健康受试者口服西嗪伪麻缓释片后伪麻黄碱的药动学

Pharmacodynamic study of pseudoephedrine compound sustained-release tablets

目的:建立人血浆中伪麻黄碱浓度的液相色谱-质谱测定法,进行人体药动学研究。方法:测定10名健康受试者口服受试制剂后血浆中伪麻黄碱浓度。结果:单剂量口服受试制剂(含伪麻黄碱120,240mg)后药动学参数T1/2β为(5.5±0.7)、(5.2±0.7)h,Tmax为(4.8±0.9)、(4.7±0.8)h,Cmax为(226.7±21.1)、(455.1±100.2)μg.L-1,CL为(41.0±18.6)、(43.9±15)L.h-1,V/F为(209.3±116.0)、(218.4±103.5)L,AUC(0-t)为(2929.9±474.9)、(5466.8±1372.6)μg.h.L-1,MRT为(10.2±0.7),(9.6±0.8)h。多剂量口服受试制剂(含伪麻黄碱120mg,bid)达稳态后药动学参数Csmsax为(272.0±52.6)μg.L-1,Csmsin为(105.0±37.2)μg.L-1,Cav为(198.6±39.0)μg.L-1,CL为(50.4±16.8)L.h-1,DF为(0.86±0.20),AUC(0-t)为(2382.6±467.4)μg.h.L-1。结论:本方法灵敏高,结果准确,伪麻黄碱在大部分人体内过程符合一室开放模型,其主要药动学参数与国内外文献相近,可为临床给药方案提供参考。

OBJECTIVE A method was established to study the pharmacokinetics of Pseudoephedrine tablet by LC-MS. METHODS 10 healthy volunteers received tested tablets for a single oral dose of Pseudoephedrine 120,240 mg and muhidose. Drug concentrations in plasma were determined. RESULTS Pharmacokinetic parameters of Pseudoephedrine after ＇single oral doses（ 120、240 mg）were as follow：T1/2β为（5.5±0.7）、（5.2±0.7）h,Tmax为（4、8±0.9）、（4.7±0.8）h,Cmax为（226.7±21.1）、（455.1±100.2）μg·L^-1,CL为（41.0±18.6）、（43.9±15）L·h^-1,V/F为（209.3±116.0）、（218.4±103.5）L,AUC（0-t）为（2929.9±474.9）、（5466.8±1372.6）μg·h·L^-1,MRT为（10.2±0.7）,（9.6±0.8）h. The main pharmacokinetic parameters of muhidose（120 mg,bid） were as follows：Cmax^ss为（272.0±52.6）μg·L^-1,Cmin^ss为（105.0±37.2）μg·L^-1,Cav为（198.6±39.0）μg·L^-1,CL为（50.4±16.8）L·h^-1,DF为（0.86±0.20）,AUC（0-t）为（2382.6±467.4）μg·h·L^-1. CONCLUSION The method was sensitive,the results were accurate, a one-compartment open pharmacokinetic model was adapted to Pseudoephedrine plasma concentration-time data analysis, the main pharmacokinetic parameters were similar to those reported domestic and abroad, so it could provide information in clinic.