Contraceptive compsn. with reduced hormone dose and reduced side-effects - contg. synergistic mixt. of biogenic, synthetic oestrogen and gestagen

摘要

Combination prepn. for contraception contains, as essential element, a mixt. (M) of biogenic oestrogen (I); synthetic oestrogen (II) and a gestagen (III). It opt. includes,. as (a) placebos; (b) biogenic or synthetic (III); (c) (I) or (II)); (d) a mixt. of (I), (II) and (III), or (e) a mixt. of (II) and (III). (I) is (Ia), oestrone, oestrane or oestriol; (II) is (IIa) or (IIb), (III) is (IIIa), desogestrel, progesterone, norethisterone acetate, chlormadinone acetate, gestodene, or cyproterone acetate, or any precursor which rapidly release such cpds. after admin.. USE/ADVANTAGE - The prepn. is used for oral (esp), intravaginal or transdermal hormone delivery. Simultaneous admin. of (I) and (II) produces a synergistic effect, so the total dose of hormone required is reduced with a consequent redn. in side effects. The daily dose, in (M), is 0.005-0.1mg ethynyl-oestradiol (IIa) or mestranol (IIb); 1 mg oestradiol (In), or its valerate, or oestrone sulphate, plug the usual recommended doses of (III), e.g. 0.125 mg/day for levonorgestrel (IIIa). Typical formulations are tablet, capsules, pessaries and transdermal patches.