盐酸曲普利啶胶囊在中国健康志愿者体内的药物动力学  

Pharmacokinetics of Triprolidine Hydrochloride Capsules in Healthy Chinese Volunteers

作　　者：李飞娥[1] 刘东[1] 刘异[1] 刘宇[1] 周红华[2] 

机构地区：[1]华中科技大学同济医学院附属同济医院药学部,武汉430030 [2]中国药科大学分析测试中心

出　　处：《中国药师》2007年第5期426-429,共4页China Pharmacist

摘　　要：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 triprolidine after the single and multiple oral administration in healthy Chinese volunteers. Method： In the single dose design, the volunteers were received a single dose of 2.5mg triprolidine. In the multiple dose design, each volunteer were received 2.5 mg triprolidine three times a day for six consecutive days. The plasma samples were assayed by LC-MS and the pharmacokinetic parameters of triprolidine were calculated with DAS 2.0. Result： The pharmacokinetic parameters of triprolidine after single dose were obtained as follows： t1/2 was （5.88± 1.62）h, tmax was （2.21 ± 0.62）h, Cmax was （27.50 ± 6.32） ng· ml^ - 1, MRT（0-∞） was （8.64 ± 1.24 ） h. AUC（0-∞） was （ 216.74 ± 67.18 ） h· ng· ml^ - 1. The multi-dose pharmacokinetic parameters of triprolidine were obtained as follows： DF was （1.13 ±0.60） ,t1/2 was （6.38 ±2.58）h, tmax was （1.71 ±0.58）h, Cmax was （27.78 ±6.52） ng·ml^-1, AUC（0-∞） was （234.98 ±91.43）h·ng·ml^-1, Cmi. was （10.12 ±9.26）ng·ml^-1,Cav was （17.41 ± 5.90）ng·ml^-1. The pharmaeokineties of tripmlidine of simple dose and multiple doses not signifieent differences were observed. Concluslon ： This method is simple and precise. The pharmacokinetics parameters of triprolidine of simple dose and multiple doses have not significent differences. There is no unusual accumulation and has good safety.

关 键 词：盐酸曲普利啶 药物动力学 LC-MS 

分 类 号：R969.1[医药卫生—药理学]