奈韦拉平片血药浓度测定及健康人体药动学

Pharmacokinetics of domestic and imported nevirapine tablets in healthy volunteers

目的：建立高效液相色谱法测定人血浆中奈韦拉平浓度，并研究了奈韦拉平片的健康人体药动学。方法：采用高效液相色谱法测定奈韦拉平血浆药物浓度，并应用苓法研究10名健康受试者单剂量口服奈韦拉平片200mg后的药动学。结果：奈韦拉平在62．5～4000μg·L^-1范围线性良好（r=0．9999），回收率，日间、日内差等均符合生物样品分析要求。药动学研究结果表明，奈韦拉平片体内过程符合一房室开放模型，主要药动学参数：Cmax为（2357±387）μg·L^-1；tmax为（3．7±1．1）h；t1/2ka为（0．7±0．9）h；t1/ke为（54．1±15．4）h；CL／F为（1．2±0．3）L·h^-1；V／F为（93．4±18．1）L；AUC0-t为（154．5±34．5）mg·h·L^-1，AUC0-∞为（173．7±44．1）mg·h·L^-1。结论：本方法便捷，灵敏，准确，适用于奈韦拉平血药浓度测定和药动学研究，本研究药动学结果可为临床用药提供依据。

OBJECTIVE To develop an HPLC method for the determining the concentration of nevirapine in plasma and investigate the pharmacokinetics in healthy volunteers. RESULTS A single oral dose 200 mg of nevirapine tablets was given to 10 healthy volunteers, and the concentrations of nevirapine in plasma were determined by established HPLC method. METHODS The linear correlation of nevirapine was observed for the concentration of 62.5 - 4 000μg. L^-1 （r = 0. 999 9）. Precision and stability of the method were fine. The results revealed that the data of nevirapine were fitted to a one-compartment open model. The main pharmacokinetic parameters of neviraplne were as follows： Comax was（2 357 ± 387）μg·L^-1 ;tmax was（3. 7±1. 0） h;t1/2ka was （0. 7 ± 0. 9） h; t1/ 2ka was （54. 1 ± 15. 4） h; CL/F was （1.2 ± 0.3） L·h ;V/F was （93.4 ± 18. 1 ） L; AUC0-1 was （154.5±34.5） mg·h·L^-1;AUC0-∞ was （173.7±44.1） mg·h·L^-1. CONCLUSION Themethod is convenient, sensitive and accurate for determining the plasma nevirapine concentration and studying pharmacokinetics.