国产与进口马来酸咪达唑仑片的生物等效性

Bioequivalence of midazolam maleate tablets in healthy volunteers

目的 :比较国产和进口马来酸咪达唑仑片在 2 0名男性健康受试者中的药物动力学和相对生物利用度。方法 :采用反相高效液相色谱测定血浆中马来酸咪达唑仑的浓度 ,并用 3P97程序拟合。结果 :单剂量 po国产和进口马来酸咪达唑仑片 15mg的 AUC0～ t分别为 (5 87.86± 16 1.6 5 )、(5 79.99± 15 1.2 5 ) h· mg/L ;cmax是 (2 2 0 .5 7± 6 7.6 4)、(199.18± 6 0 .5 3) m g/L ;tma为 (1.5 8± 0 .5 9)、(1.30± 0 .44 ) h;T1 / 2 为 (2 .94± 1.40 )、(3.2 6± 1.37) h,国产和进口片剂的所有药物动力学参数经统计学处理均无显著性差异 (P>0 .0 5 )。结论 :国产马来酸咪达唑仑片的相对生物利用度为 (10 2 .2 5± 18.2 8) % ,双单侧检验法证明 ,与进口片具有生物等效性。

AIM: To compare pharmacokinetics and bioavailability of 2 midazolam tablets in 20 healthy volunteers after a single oral dose (15 mg) of domestic midazolam maleate tablets compared with imported. METHODS: The plasma concentrations of midazolam maleate were determined by reversed phase high performance liquid chromatography and estimated by 3P97 program. RESULTS: The pharmacokinetic parameters of domestic and imported tablets were as follows: AUC 0～t (587 86±161 65), (579 99±151 25) h·mg/L; c max (220 57±67 64), (199 18±60 53) mg/L; t max (1 58±0 59), (1 30±0 44) h; T 1/2 (2 94±1 40), (3 26±1 37) h, respectively. There was no statistically difference between domestic and imported tablets in pharmacokinetic parameters. CONCLUSION: The relative bioavailability of the domestic tablets is (102 25±18 28)%. There is no significant difference between 2 tablets ( P >0 05). The 2 tablets are bioequivalent.