国产雷米普利胶囊在健康人体的药代动力学和相对生物利用度

Pharmacokinetics and relative bioavailability of domestic ramipril capsule in healthy volunteers

目的研究健康受试者口服雷米普利胶囊(抗高血压药)的药代动力学和相对生物利用度。方法20名健康受试者随机服用雷米普利受试和参比制剂各10mg,用HPLC-MS/MS法测定血浆中雷米普利和雷米普利拉的浓度。结果主要药代动力学参数,试验与参比制剂中雷米普利的tmax分别为(0.60±0.17),(0.63±0.25)h;Cmax分别为(40.11±14.48),(41.78±13.18)ng·mL-1;t1/2分别为(2.75±1.36),(2.28±1.28)h;AUC0-12分别为(42.09±11.22),(41.81±12.89)ng·h·mL-1;试验制剂的相对生物利用度为(101.47±16.02)%。试验与参比制剂中雷米普利拉的tmax分别为(2.70±0.47),(2.60±0.60)h;Cmax分别为(42.02±12.53),(41.80±14.65)ng·mL-1;t1/2分别为(17.99±6.28),(18.51±5.81)h;AUC0-72分别为(310.65±91.42),(310.21±102.74)ng·h·mL-1。试验制剂的相对生物利用度为(101.09±15.28)%。结论参比与试验制剂具有生物等效性。

Objective To study the pharmacokinetics and relative bioavailability of domestic ramipril capsule in healthy volunteers. Methods A single oral capsule （test） and tablet （reference） of both 10mg were given to 20 healthy volunteers at random. Plasma concentration of ramipril and ramiprilat were determined by HPLC - MS/MS. Results The main pharmacokinetic parameters of ramipril were as follow ： tmax were （0.60 ± 0.17）and（0.63 ± 0.25） h , Cmax were（40. 11 ± 14.48）and（41.78 ± 13.18 ）ng·mL^-1, t1/2 were （ 2.75 ± 1.36 ） and （ 2.28 ± 1.28 ） h, AUC0-12 were（42.09 ± 11.22） and（41.81 ± 12.89）ng·mL^-1 for test and reference respectively. The main pharmacokinetic parameters of ramiprilat were as follow ： tmax were （ 2.70 ± 0.47 ） and （ 2.60 ± 0.60 ） h , Cmax were（42.02 ± 12.53）and（41.80 ± 14.65 ）ng·mL^-1,t1/2 were （ 17.99 ± 6.28 ） and （ 18.51 ± 5.81 ） h, AUC0-72 were （ 310.65 ± 91.42 ） and （310.21 ± 102.74） ng·mL^-1 for test and reference respectively. The relative bioavailability of ramipril were （ 101.47 ± 16.02 ） %, and （101.09 ± 15.28 ）% for ramiprilat. Conclusion The praperations of test and reference were bioequivalent .