EP0065385A2
Expired / Lapsed
EP
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Methods and compositions for intravaginal contraception
Assignee: Syntex USA LLC
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Filing: 1982-05-06
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Granted: —
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Expires: 2002-05-06
Abstract
Abstract A gel formation, which is inherently spermicidal and which provides an efficient delivery system for spermicidal and other contraceptively effective compounds intravaginally is disclosed. A contraceptive composition incorporating it comprises: a) a contraceptively effective amount of a sperm function inhibitor; b) between about 10% and 30% by weight of a polyoxyethylene-polyoxypropylene block copolymer, having an average molecular weight between about 5,000 and 15,500; and c) water, and, optionally, other non-toxic pharmaceutically acceptable excipients.
Inventors
- 👤 Brian H. Vickery
- 👤 Shabbir Anik
- 👤 Richard E. Jones
Bibliographic Details
Application Number
—
Jurisdiction
EP
Data Source
google_patents
Last Synchronized
2026-11-05 00:34
CPC Classifications
A; A61; A61K; A61K31/00; A61K31/33; A61K31/395; A61K31/41; A61K31/415; A61K31/74; A61K31/765; A61K31/77; A61K9/00; A61K9/0012; A61K9/0034; Y; Y10; Y10S; Y10S424/00; Y10S424/14
Claims Analysis
Total Claims: 16
Claim 1
Independent Claim
52 words
A contraceptive gel composition for intravaginal application, which comprises: a) a contraceptively effective amount of a sperm function inhibitor; b) between about 10% and 30% by weight of a polyoxyethylene-polyoxypropylene block copolymer, having an average molecular weight between about 5,000 and 15,500; and c) water, and, optionally, other non-toxic pharmaceutically acceptable excipients.
Claim 2
Dependent Claim
52 words
A contraceptive gel composition for intravaginal application, which comprises: a) a contraceptively effective amount of a sperm function inhibitor; b) between about 10% and 30% by weight of a polyoxyethylene-polyoxypropylene block copolymer, having an average molecular weight between about 5,000 and 15,500; and c) water, and, optionally, other non-toxic pharmaceutically acceptable excipients.
Claim 3
Dependent Claim
22 words
The composition of claim 1 wherein the polyoxyethylene-polyoxypropylene block copolymer in (b) is between 15% and 20% by weight of the gel.
Claim 4
Dependent Claim
25 words
The composition of claim 1 or claim 2 wherein the polyoxyethylene-polyoxypropylene block copolymer in (b) has an average molecular weight between about 10,000 and 12,000.
Claim 5
Dependent Claim
46 words
The composition of any one of claims 1, 2 and 3 wherein the other non-toxic pharmaceutically acceptable excipients in (c) include about 10% to 30% by weight of polyethylene glycol of average molecular weight 400 and about 10% to 30% by weight of lower alkylene glycol.
Claim 6
Dependent Claim
20 words
The composition of any one of the preceding claims wherein the sperm function inhibitor in a) is a 1-substituted imidazole.
Claim 7
Dependent Claim
80 words
A contraceptive gel composition for intravaginal application which consists essentially of (a) between about 0.01% and 1% of a 1-substituted imidazole, as a sperm function inhibitor; (b) between about 15% and 20% by weight of polyoxyethylene-polyoxypropylene block copolymer having an average molecular weight between about 10,000 and 12,000; and (c) between about 10% and 30% by weight of polyethylene glycol of average molecular weight 400 and between about 10% and 30% of glycerin, water, and optionally non-toxic pharmaceutically acceptable excipients.
Claim 8
Dependent Claim
80 words
A contraceptive gel composition for intravaginal application which consists essentially of (a) between about 0.01% and 1% of a 1-substituted imidazole, as a sperm function inhibitor; (b) between about 15% and 20% by weight of polyoxyethylene-polyoxypropylene block copolymer having an average molecular weight between about 10,000 and 12,000; and (c) between about 10% and 30% by weight of polyethylene glycol of average molecular weight 400 and between about 10% and 30% of glycerin, water, and optionally non-toxic pharmaceutically acceptable excipients.
Claim 9
Dependent Claim
84 words
The composition of claim 5 or claim 6 wherein the 1-substituted imidazole in (a) is of the formula or a pharmaceutically acceptable salt thereof, wherein R 1 and R 2 are each independently alkyl, alkenyl, phenyl, phenyl lower alkyl, or-phenyl.lower alkenyl wherein each phenyl ring is optionally substituted by one or more lower alkyl, halo, lower alkoxy, trifluoromethyl, nitro or cyano groups; R 3 is hydrogen or lower alkyl; X is oxygen or sulfur; and n is an integer of from 1 to 4.
Claim 10
Dependent Claim
59 words
The composition of claim 7 wherein R 1 is alkyl of four to eight carbon atoms; R 2 is benzyl optionally substituted by one or more lower alkyl, halo, lower alkoxy, trifluoromethyl, nitro or cyano; R 3 is hydrogen or lower alkyl; X is oxygen or sulfur; and n is 1; or a pharmaceutically acceptable acid addition salt thereof.
Claim 11
Dependent Claim
35 words
The composition of claim 8 wherein R 1 is n-hexyl, R 2 is 2,4-dichlorobenzyl, R 3 is hydrogen, X is oxygen and n is 1, namely, 1-[2-(2,4-dichlorobenzyloxy)-n-octyl]imidazole or a pharmaceutically acceptable acid addition salt thereof.
Claim 12
Dependent Claim
21 words
The composition of any one of claims 1 to 4 wherein the sperm function inhibitor in a) is an acrosyn inhibitor.
Claim 13
Dependent Claim
25 words
The composition of any one of the preceding claims wherein the sperm function inhibitor in a) is about 0.01 - 1% wt/volume of the composition.
Claim 14
Independent Claim
46 words
A method of contraception in human beings which method comprises administering, intravaginally, prior to coitus, to a female subject in need of, or desirous of, protection against conception, between about 0.5 ml and 6 ml of a gel composition of any one of the preceding claims.
Claim 15
Dependent Claim
19 words
The method of claim 12 wherein the amount of composition administered is between about 0.5 ml and 2 ml.
Claim 16
Dependent Claim
23 words
The method of claim 12 or claim 13 wherein the composition is administered between about 8 hours and 2 minutes prior to coitus.
References Cited (Backward Citations)
No citation records indexed.
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