健康受试者口服西嗪伪麻缓释片后西替利嗪的药动学

目的:建立口服西嗪伪麻缓释片后西替利嗪血药浓度的液相色谱-质谱(LC-MS)测定法,进行人体药动学研究。方法:采用LC-MS法,测定10名健康受试者口服受试制剂(单剂量含西替利嗪5,10 mg和多剂量)后血浆中西替利嗪浓度。结果:口服受试制剂(单剂量含西替利嗪5 mg)后,估算的西替利嗪的药动学参数t1/2β为(9．8±s 2．3)h;tmax为(1．1±0．3)h,cmax为(171±14)μg·L-1,V1／F为(31±5)L,V／F为(45± 9)L,AUC0-(?)为(1 730±187)μg·h·L-1,MRT0-(?)为(10．4±0．7)h。口服受试制剂(单剂量含西替利嗪10 mg) 后,估算的西替利嗪的药动学参数t1/2β为(9．2±1．8)h;tmax为(1．3±0．5)h,cmax为(343±54)μg·L-1,V1／F为 (26±11)L,V／F为(38±12)L,AUC0-(?)为(3 226±298)μg·h·L-1,MRT0-(?)为(10．1±0．8)h。多剂量口服受试制剂后,估算的西替利嗪的药动学参数t1/2β为(10．0±2．3)h,tmax为(1．3±0．4)h,cmax为(268±25)μg·L-1,V1／ F为(17±5)L,V／F为(26±9)L,AUC0-(?)为(2 616±324)μg·h·L-1,MRT0-(?)为(10．0±0．8)h。结论:本方法结果准确,灵敏度高,西替利嗪在大部分人体内的过程符合二室开放模型,其主要药动学参数与国内外文献报道单方西替利嗪数据一致。

Pharmacokinetics of cetirizine through healthy volunteers taking cetirizine and pseudoephedrine sustained-release tablets

AIM:A method was established to study the pharmacokinetics of cetirizine through taking cetirizine, and pseudoephedrine sustained-release tablet in 10 Chinese healthy volunteers. METHODS:Ten healthy volunteers received test tablets respectively for a single oral dose of cetirizine 5,10 mg and multidose. Drug concentrations in plasma were determined by LC-MS. RESULTS:The main pharmacokinetic parameters of test tablets were as follows:t1/2β were(9.8 ± s 2.3) h, (9.2 ± 1.8) h and (10.0 ± 2.3) h;tmax were (1.1 ± 0.3) h, (1.3 ±0.5) h and (1.3 ±0.4) h; cmax were (171 ± 14) μg·L-1,(343 ±54) μg·L-1 and (268 ±25) μg·L-1;V1/F were (31 ± 5) L,(26 ± 11) L and (17 ± 5) L; V/F were(45 ± 9) L,(38 ± 12) L and (26 ± 9) L;AUC0-(?), were (1 730 ± 187) μg·h·L-1, (3 226 ± 298) μgh·L·-1 and (2 616 ± 324) μg·h·L-1 ;MRT0-(?), were(10.4 ± 0.7) h, (10.1 ± 0.8) h and (10.0 ± 0.8) h.The above mentioned data reflected the respective pharmacokinetics of a single oral dose of cetirizine 5 mg,10 mg and multidose in healthy volunteers. CONCLUSION:Utilization of LC-MS for determination the concentration and pharmacokinetics of cetirizine in human plasma is accurate, sensitive and reliable; coinciding to the process taken in a two-compartment open pharmacokinetic model and revealing the equality with other reported by domestic and imported articles.