Pharmacokinetics of centchroman in healthy female subjects after oral administration
Lal, J.; Asthana, O.P.; Nityanand, S.; Gupta, R.C.
Contraception 52(5): 297-300
1995
ISSN/ISBN: 0010-7824 PMID: 8585886 DOI: 10.1016/0010-7824(95)00213-tDocument Number: 294823
The pharmacokinetics of centchroman, a non-steroidal antifertility agent, were assessed in serum of eleven healthy female subjects after a single 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 administration. The concentration-time profile was best described by a two-compartment open model with bi-exponential disposition functions. The mean terminal elimination half-life (t-1/2) was 165 (s.d., 49) h with 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 this study with those obtained after a single 60 mg oral dose did not show statistically significant differences in the rate of absorption, distribution and elimination. The C-max and AUC-o- infin were dose-dependent. Thus, the absorption and disposition of centchroman are of first-order, reproducible and dose-independent.