国产与进口赖诺普利片在健康人体的药代动力学和生物等效性  

Pharmacokinetics and bioequivalence of domestic and imported lisinopril tablets in healthy volunteers

作　　者：王晓波[1] 姚文[1] 袭荣刚[1] 吴学东 王文智 宋冬梅[3] 刘婷立[3] 

机构地区：[1]解放军第210医院国家药物临床试验机构,辽宁大连116021 [2]河北万岁药业有限公司,河北沧州061000 [3]沈阳亿灵医药科技有限公司,沈阳110179

出　　处：《中国临床药理学杂志》2010年第6期427-430,共4页The Chinese Journal of Clinical Pharmacology

摘　　要：目的评价国产与进口赖诺普利片(降血脂药)在健康人体的药代动力学和生物等效性。方法 20名健康男性受试者随机分组,按自身交叉、单剂量口服赖诺普利受试和参比制剂各20mg后,用高效液相色谱-串联质谱法测定血浆中赖诺普利的浓度,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。结果赖诺普利片受试制剂和参比制剂的tm ax分别为(6.00±0.46),(6.35±0.88)h;Cm ax分别为(81.47±40.92),(80.91±37.45)ng·mL-1;t1/2分别为(10.99±6.12),(10.71±3.40)h;AUC0-48分别为(784.90±379.40),(815.40±377.60)ng·h·mL-1;AUC0-∞分别为(838.50±392.00),(868.00±392.20)ng·h·mL-1,受试制剂的相对生物利用度F为(97.1±11.9)%。结论国产与进口赖诺普利片具有生物等效。Objective To evaluate the bioequivalence of domestic lisinopril tablets and imported tablets in healthy volunteers. Methods A single oral dose of 20 mg domestic and imported lisinopril tablets was given to 20 healthy volunteers in a randomized crossover study. Lisinopril concentrations in plasma were determined by HPLC - MS/MS methods. Results The main pharmacokinetic parameters of the domestic and imported tablets were as follow ： tmax were （ 6.00 ± 0. 46 ）, （ 6. 35 ±0. 88 ） h ; Cmax were （ 81.47 ± 40. 92 ）, （ 80. 91 ± 37.45 ） ng · mL^- 1 ; t1/2 were （10.99 ± 6.12）, （10.71 ± 3.40） h; AUC0-48 were （784.90 ± 379.40）, （815.40 ±377.60） ng·h·mL^-1 ;AUC0-∞ were （838.50 ±392. 00） ,（868.00 ±392.2） ng · h · mL^-1, respectively. The relative bioavailability of domestie lisinopril tablets to imported tablets was （97.1 ± 11.9） %. Conclusion The results demonstrated that the two preparations were bioequivalent.

关 键 词：赖诺普利 生物等效性 药代动力学 高效液相色谱-串联质谱 

分 类 号：R969.1[医药卫生—药理学] R972.6[医药卫生—药学]