PHARMACEUTICAL COMPOSITIONS

摘要

1,204,171. Contraceptive compositions. H. SMITH. 11 Sept., 1967 [29 June, 1967], No. 41288/67. Heading A5B. Contraceptive compositions comprise as antifertility agent, a steroid of general formula: in which R1 is a lower alkyl group having 2 to 6 carbon atoms; X is a hydrogen, oxo, thioketalised oxo, hydroxy or acyloxy group; Y is an acetylmethylene group or a halogen substituted or unsubstituted alkyl, alkenyl or alkynylhydroxy-methylene group or its 17-ester or spirocycloalkylanalogue; Z is methylene or a hetero-atom and ring A contains a double bond at the 4 (5)-position optionally with a further double bond at the 9 (10) or 6 (7)- positions or contains a double bond at the 5(10)-position optionally with a further double bond at the 6(7) position, with one or more optional alkyl substituents, at the 6, 7 or 16- positions, or its D-homo analogue, in association with a pharmaceutically acceptable carrier (a) in an amount of form 5 to 150 micrograms (5 to 90 micrograms when Y is a haloalk-1-ynylhydroxymethylene, haloalk-1-ynylacyloxymethylene, ethynylacyloxymethylene or acetylmethylene group) formulated for daily administration and release in one day or (b) formulated as a delayed release composition for administration less frequently than daily comprising an amount of from 5 to 150 micrograms multiplied by the number of days over which it is to be released. Preferred compounds include dl-13#-ethyl-17α-ethynyl-17#- hydroxygona-4, 9-dien-3-one and d-13#-ethyl -17#-hydroxy-17α-vinylgon-4-en-3-one. The anti-fertility agent may be present as the racemate or d-enantiomer. The composition may be administered orally, parenterally or rectally in the form of tablets, capsules, powders, dispersible granules, cachets, solutions, suspensions, emulsions, vials, ampoules, suppositories or a delayed release composition, such as an implant, containing a plastic or a modified carboxymethyl cellulose.