枸橼酸他莫昔芬片剂的药代动力学和相对生物利用度研究  

Pharmacokinetics and Relative Bioavailability of Tamoxifen in Healthy Volunteers

作　　者：谢林[1] 刘晓东[1] 龚小健[1] 刘国卿[1] 

机构地区：[1]中国药科大学药理学教研室

出　　处：《中国药科大学学报》1995年第2期84-86,共3页Journal of China Pharmaceutical University

摘　　要：采用高效液相色谱法进行枸橼酸他莫昔芬片的药代动力学和生物利用度研究。８名健康受试者分别随机ｐｏ屯溪产和上海产枸橼酸他莫昔芬片３０ｍｇ，其血药浓度－时间曲线均符合－房室模型。屯溪产枸橼酸他莫昔芬片的主要药代动力学参数Ｔ１／２ｋα＝０．７８±０．２３ｈ，Ｔ１／２ｋｅ＝１２．０９±２．４５ｈ，Ｔ（ｍａｘ）＝３．７３±０．８１ｈ，Ｃ（ｍａｘ）＝１１８．８±２９．０ｎｇ／ｍｌ，ＡＵＣ＝２３８４±４４５ｎｇ·ｈ·ｍｌ－１。其相对生物利用度为１０４．２％。The pharmacokinetics of tamoxifen from Tunxi(T1)and Shanghai(T2)were separately studied in healthy male volunteers after single oral administration at the dosage of 30 mg(3 tablets).Tamoxifen concentration in plasma was determined by HPLC.The concentration-time course of tamoxifen was fitted to one-compartment model.The pharmacokinetic parameters were estimated as follows:T1,T1/2ka=0.78±0.23h,T1/2ke=12.09±2.45h,Tmax=3.73±0.81h,Cmax=118.8±29.0ng/ml,and AUC=2384±445 ng·h·ml-1;T1/2ka=0.71±0.22h,T1/2ke=12. 69±3.16h,Tmax=3.57±0. 90h,Cmax=109.3±19.3 ng/ml,and AUC=2284±416 ng·h·ml-1.Relative bioavailability of T1 was 104.2%,compared with T2.

关 键 词：枸橼酸他莫昔芬 药代动力学 生物利用度 HPLC 

分 类 号：R979.1[医药卫生—药品]