【摘要】 目的建立LC-MS/MS法测定氨溴索血药浓度,研究口服氨溴特罗颗粒剂与氨溴特罗口服液中氨溴索在人体内的生物等效性。方法采用双周期随机交叉试验设计,研究了18名健康男性受试者单剂量口服氨溴特罗颗粒(受试制剂)与氨溴特罗口服液(参比制剂)的药动学。采用LC-MS/MS法测定血浆中氨溴索的浓度。评价两制剂中氨溴索在人体内的生物等效性。结果单次给予受试制剂或参比制剂(含盐酸氨溴索60 mg)后氨溴索的主要药物动力学参数分别为:Cmax为(183.86±108.22)、(216.68±198.50)μg.L-1;tmax为(2.1±0.8)、(2.2±1.0)h;AUC0-96为(2 274.13±1 159.02)、(2 016.97±928.48)μg.h.L-1;AUC0-∞为(2 307.42±1 203.33)、(2 056.64±961.25)μg.h.L-1;t1/2为(14.4±4.6)、(17.2±6.9)h。与参比制剂相比,受试制剂的相对生物利用度为(111.3±18.0)%。结论受试制剂与参比制剂中氨溴索的主要药动学参数之间无明显差异,非参数检验未发现两制剂的tmax有显著性差异。双单侧t检验结果表明两制剂为生物等效制剂。更多还原

【Abstract】 Objective To develop an LC-MS/MS method for the determination of ambroxol in the plasma and evaluate the bioequivalence of ambrocol granules and ambrocol oral solution.Methods A single oral dose of ambrocol granule(test preparation,T) and ambrocol oral solution(reference preparation,R) was administered to 18 healthy volunteers in a randomized crossover study,and the pharmacokinetics and bioavailability were studied.Results The main pharmacokinetic parameters of ambrocol(T and R) were as follows:Cmax was(183.86±108.22) and(216.68±198.50)μg·L-1;tmax was(2.1±0.8) and(2.2±1.0)h;AUC0~96 was(2 274.13±1 159.02) and(2 016.97±928.48)μg·h·L-1;AUC0~∞ was(2 307.42±1 203.33) and(2 056.64±961.25)μg·h·L-1;t1/2 was(14.4±4.6) and(17.2±6.9)h.The relative bioavailability of ambrocol of preparation T was(111.3±18.0)% when compared with tablet R.Conclusion Statistic analysis shows no significant difference between the two preparations,and bioequivalence is observed.更多还原