雷米普利胶囊人体生物等效性研究

 目的评价国产雷米普利胶囊与已上市的雷米普利片的人体生物等效性。方法18名男性健康志愿者随机交叉po雷米普利受试制剂和参比制剂各10 mg,采用液相色谱-质谱法同时测定雷米普利及其活性代谢物雷米普利拉的药物浓度。结果参比制剂及受试制剂的雷米普利的t_max分别为(0.53±0.14)和(0.58±0.17)h,ρmax分别为(42.34±13.37)和(43.84±13.65)μg·L^-1,AUC_0-72分别为(41.70±13.62)和(42.57±11.54)μg·h·L^-1,t_1/2(ke)分别为(2.55±1.55)和(2.40±0.85)h,雷米普利拉的t_max分别为(2.44±0.62)和(2.50±0.51)h,ρ_max分别为(43.28±13.83)和(39.75±13.73)μg·L^-1,AUC_0-72分别为(311.34±99.34)和(312.34±97.74)μg·h·L^-1,t_1/2(ke)分别为(18.80±6.82)和(17.99±5.94)h,国产雷米普利胶囊相对生物利用度以雷米普利计为(104.44±13.07)%,以雷米普利拉计为(101.62±14.56)%。结论方差分析和双单侧t检验结果表明,两种制剂生物等效。

Studies on Bioequivalence of Ramipril Capsule in Healthy Volunteers

OBJECTIVE To evaluate the bioequivalence of domestic ramipril capsule and imported ramipril tablet in the healthy volunteers.METHODS A single oral dose of 10 mg test or reference preparations of ramipril was given to 18 healthy volunteers in a randomized crossover study.The serum concentrations of ramipril and its active metabolite ramiprilat were determined by HPLC-MS assay.RESULTS The main pharmacokinetic parameters of the two products of ramipril were as follows t_max(0.53±0.14)and(0.58±0.17)h;ρ_max(42.34±13.37)and(43.84±13.65)μg·L^-1;AUC_0-72(41.70±13.62)and(42.57±11.54)μg·h·L^-1;t_1/2(ke)(2.55±1.55) and(2.40±0.85)h,respectively.The main pharmacokinetic parameters of the two products of ramiprilat were as follows t_max(2.44±0.62)and(2.50±0.51)h;ρ_max(43.28±13.83)and(39.75±13.73)μg·L^-1;AUC_0-72(311.34±99.34)and(312.34±97.74)μg·h·L^-1;t_1/2(ke)(18.80±6.82) and(17.99±5.94)h,respectively.The relative bioavailability of the test to reference capsule of ramipril and ramiprilat were(104.44±13.07)% and(101.62±14.56)%,respectively.CONCLUSION The results of variance analysis and two one-side t test show that the two formulations are bioequivalent.