【摘要】 健康志愿者10人,随机、交叉、单剂量口服国产及进口格列齐特（gliclazide）片80mg,不同时间测得的血药浓度数据在COMPAQ计算机上用MCPKP程序进行拟合处理,符合开放性单室模型。国产和进口格列齐特的C_max,T_max,T_1/2k和AUC分别为6.48和1.65μg/ml,3.01和5.66h,10.5和12.6h,117和35.0h·μg/ml。国产格列齐特片的相对生物利用度为进口片的334%。更多还原

【Abstract】 The pharmacokinetics of gliclazide, N-（4-methylphenylsulfonyl）-N-（3-azabicyclo 3, 3, 0octyl）urea, a potential hypoglycemic drug, was in-vestigated in 10 healthy Chinese volunteers. Theblood level of gliclazide at different times after sin-gle oral administration of 80 mg of the domestic andimported tablets was determined by high perfor-mance liquid chromatography. The MCPKP-auto-matic pharmacokinetic program was used for the se-lection of optipal compartment model and calcula-tion of pharmacokinetic parameters using weightednonlinear least square regression. The resultsshowed that the plasma drug was in line with theone-compartment open model. The C_max, T_max, T_1/2kand AUC of the domestic and imported tablets were6.48±3.0 and 1.8±1.65μg/ml, 3.01±0.96and 5.66±2.2h, 10.5±2.5 and 12.6±4.7h,117±50 and 35.0±31h·μg^-1·ml^-1, respec-tively. The relative biological availability of the do-mestic gliclazide was 334% compared with that ofthe imported.更多还原