Title of Invention	"A PROCESS FOR THE PREPARATION OF A SPERMICIDAL SUBSTANCE"
Abstract	A process for the preparation of spermicidal substance comprising dissolving a spermicidal agent of neem as herein described in an emulsifier in the ratio of 1;1.3::1:1.7 mixing said solution of the spermicidal agent with a herbal agent in the ratio of 1:1 to 5:1, and a vehicle as herein described and having a molecular weight between 1000-3000 being added into said mixture.

Full Text

FIELD OF INVENTION. This invention relates to a process for the preparation of a spermicidal substance. In particular, this invention relates to a process for the preparation containing neem, which is in the form of pessary. 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 speraicidel agent. However, a disadyantage associated with such a spermicidal preparation, and as described herelnaboye, la that certain of the neem oil residues 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 spermicidal preparation containing neem. Another object of this invention is to propose a process for the preparation of a sperinicidal preparation containing neem which is efficient. Still another abject of this invention is to propose a process for the preparation of a spennicidel preparation containing neem which has no side effects. yet another object of this invention is to propose a process for the preparation of a spermlcidal preparation containing neem which is in the form of a pessary, which thus avoids the possibilities of any infection as may be imported by the use of an applicator. At the outset of the description, which follows, it is to be understood that the ensuing description only illustrates a particular form of this invention. Such a particular form is only an exemplary embodiment and without intending to be imply any restriction to the scope of the invention. Any suitable modification or improvement occurring to a man in the art is also within the scope of the invention. BRIEF DESCRIPTION OF INVENTION. According to this invention there is provided a process for the preparation of spermicidal substance comprising dissolving a spermicidal agent of neem as herein described in an emulsifier in the ratio of 1 1.3::l;1.7 mixing said solution of the spermicidal agent with a herbal agent in the ratio of 1:1 to 5:1, and a vehicle as herein described and having a molecular weight between 1000-3000 being added into said mixture. In accordance with this invention, the spermicidal preparation is in the form of a pessary which is locally applied into the vagina, and thus avoids the danger of containination by an applicator. The spermicidal preparation prepared by the process 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.!272/De!/93 and 1713/Del/94. Patent application No.l272/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 miscibie solution containing odoriferous constituents, subjecting the miscibie 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 1:3 to 3:1. The spermicidal preparation further comprises a vehicle, which may be selected from a singular or a combination of polymer. Thus, and as by way of example, the vehicle may comprise a combination of a first polyethylene glycol having a first molecular weight and a second polyethylene glycol having a second molecular weight, higher than the first polyethylene glycol, and wherein the polyethylene glycol of a higher molecular weight is present in a greater amount than the polyethylene glycol of a lower molecular weight, The vehicle may also for example comprises carboxy methyl cellulose, polyvinyl pyfrolidine or glycol gelatin. Preferably, the average range of molecular weight is between 1000-3000 and preferably 1250-1500. The invention resides in the step of admixing any known emulsifier. 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 effect among the ingredient thereof The preparation is novel and useful and no chemical reaction exist. EXAMPLE 1 For every 1 pessary 0.400 gm of polyethylene glycol of a molecular weight 1500 was mixed with 0.300 gms of polyethylene glycol of a molecular weight 1000. The mixture was melted slowly over a water bath. 0,125 gms of Tween - 80 as an emulsifier was dissolved in 0.75 gm of the active neem component and 0.75 gms of mint, and this mixture was dissolved in the molten polyethylene glycol mixture. It was immediately poured into necessary mould, cooled and removed. EXAMPLE 2. For every 1 pessary 0.400 gm of polyethylene glycol of a molecular weight 1500 was mixed with 0.300 gms of polyethylene glycol of a molecular weight 1000. The mixture was melted slowly over a water bath. 0.125 gms of Tween — 80 as an amuleifier was dissolved in 0.100 gm of the active neem component and 0.50 gm of lemon grass and this mixture was dissolved in the molten polyethylene glycol mixture. It was immediately poured into necessary mould, cooled and removed. Example 3. For every 1 pessary 0.400 gm of polyethylene glycol of a molecular weight 2000 was mined with 0.300 gms of polyethylene glycol of a molecular weight 1500. The mixture was melted slowly over a water bath. 0.125 gm* of Tween - 80 as an emulslfier was dissolved in 0.75 gm of the active neem component and 0.75 gms of mint and this miMture was dissolved in the molten polyethylene glycol mixture- It was immediately poured into necessary mould, cooled and removed. The preparati ons of Examples 1 to 3 were subjected to the following evaluationi 1. Physical Evaluations a) Melting point b) Hardness c) Dissolution a) Melting Points Melting point of the formulations was determined using capillary tube method. All the formulations started melting at 37°C and liquefied at 38°. b) Hardness, Hardness was deter mined using Stokes Hardness Tester. The average hardness of the pamaries Has found tobe 1-5 kg/cm2 which is acceptable. c) Dissolution A pessary was taken and placed between two wire mashes of sieve No.9, This was kept in a static waterbath 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 2.0 minutes for Formulation 31 and 1-5 minutes for Formulation 32 and 33. BIOLOGICAL ACTIVITY: One pessary Mas taken and dissolved in 25mI of buffer solution of pH 4.4. 100MC of this solution was added to 100mc of semen, mixed and examined undar microscope. All the sperms were found in motile within 10 seconds. TABLE 2a Evaluation of pessaries 61 Formulation Melting Hardness Dissolution Biological No. No Point Kg/c02 (seconds) activity. 1 1 37-39°C 1.44-10 120 + 5 Active at — - this con-centration in lass than 10 sec. 2 2 37-39°C 1.4+25 90 + 5 " 3 3 37-39°C 1.4+10 90 + 5 " * Average of 5 determinations. We Claims:- 1. A process for the preparation of spermicidal substance comprising dissolving a spermicidal agent of neem as herein described in an emulsifier in the ratio of 1;1.3::1:1.7 mixing said solution of the spermicidal agent with a herbal agent in the ratio of 1:1 to 5:1, and a vehicle as herein described and having a molecular weight between 1000-3000 being added into said mixture. 2. A process as claimed in claim I wherein said vehicle comprises polyethylene glycol, carboxy methyl cellulose, polyvinyl pyrrolidine, glyco gelatin either alone or in combination thereof. 3. A process as claimed in claim 2 wherein said vehicle has a first polyethylene glycol having a first molecular weight (of 1000-1500) and a second polyethylene glycol having a second molecular weight (of 1500-2000), higher than the first polyethylene glycol, wherein said second polyethylene glycol is present in the amount greater than said first polyethylene glycol. 4. A process as claimed in claim 2 wherein said vehicle has a molecular weight preferably between 1250-1500. 5. A process as claimed in claim 1 wherein said spermicidal agent and herbal agent are present in the spermicidal preparation preferably in the ratio of 1:1 to 3:1. 6. A process as claimed in claim 1 wherein said herbal agent are selected from essential oils, such as oil of citronella, lemon grass, mint, geranium or palma rosa. 7. A process for the preparation of a spermicidal substance substantially as herein described.

Documents:

491-del-1998-abstract.pdf

491-del-1998-claims.pdf

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

491-del-1998-correspondence-others.pdf

491-del-1998-correspondence-po.pdf

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

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

491-del-1998-form-1.pdf

491-del-1998-form-2.pdf

491-del-1998-form-3.pdf

491-del-1998-form-4.pdf

491-del-1998-form-6.pdf

491-del-1998-form-9.pdf

491-del-1998-gpa.pdf

491-del-1998-petition-others.pdf