Pharmacokinetics of centchroman in healthy female subjects after oral administration.
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 (Cmax) of 55.53 (s.d., 15.45) microgram/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 (t1/2) 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 Cmax and AUC0-infinity were dose-dependent. Thus, the absorption and disposition of centchroman are of first-order, reproducible and dose-dependent.
Lal
J
J
Pharmacokinetics & Metabolism Division, Central Drug Research Institute, Lucknow, India.
Asthana
O P
OP
Nityanand
S
S
Gupta
R C
RC
D000284:Administration, Oral; D000328:Adult; D002486:Centchroman / Q000008:administration & dosage / Q000097:blood / Q000493:pharmacokinetics*; D003283:Contraceptives, Postcoital, Synthetic / Q000008:administration & dosage / Q000097:blood / Q000493:pharmacokinetics*; D004305:Dose-Response Relationship, Drug; D005260:Female; D006207:Half-Life; D006801:Humans; D013997:Time Factors
D003283:Contraceptives, Postcoital, Synthetic; D002486:Centchroman