氢溴酸加兰他敏缓释片人体药物动力学研究  

Study of Pharmacokinetics of Galanthamine Hydrobromide Extended-release Tablets in Healthy Volunteers

作　　者：文爱东[1] 杨志福[1] 吴寅[1] 周敏[1] 陈苏宁[1] 李薇[1] 

机构地区：[1]第四军医大学西京医院药剂科,西安710032

出　　处：《中国药师》2007年第3期214-217,共4页China Pharmacist

摘　　要：目的:建立HPLC-MS方法分析人血浆中氢溴酸加兰他敏的含量,并研究氢溴酸加兰他敏缓释片在健康人体内的药物动力学特征。方法:12名健康受试者口服单剂量(10mg)或多剂量氢溴酸加兰他敏缓释片(10 mg×7 d)后,分别在不同时间点收集血样,HPLC-MS法测定,采用DASS 2.0软件计算给药后的药物动力学参数。结果:健康受试者单剂量口服氢溴酸加兰他敏缓释片的t_(max)为(4.0±1.4)h;C_(max)为(27.2±3.3)μg·L^(-1);t_(1/2)为(10.3±0.9)h;MRT为(15.4±1.3);AUC_(0-60h)为(483.1±70.4)μg·h·L^(-1)。多剂量口服氢溴酸加兰他敏的AUC_(0→∞)为(916.0±99.0)μg·h·L^(-1),C_(max)^(ss)为(56.8±11.6)μg·L^(-1),C_(min)^(ss)为(15.5±4.0)μg·L^(-1),C_(ss)为(38.2±4.1)μg·L^(-1),DF为(1.1±0.3),t_(max)为(3.6±1.9)h,t_(1/2)为(11.7±1.4)h。结论:氢溴酸加兰他敏缓释片主要药动学参数单剂量和多剂量之间无显著性差异,具有明显的缓释特征,多剂量给药后体内无蓄积。Objective： To investigate the pharmacokinetic characteristic of galanthamine hydrobmmide extended-release tablet （10 mg） in healthy volunteers by HPLC-MS. Method： After the single dose （ 10 mg）, or the multiple doses of galanthamine hydrobromide extended-release tablet （ 10 mg） for 7 days were administrated orally in 12 healthy volunteers respectively, the samples were collected at different times and were determined by HPLC-MS method. The parameters of pharmacokinetics were calculated by DASS 2.0 soft- ware. Result： The major pharmacokinetic parameters of the single dose of galanthamine were as follows： tmax Was（4.0 ± 1.4） h; Cmax, was （27.2 ±3.3） μg·L^-1, t1/2 was （ 10.3 ±0.9） h, MRT was （ 15.4 ± 1.3）, AUC0-60h was （483.1 ±70.4） μg·h·L^-1. Major pharmacokinetic parameters for multiple doses were as follows ： A UC0→∞ was （ 916.0 ± 99.0） μg· h· L^ -1, Cmax^ss was （56.8 ± 11.6） μg· L^-1 ,Cmin^ss was （15.5 ±4.0） μg·L^-1, Css was （38.2±4.1） μg·L^-1 ,DF was （1.1±0.3） ,tmax Was （3.6 ± 1.9）h,t1/2 was （11.7 ± 1.4） h. Conclusion： There were no significant differences in pharmacokinetic parameters of galanthamine hydrobromide extended-release tablet （ 10 mg） between single and multiple administration, no accumulation after muhidoses administration in vivo.

关 键 词：氢溴酸加兰他敏 药物动力学 单剂量 多剂量 HPLC-MS 

分 类 号：R969.1[医药卫生—药理学]