Anttila M, Valavaara R, Kivinen S, Mäenpää J
Farmos Group Ltd., Research Center, Turku, Finland.
J Steroid Biochem. 1990 Jun 22;36(3):249-52. doi: 10.1016/0022-4731(90)90019-o.
The pharmacokinetics of toremifene has been investigated in man after single and multiple oral doses. Toremifene was completely absorbed without first-pass metabolism. Peak concentration in serum was achieved in 4 h. Mean half-lives of distribution and elimination were 4 h and 5 days, respectively. Kinetics was linear in the studied dose-range of 10-680 mg. Toremifene was over 99% bound to plasma proteins and extensively metabolized. The main metabolites in serum were demethyl- and deaminohydroxytoremifene. In patients receiving multiple dosing of 60 mg/day serum steady-state level of toremifene was 0.8 microgram/ml on average. The level of demethyl metabolite was twice and that of deaminohydroxy metabolite was one tenth of toremifene.
已对托瑞米芬在人体单剂量和多剂量口服后的药代动力学进行了研究。托瑞米芬可被完全吸收，且无首过代谢。血清中的峰值浓度在4小时时达到。分布半衰期和消除半衰期的平均值分别为4小时和5天。在所研究的10 - 680毫克剂量范围内，药代动力学呈线性。托瑞米芬与血浆蛋白的结合率超过99%，且代谢广泛。血清中的主要代谢产物为去甲基托瑞米芬和脱氨基羟基托瑞米芬。在接受每日60毫克多剂量给药的患者中，托瑞米芬的血清稳态水平平均为0.8微克/毫升。去甲基代谢产物的水平是托瑞米芬的两倍，脱氨基羟基代谢产物的水平是托瑞米芬的十分之一。
