Disposable intravaginal contraceptive devices releasing 1-substituted imidazoles

Claim 1

A contraceptive device which releases spermicide and a pharmaceutically acceptable chelating agent during intravaginal placement in a female mammal comprising (a) an inert, flexible polymeric material formed into a configuration suitable for vaginal insertion and long term retention in the vagina and permeable to the release of said spermicide and a pharmaceutically acceptable chelating agent; (b) an effective amount of a 1-substituted imidazole spermicide or the pharmaceutically acceptable acid addition salts thereof, included within the matrix of said polymeric material, the imidazole having the formula ##STR3## wherein: (i) R is alkyl of one to twelve carbon atoms, phenyl or phenyl-lower-alkyl of one to four carbon atoms wherein the phenyl ring is optionally substituted by one or more lower alkyl of one to four carbon atoms, lower alkoxy of one to four carbon atoms, halo or trifluoromethyl; R 2 together with R 3 is ethylenedithio or propylenedithio wherein the alkylene chain is optionally substituted by one lower alkyl of one to four carbon atoms; and n is 1, 2 or 3; (ii) R is cycloalkyl of five to seven carbon atoms or cycloalkylalkyl of six to ten carbon atoms; R 2 is hydrogen or lower alkyl of one to four carbon atoms; R 3 is alkyl of two to twelve carbon atoms, cycloalkyl of five to seven carbon atoms or cycloalkylalkyl of six to ten carbon atoms; and n is 1, 2 or 3; (iii) R is phenyl or phenyl-lower-alkyl of one to three carbon atoms wherein the phenyl ring is optionally substituted by one or more lower alkyl of one to four carbon atoms, lower alkoxy of one to four carbon atoms, halo or trifluoromethyl; R 2 is hydrogen or lower alkyl of one to four carbon atoms; R 3 is alkyl of one to twelve carbon atoms, phenyl-lower-alkyl of one to three carbon atoms wherein the phenyl ring is optionally substituted by one or more lower alkyl of one to four carbon atoms, lower alkoxy of one to four carbon atoms, halo, or trifluoromethyl; and n is 1, 2 or 3; (iv) R is alkyl of one to twelve carbon atoms; R 2 is hydrogen or lower alkyl of one to four carbon atoms; R 3 is hydrogen or alkyl of one to twelve carbon atoms; and n is 1, 2, 3 or 4; or (v) R and R 4 are each alkyl of one to twelve carbon atoms, alkenyl of two to twelve carbon atoms, phenyl, phenyl-lower-alkyl of one to four carbon atoms or phenyl-lower-alkyl of two to four carbon atoms wherein the phenyl ring is optionally substituted by one or more lower alkyl of one to four carbon atoms, lower alkoxy of one to four carbon atoms, halo, or trifluoromethyl; R 2 is hydrogen or lower alkyl of one to four carbon atoms; R 3 and X-R 4 wherein X is oxygen or sulfur; and n is 1, 2 or 3; and (c) an effective amount of a pharmaceutically acceptable chelating agent.