PHARMACOKINETICS OF CENTCHROMAN IN HEALTHY FEMALE SUBJECTS AFTER ORAL-ADMINISTRATION

The pharmacokinetics of centchroman, a non-steroidal antifertility age nt, were assessed in serum of eleven healthy female subjects after a s ingle 30 mg oral dose. Maximum serum concentration (C-max) of 55.53 (s .d., 15.45) mu g/L was attained at 5.18 (s. d., 1.78) h after oral adm inistration. The concentration-time profile was best described by a tw o-compartment open model with bi-exponential disposition functions. Th e mean terminal elimination half-life (t(1/2)) was 165 (s.d., 49) h wi th a clearance of 6.17 (s.d., 1.67) L/h and volume of distribution of 1420 (s.d., 478) L. Comparison of the pharmacokinetic parameters of th is study with those obtained after a single 60 mg oral dose did not sh ow statistically significant differences in the rate of absorption, di stribution and elimination. The C-max and AUCo(x) were dose-dependent. Thus, the absorption and disposition Of centchroman are of first-orde r, reproducible and dose-independent.