盐酸头孢他美酯的药代动力学研究

Pharmacokinetics of Cefetamet Pivoxil Hydrochloride Tablets in Healthy Volunteers

观盐酸头孢他美酯的药代动力学特征。１２名健康志愿受试者单次口服５００ ｍｇ盐酸头孢他美酯片剂。方法：采用高效液相色谱法测定给药后不同时间的血浆中头孢他美浓度，用３Ｎ７程序拟合房室模型和计算药代动力学参数。结果：盐酸头孢他美酯口服后血浆中活性成分为头孢他美，血药浓度－时间曲线为二室模型，主要药代动力学参数Ｔｍａｘ为２．３± ０．５ｈ， Ｃｍａｘ为４．４３±１．３３ ｍｇ·Ｌ－１， Ｔ１／２β为２．３１± ０．４２ｈ， Ｖｄ／Ｆ为 ０．８６ ± ０．３３Ｌ· ｋｇ－１， ＣＬ／Ｆ为 １６．７５ ± ４．４３ Ｌ· ｈ－１， Ａ ＵＣ为 ２４．５６６±５．８２５ ｍｇ ·ｈ·Ｌ－１。结论：提示前体药物头孢他美酯的体内过程我国汉族人与西方人基本相似。

OBJECTIVE: The pharmacokinetic profiles of cefetamet pivoxil was studied in 12 healthy male volunteers. METHOD: Each volunteer received a single dose 500 mg cefetamet pivoxil hydrochloride in suppository. The concentration of cefetamet in plasma were determined by HPLC-UV method. RESULTS: The concentration-time curves of cefetamet was fitted to a two-compartment model. The pharmacokinetics parameters of cefetamet were : Tmax was 2.3 ±0.5 h, Cmax was 4.43 ±1 .33 mg·L-1AUC was 24.566 ± 5.825 mg·h·L-1, T1/2β was 2.31 ± 0.42 h, Vd/F and CL/F were 0.86 ± 0.33 L·kg-1 and 16.75 ± 4.43 L·h-1, respectively. CONCLUSION: The disposition for cefetamet pivoxil are similar between Caucasian and Chinese.