【摘要】 目的:建立高效液相色谱测定人血浆中茚地那韦药物浓度的方法,并研究了茚地那韦健康人体内的药动学。方法:采用高效液相色谱法,色谱柱为 Hypersil C₁₈柱（4.6mm×200mm,5μm）,流动相为乙腈-10mmol·L^-1磷酸盐缓冲液（pH 5.5）（43:57）;流速:1.0mL·min^-1,检测波长210nm,进样量:20μL。结果:茚地那韦在0.03～16.38μg·mL^-1范围内线性良好（r=0.9999）,回收率及日内、日间差均符合生物样品分析要求。应用本法研究10名健康受试者口服茚地那韦胶囊800mg 后的药动学,结果表明,其体内过程符合一房室开放模型,主要药动学参数如下:C_max为（10.27±2.17）μg·mL^-1;t_max为（0.79±0.27）h;t_1/2kα为（0.30±0.26）h;t_1/2ke为（1.31±0.22）h;V/F 为（74.61±14.03）L;AUC_0-t为（23.04±3.57）μg·h·mL^-1;AUC_0-∞为（23.31±3.57）μg·h·mL^-1。结论:此方法便捷、准确、灵敏,适于茚地那韦血药浓度测定和药动学研究,本试验所得药动学参数可为临床合理用药提供理论依据。更多还原

【Abstract】 Objective:To develop an HPLC method for the concentration determination in human plasma and inves- tigation the pharmacokinetics of indinavir.Methods:The chromatographic column was Hypersil C₁₈column（4.6mm× 200mm,5μm）.The mobile phase,acetonitrile-pH 5.5 phosphate buffer（43:57 ）was used at a flow rate of 1.0 mL· min^-1.The wavelength was 210 nm.The injection volume was 20 μL.Results:The linear correlation of indinavir was observed in the range of 0.03-16.38 μg·mL^-1（r=0.9999）.Precision and accuracy of the method were fine.The pharmacokinetic analysis of indinavir was studied in healthy volunteers after oral administration of 800 mg indinavir capsules.Finding revealed that the data of indinavir were fitted to an open one-compartment model.The main pharmacokinetic parameters of indinavir were as follow:C_max,was（10.27±2.17）μg·mL^-1;t_max, was（0.79±0.27）h;t_1/2kαwas（0.30 +0.26）h;t_1/2kewas（ 1.31±0.22）h; V/F was（74.61±14.03）L;AUC_O-t was（23.04±3.57 ）μg·h· mL^-1; AUC_O-∞was（23.31±3.57 ）μg·h·mL^-1.Conclusion:The method is con- venient,sensitive,accurate and reproducible,and can be applied to determine the drug plasma indinavir concentra- tion and study on pharmacokinetics.更多还原