5 to 20% by weight, being added to said mixture to get said preparation. 2. A process as claimed in claim 1 wherein said vehicle is polyethylene glycol having a molecular weight of 4000-8000. 3. A process as claimed in claim 1 wherein said spermicidal agent and herbal agent present in the spermicidal preparation is preferably in the ratio of 1:1 to 3:1. 4. A process as claimed in claim 1 wherein said hydroxy carboxyfic acids are as citric acid and tartaric acid. 5. A process as claimed in claim 1 wherem said vehicle optionally is carboxy methyl cellulose, polyvinyl pyrrolidine or gtyco gelatin. 6. A process for the preparation of a spermicidal substance substantially as herein described.

Documents:

494-del-1998-abstract.pdf

494-del-1998-claims.pdf

494-del-1998-complete specification (granted).pdf

494-del-1998-correspondence-others.pdf

494-del-1998-correspondence-po.pdf

494-del-1998-description (complete).pdf

494-del-1998-description (provisional).pdf

494-del-1998-form-1.pdf

494-del-1998-form-2.pdf

494-del-1998-form-3.pdf

494-del-1998-form-4.pdf

494-del-1998-form-9.pdf

494-del-1998-gpa.pdf

494-del-1998-petition-others.pdf