知识与财富的链接
目的研究马来酸依那普利片在健康人体内的药动学及相对生物利用度。方法用双周期交叉实验设计,采用液相色谱-质谱-质谱联用法测定18名健康男性受试者口服马来酸依那普利片(受试制剂)和悦宁定(参比制剂)后不同时刻血浆中依那普利和其活性代谢物依那普利拉的浓度,绘制血药浓度-时间曲线并计算主要药动学参数。结果18名受试者口服含马来酸依那普利20 mg的受试制剂和参比制剂后血浆中依那普利的tm ax分别为(0.83±0.44)和(0.93±0.37)h,ρm ax分别为(70.54±26.84)和(67.01±23.75)μg.L-1,t1/2分别为(2.13±0.52)和(2.14±0.42)h,AUC0t-分别为(122.82±45.31)和(121.45±43.06)μg.h.L-1,AUC0-∞分别为(123.77±45.36)和(122.55±43.32)μg.h.L-1;依那普利拉的tm ax分别为(3.72±1.18)和(3.61±0.92)h,ρm ax分别为(33.14±9.72)和(34.15±10.98)μg.L-1,t1/2分别为(8.88±1.35)和(8.99±1.09)h,AUC0-t分别为(301.64±82.71)和(316.47±99.09)μg.h.L-1,AUC0-∞分别为(307.32±83.54)和(322.70±100.67)μg.h.L-1,以AUC0-t计算,马来酸依那普利的平均相对生物利用度为(103.0±20.1)%,依那普利拉的平均相对生物利用度为(98.4±22.4)%。结论根据双单侧检验表明2种制剂具有生物等效性。
0bjective To study pharmacokinetics and relative bioavailability of enalapril maleate tablet in healthy volunteers. Method A LC/MS/MS method was developed to determine the plasma concentrations of enalapril and its major active metabolite enalaprilat in 18 healthy Chinese male volunteers following a 20 mg dose of enalapril tablets (test formulation) and Renitec (reference formulation) with two cross-over design, the blood concentration-time curves were plotted and the main pharmacokinetic parameters were calculated. Result The main pharmacokinetic parameters of enalapril were: tmax(0.83 ± 0.44) and (0.93 ± 0.37) h, ρmax(70.54 ± 26.84) and (67.01 ± 23.75) mg·L-1, t1/2(2.13 ± 0.52) and (2.14 ± 0.42) h, AUC0-t(122.82 ± 45.31) and (121.45 ± 43.06) mg·h·L-1, AUC0-¥(123.77 ± 45.36) and (122.55 ± 43.32) mg·h·L-1 respectively. The main pharmacokinetic parameters of enalaprilat were: tmax(3.72 ± 1.18) and (3.61 ± 0.92) h, ρmax(33.14 ± 9.72) and (34.15 ± 10.98) mg·L-1, t1/2(8.88 ± 1.35) and (8.99 ± 1.09) h, AUC0-t(301.64 ± 82.71) and (316.47 ± 99.09) mg·h·L-1, AUC0-¥(307.32 ± 83.54) and (322.70 ± 100.67) mg·h·L-1 respectively. According to AUC0-t , the relative bioavailability of enalapril maleate and enalaprilat were (103.0 ± 20.1) and (98.4 ± 22.4) %, respectively. Conclusion According to the two one –sided t-tests, the two formulations are bioequivalent．
