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目的:研究单剂量和多剂量盐酸曲普利啶胶囊在中国健康志愿者体内的药物动力学特征。方法:健康受试者单次(2.5 mg)或多次(2.5 mg,tid,连续服药6d)口服盐酸曲普利啶胶囊,用LC-MS法测定血浆中曲普利啶浓度,用DAS 2.0处理数据。结果:本法线性良好,精密度、准确度、回收率均符合要求。所得药物动力学参数如下,单剂量:t_(1/2)=(5.88±1.62)h,t_(max)=(2.21±0.62)h,C_(max)=(27.50±6.32)ng·ml~(-1),AUC_(0-∞)=(216.74±67.18)h·ng·ml~(-1),MRT_(0-∞)=8.64±1.24 h。多剂量:t_(1/2)=(6.38±2.58)h,t_(max)=(1.71±0.58)h,AUC_(8S)=139.29±47.22 h·ng·ml~(-1),C_(max)=(27.78±6.52)ng·ml~(-1),C_(min)= (10.12±9.26)ng·ml~(-1),C_(av)=(17.41±5.90)ng·ml~(-1),DF=1.13±0.60。结论:该法灵敏度高,操作简便,盐酸曲普利啶胶囊多剂量给药与单剂量给药的药物动力学参数基本一致,无蓄积,给药后安全性良好。
Objective: To study the pharmacokinetics of single and multiple doses of triprolidine hydrochloride in Chinese healthy volunteers. Methods: Healthy subjects were given oral dipyridamole hydrochloride capsules in single or double doses (2.5 mg, tid for 6 days), and plasma concentrations of triprolidine were determined by LC-MS. DAS 2.0 Data processing. Results: The method is good linearity, precision, accuracy, recovery rate are in line with the requirements. The pharmacokinetic parameters were as follows: single dose: t_ (1/2) = (5.88 ± 1.62) h, t max = 2.21 ± 0.62 h, C_max = 27.50 ± 6.32 ng · ml ~ (-1), AUC_ (0-∞) = (216.74 ± 67.18) h · ng · ml -1 and MRT_ (0-∞) = 8.64 ± 1.24 h. The results of multiple dose: t 1/2 (6.38 ± 2.58) h, t max = 1.71 ± 0.58 h, AUC 8S = 139.29 ± 47.22 h · ng · ml -1, C_ max = 27.78 ± 6.52 ng · ml -1, C min = 10.12 ± 9.26 ng · ml -1, C av = 17.41 ± 5.90 ng · ml ~ (-1), DF = 1.13 ± 0.60. Conclusion: The method is sensitive and easy to operate. The pharmacokinetic parameters of multidose and single-dose administration of the compound dipyridamole hydrochloride capsule are basically the same, without accumulation, and have good safety after administration.