【摘要】 目的:研究孟鲁司特钠在健康人体内的药动学及国产制剂的人体生物等效性。方法:采用三制剂三周期二重3×3拉丁方实验设计,24例健康男性受试者交叉口服试验制剂和参比制剂10 mg,24h时间周期内间隔采集静脉血,处理后血浆样本用HPLC测定。计算片剂和咀嚼片剂的药动学参数,并以进口片剂作对比,估算国产制剂人体相对生物利用度,评价生物等效性。结果:国产孟鲁司特钠片剂/咀嚼片制在中国健康男性受试者体内的药动学特征基本符合线性动力学一室开放模型,其AUC_0～24h分别为（3051．11±671．30）和（3038．37±585．03）μg·h·L^-1;C_max分别由（341．01±75．11）和（342．36±75．93）μg·L^-1;T_max分别为（3．52±0．31）和（3．42±0．46）h。计算得孟鲁司特钠片剂/咀嚼片剂的平均人体相对生物利用度分别为（99．95±8．22）%和（100．05±9．32）%。结论:孟鲁司特钠国产制剂与进口片剂具生物等效性。更多还原

【Abstract】 Objective:To study the pharmacnkinetic profiles and the bioequivalence of domestic montelukast film-coated/chewable tablets（test）versus imported montelukast tablets（reference）.Meth- ods:24 male healthy volunteers were orally administered with a single crossover dose of montelukast 10mg in a 3×3 Latina square design of three preparations,three cycles and double dummy clinical trial. The blond samples from the volunteers were collected in 24h after each single dose of test or reference samples to measure the plasma concentration of montelukast by HPLC.Results:Montelukast pharmaco- kinetic profiles in Chinese male healthy population featured a linear and open one-compartment model. The PK parameters of montelukast film-coated tablets and chewable tablets were AUC_0-24h（3051.11±671.30）and（3038.37 +585.03）μg·L^-1·h;C_max（341.01±75.11）and（342.36±75.93）μg·L^-1; T_max（3.52±0.31）and（3.42±0.46）h,respectively.The relative bioavailability of montelukast film- coated tablets and chewable tablets were（99.95±8.22）% and（100.05±9.32）%,respectively: Conclusion:The domestic montelukast were binequivalent to imported montelukast tablets.更多还原