氯雷他定口腔崩解片人体药动学及生物等效性评价
Pharmacokinetics and bioequivalent of loratadine orally disintegrating tablets in healthy volunteers
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摘要: 目的: 评价氯雷他定口腔崩解片和氯雷他定片的人体生物等效性。方法: 20名男性健康志愿者随机交叉口服氯雷他定口腔崩解片和氯雷他定片各20mg,采用液相色谱-串联质谱法测定血药浓度。以DAS2.0软件计算其药动学参数,考察其生物等效性。结果: 受试氯雷他定口腔崩解片和参比氯雷他定片的Tmax分别为(1.14±0.43) h和(1.33±1.02) h;Cmax分别为(37.0±16.0)μg/L和(41.0±17.1)μg/L;AUC0-15h分别为(99.6±49.5)μgL-1h-1和(89.4±43.2)μgL-1h-1;AUC0-∞分别为(108.0±50.7)μgL-1h-1和(101.7±39.2)μgL-1h-1。以AUC0-15h计算,受试氯雷他定口腔崩解片和参比氯雷他定片比较的人体相对生物利用度为(115.1±32.0)%。结论: 受试制剂氯雷他定口腔崩解片和参比制剂氯雷他定片具有生物等效性。Abstract: Objective: To evaluate the bioequivalence of loratadine orally disintegrating tablets and loratadine tablets in healthy volunteers.Methods: A single oral dose of 20 mg test or reference formulations were given to 20 male healthy volunteers in a randomized crossover design.The serum concentration of loratadine was determined by liquid chromatography-tandem mass spectrometry(LC-MS/MS) method.Pharmacokinetic parameters and relative bioavailability were calculated with DAS program to evaluate the bioequivalence of the two formulations.Results: Pharmacokinetic parameters of loratadine reference formulation were obtained as follows:Tmax was(1.33±1.02) h,Cmax was(41.0±17.1) μg/L,AUC0-15hwas(89.4±43.2) μg·L-1·h-1,AUC0-∞ was(101.7±39.2) μg·L-1·h-1.For test formulation:Tmax was(1.14±0.43) h,Cmax was(37.0±16.0) μg/L,AUC0-15hwas(99.6±49.5) μg·L-1·h-1,AUC0-∞ was(108.0±50.7) μg·L-1·h-1.Calculated with AUC0-15h,the bioavailability of two formulations was(115.1±32.0)%.Conclusions: The loratadine orally disintegrating tablets and loratadine tablets were bioequivalent.