不同厂家辛伐他汀片药动学和生物利用度的研究

Pharmacokinetic and relative bioavailability of simvastatin tablet in healthy volunteers

目的 :选择 1 0名男性健康志愿者 ,开展国产仿制辛伐他汀片的药动学和相对生物利用度的研究 ,旨在为药剂部门招标选择药品和临床更合理、经济选择药品提供临床实验依据。方法 :采用高效液相色谱法 (HPLC) ,以紫外 2 39nm为检测波长 ,测定单剂量口服国产仿制和原研制辛伐他汀片在健康人体内的血药浓度。结果 :国产和原研制的辛伐他汀片的Cmax分别为 (1 2 .0± 3.0 )mg·L-1 和 1 2 .5 8mg·L-1 ;tmax分别为 (2 .0± 0 .4 )h和 (1 .89± 0 .34)h ;t1 / 2 分别为 (2 .1 8± 0 .31 )h和 (2 .2 2± 0 .2 6 )h ;Ka 分别为 (1 .3± 1 .0 )h-1 和 (1 .0± 1 .3)h-1 ;AUC分别为 (75 .0± 1 8.2 )和 (79.1± 1 6 .8)。结论 :国产仿制辛伐他汀片的相对生物利用度为 (97.2± 8.3) %,经配对t检验 ,两种制剂各药动学参数差别无显著性 ,表明国产仿制辛伐他汀片和原研制辛伐他汀片具有生物等效性。

OBJECTIVE To study the pharmacokinetic and relative bioavailability of simvastatin tablet in healthy volunteers. METHODS A high performance liquid chromatography(HPLC) was established for the determination of simvastatin in plasma after a single oral dose of 20 mg domestic simvastatin tablet and imported simvastatin tablet in a crossed design ,the detector was operated at UV 239 nm .RESULTS The pharmacokinetic parameters after a single oral dose of 20 mg domestic simrastain tablet and imported simvastatin tablet were as follows: C max were ( 12.0 ± 3.0) mg ·L -1 and ( 12.58 ± 3.61) mg ·L -1 ; t max were ( 2.0 ± 0.4) h and ( 1.89 ± 0.34) h ; t 1/2 were ( 2.18 ± 0.31) h and ( 2.22 ± 0.26) h ; K a were ( 1.3 ± 1.0 ) h -1 and ( 1.01 ± 1.31 ) h -1 ;AUC were ( 75.0 ± 18.2 ) and ( 79.1 ± 16.8 ).CONCLUSIONS The relative bioavailability of the domestic tablet was ( 97.2 ± 8.3)% .