Georgarakis Manolis, Tsakalof Andreas, Zougrou Fotini, Kontopoulos Georgios, Tsiptsios Iakovos
Laboratory of Pharmaceutics and Drug Control, Department of Pharmacy, Aristotle University of Thessaloniki, Thessaloniki, Greece.
Arzneimittelforschung. 2004;54(1):15-9. doi: 10.1055/s-0031-1296931.
An open, two-period, randomized, crossover trial of two lisinopril (1-[N2-[(S)-1-carboxyl-3-phenylpropyl]-L-lysil]-L-proline, CAS 76547-98-3) formulations (Adicanil as test and another commercially available preparation as reference) was performed in 24 healthy volunteers. A single 20 mg oral dose of lisinopril was administrated and pharmacokinetic parameters were compared. Lisinopril plasma concentrations were measured by a fully validated LC-MS method. The parametric 90% confidence intervals of the geometric mean values of the test/reference ratios were 95.38% to 105.94% (point estimate: 100.52%) for AUC(0-last), 94.01% to 103.47% (point estimate: 98.63%) for AUC(0-infinity) and 92.34% to 103.97% (point estimate: 97.98%) for Cmax, being within the acceptance criteria for bioequivalence (80%-125%). T(1/2), k(el) and Tmax values were also tested and the difference was not statistically significant. Therefore, it is concluded that the test and the reference lisinopril formulations are bioequivalent both in the extent and the rate of absorption.
对24名健康志愿者进行了一项开放、两阶段、随机、交叉试验，比较两种赖诺普利（1-[N2-[(S)-1-羧基-3-苯基丙基]-L-赖氨酸]-L-脯氨酸，CAS 76547-98-3）制剂（Adicanil作为试验制剂，另一种市售制剂作为参比制剂）。给予单次20mg口服剂量的赖诺普利，并比较药代动力学参数。赖诺普利血浆浓度通过完全验证的LC-MS方法测定。试验/参比制剂比值几何均值的参数90%置信区间，AUC(0-last)为95.38%至105.94%（点估计值：100.52%），AUC(0-无穷大)为94.01%至103.47%（点估计值：98.63%），Cmax为92.34%至103.97%（点估计值：97.98%），均在生物等效性接受标准（80%-125%）范围内。还对T(1/2)、k(el)和Tmax值进行了测试，差异无统计学意义。因此，得出结论：试验制剂和参比赖诺普利制剂在吸收程度和吸收速率方面均具有生物等效性。
