STABLE OILY PREPARATIONS OF EPITHIO-STEROIDS

1318662 Stable compositions of epithio steroids SHIONOGI & CO Ltd 8 June 1971 [8 June 1970 (2)] 19485/71 Heading A5B [Also in Divisions C2 and C5] Epithiosteroids are stabilized by admixture with pharmaceutically acceptable oils having peroxide values POV of 0-2.5 (POV is the amount in mg. of active oxygen in 100g. of oil.) The resulting compositions are hormonally active, especially as anti-progestational, anti-estrogenic, myogenic, anti-lipaemic and androgenic agents, and retain their activity for longer periods than similar compositions made with oils of higher POV values. The steroids may, for example, be of the androstane, estrane, pregnane, cholane or cholestane series or nor or homo homologues thereof and may contain an epithio group at, for example, position 1,2; 2,3; 3,4; 4,5; 5,6; 6,7; 11,12; 14,15; 15,16; or 16,17 and one or more substituents selected from, for example, halogen atoms, double bonds and alkyl, alkenyl, acyloxy, cycloalkenyloxy, alkoxy cycloalkyloxy, alkoxycycloalkenyloxy, hydroxy, oxo, ketal, carboxyl and esterified carboxyl groups. Suitable oils include vegetable oils, C 1-10 alkyl esters of C 6-18 fatty acids and glycerides of C 8-10 fatty acids, and mixtures thereof. The compositions can be prepared simply by dissolving the steroid in the oil, possibly with gentle heating, e.g. 40‹-70‹C, and desirably in an inert atmosphere. The compositions are preferably prepared as injection solutions but they may also be made up into other dosage forms such as capsules. They may also contain antiseptics, bacteriostats and/or preservatives.