奈韦拉平片在健康人体的药代动力学和生物等效性  

Pharmacokinetics and bioequivalence of navirapine tablets in healthy volunteers

作　　者：赵立子[1] 钟国平[1] 谢文俊[1] 曾桂雄[1] 黄丽惠[1] 汤琤[1] 毕惠嫦[1] 马中富[2] 黄民[1] 

机构地区：[1]中山大学临床药理研究所,广州510080 [2]中山大学附属第一医院,广州510080

出　　处：《中国临床药理学杂志》2009年第1期30-33,共4页The Chinese Journal of Clinical Pharmacology

摘　　要：目的研究2种国产奈韦拉平片(抗病毒药)在健康人体内的药代动力学,并评价这2种制剂的生物等效性。方法20例健康成年男性受试者随机分组,按自身对照单次口服奈韦拉平片200 mg后,采用HPLC法测定奈韦拉平的血浆浓度,非房室模型法计算各主要药代动力学参数,并进行方差分析和生物等效性评价。结果参比制剂与受试制剂奈韦拉平的tmax分别为(3.5±2.1)、(3.0±1.9)h;Cmax分别为(2.6.±0.5)、(2.6±0.5)mg·L-1;t1/2分别为(57.6±10.4)、(58.6±10.2)h;MRT分别为(55.6±6.5)、(56.8±5.0)h;AUC0-t分别为(167.6±36.1)、(171.8±32.7)mg·L-1.h;AUC0→∞分别为(169.9±36.6)、(174.2±33.1)mg·L-1.h;CL/F分别为(1.2±0.3)、(1.2±0.2)L.h-1;Vd/F分别为(100.3±20.4)、(99.4±20.8)L;受试制剂相对于参比制剂的生物利用度为(103.7±11.6)%。结论受试制剂与参比制剂具有生物等效性。Objective To study the pharmacokinetics and bioequivalence of two demostic nevirapine tablets in haeahhy volunteers. Methods Twenty healthy volunteers were randomized into two groups, whose plasma concentrations of nevirapine were determined at different time after single oral dose of 200 mg nevirapine tablets by own control by HPLC method, the pharmacokinetic parameters were computed and which were experienced variance analysis. Results The main pharmacokinetic parameters of reference and test navirapine tablets were as follows ： tmax were （3.5 ± 2.1）,（3.0 ± 1.9） h;Cmax were （2.6 ± 0.5 ）, （2.6 ± 0.5） mg· L^-1;t1/2 were （57.6 ± 10.4）, （58.6 ± 10.2） h;MRT were （55.6 ± 6.5 ）,（56.8 ±5.0 ）h;AUCo -t,were （167.6 ± 36.1） , （171.8 ± 32.7） mg·L^-1 · h;AUC0-∞（169.9 ± 36.6 ）, （174.2 ±33.1 ）mg·L^-1 · h;CL/F （1.2 ±0.3）,（1.2±0.2 ）L· h^-1; Vd/F were （ 100.3 ± 20.4 ）, （99.4 ± 20.8） L, respectively. The relative bioavailability of the test preparation was （ 103.7 ± 11. 6 ） %. Conclusion The results shows that the test and reference preparations of nevirapine were bioequivalent.

关 键 词：奈韦拉平 高效液相色谱法 药代动力学 生物等效性 

分 类 号：R969.1[医药卫生—药理学] R978.7[医药卫生—药学]