摘要
目的研究贝那普利的药动学特征,评价两种贝那普利制剂生物等效性。方法24名健康男性受试者随机交叉、先后单剂量口服贝那普利被试制剂和参比制剂20mg,采用液相色谱-串联质谱法(LC/MS/MS)测定血浆中贝那普利及其活性代谢物贝那普利拉浓度。结果被试制剂和参比制剂中贝那普利原型的Cm ax,tm ax,t1/2,AUC0-∞分别为(193.8±84.0)ng/mL和(226.3±110.3)ng/mL,(0.70±0.35)h和(0.47±0.20)h,(1.22±0.20)h和(1.30±0.16)h,(182.1±61.4)ng.h/mL和(180.3±73.6)ng.h/mL,贝那普利拉的Cm ax,tm ax,t1/2,AUC0-∞分别为(275.9±129.3)ng/mL和(266.6±105.9)ng/mL,(1.44±0.42)h和(1.31±0.36)h,(5.29±0.65)h和(5.41±0.80)h,(1187.6±481.9)ng.h/mL和(1155.3±481.8)ng.h/mL,根据贝那普利和贝那普里拉分别计算的相对生物利用度为(104±14)%和(103±9)%。结论贝那普利两种制剂具有生物等效性。
OBJECTIVE To study the pharmacokinetic profiles of benazepril and evaluate the bioequivalence of two benazepril tablet preparations. METHODS An open randomized, two-period crossover study was performed on 24 healthy volunteers with a single dosage of 20mg benazepfil. A sensitive LC/MS/MS method was established to determine the plasma concentrations of benazepril and its active metabolite benazeprilat. RESULTS To benazepfil, the main pharmacokinetic parameters of test and reference preparations were as follows： Cmax（193.8± 84.0） ng/mL and （226.3 ± 110.3） ng/mL, tmax（0.70 ±0.35）h and （0.47 ±0.20）h, t1/2（1.22 ± 0.20） h and （ 1.30 ± 0. 16） h, AUC0-∞ （ 182.1± 61.4） ng· h/mL and （ 180.3 ± 73.6） ng · h/mL. To benazepfilat, the pharma- cokinetic parameters were as follows ： Cmax （275.9 ± 129.3） ng/mL and （ 266.6 ± 105.9） ng/mL, tmax（ 1.44 ± 0.42） h and （ 1.31 ± 0.36）h, t1/2（5.29 ±0.65）h and （5.41±0.80）h, AUC0-∞ （1187.6 ±481.9）ng · h/mL and （1155.3 ±481.8）ng · h/mL. The relative bioavailability of test preparation were （ 104 ± 14）% for benazepfil and （ 103 ±9）% for benazepfilat. CONCLUSION The two preparations were bioequivalem.
出处
《中国现代应用药学》
CAS
CSCD
北大核心
2007年第1期36-39,共4页
Chinese Journal of Modern Applied Pharmacy
基金
863国家攻关项目<临床试验关键技术及平台研究>(2002AA2Z341A
2004AA2Z3760)
