论文部分内容阅读
目的:研究氯雷他定(LOR)及其活性代谢物去羧乙氧基氯雷他定(DCL)在中国健康受试者体内的药动学。方法:20名健康中国男性受试者口服氯雷他定20mg,采用液相色谱-质谱-质谱联用法测定血浆中LOR和DCL的药物浓度。结果:LOR和DCL的C_(max)分别为(17±14)和(16±9)μg/L;T_(max)分别为1.2和1.5h;AUC_(0-∞)分别为(47±49)和(181±122)μg·h·L~(-1);LOR的T_(1/2)平均为(6±4)h,DCL的T_(1/2)平均为(13.4±2.6)h;AUC_(DCL)/AUC_(LOR)比值的范围从0.36到54.5。结论:中国受试者口服单剂量氯雷他定片后,在体内迅速吸收并转化为DCL,母体药物AUC的个体差异极为显著,而活性代谢物DCL的AUC则只表现出中等强度的个体差异。
Objective: To study the pharmacokinetics of loratadine (LOR) and its active metabolite decarboxyethionate loratadine (DCL) in Chinese healthy volunteers. Methods: Twenty healthy Chinese male subjects received loratadine 20 mg orally, and the concentrations of LOR and DCL in plasma were determined by liquid chromatography-mass spectrometry-mass spectrometry. RESULTS: The Cmax of LOR and DCL were (17 ± 14) and (16 ± 9) μg / L, respectively; the T max was 1.2 and 1.5 h, respectively; the AUC 0- ∞ was 47 ± 49 ) And (181 ± 122) μg · h · L -1, respectively. The average T 1/2 of LOR was (6 ± 4) h and the average of T 1/2 of DCL was (13.4 ± 2.6) h; AUC_ (DCL) / AUC_ (LOR) ratios ranged from 0.36 to 54.5. CONCLUSION: After single oral doses of loratadine tablets, Chinese subjects rapidly absorbed and transformed into DCL in vivo. The individual differences of the AUC of the parent drug were extremely significant. However, the AUC of the active metabolite DCL showed only moderately strong individual differences .