伊曲康唑胶囊的人体药代动力学研究

Pharmacokinetic study of itraconazole after multiple oral dosing in 9 healthy volunteers

目的：研究伊曲康唑胶囊的人体药代动力学。方法：采用反相高效液相色谱法测定９名男性健康志愿者多剂量ｐｏ伊曲康唑胶囊２００ｍｇ（１００ｍｇ×２粒）后的血药浓度，以３Ｐ８７实用药代动力学程序计算稳态后一次给药的药代动力学参数。结果：消除相ｔ１／２平均为４１．８８ｈ；ｔｍａｘ平均为４．３８ｈ；ｃｍａｘ平均为１２３０．８５ｎｇ·ｍｌ－１；ＡＵＣ平均为５１８５６．４９ｎｇ·ｈ·ｍｌ－１。结论：本实验测得的ｔ１／２值和ｃｍａｘ均明显高于文献值，为今后合理用药打下了基础。

BJECTIVE :The pharmacokinetics of itraconazole was investigated in 9 healthy Chinese volunteers. METHODS: The dosing regimen was 200 mg,b.i.d for 7 days,and on day 8 the last dose of 200 mg.The blood samples were collected before,during and after dosing.The serum levels of itraconazole were determined by high performance liquid chromatography.The 3P87 software was used for the calculation of pharmacokinetic parameters.RESULTS: The awerage maxium concentration of drug in serum was 1230.85 ngml-1,the mean time for drug to reach peak level in serum was 4.38h,the mean elimination halflife was 41.88h,the mean area under cuvre (AUC) was 51856.49 nghml-1. CONCLUSION: The valuas of t1/2 and cmax obtained here were higher than that reported before.It offered necessacy information for rational use of itraconazole in Chinese.