单剂量和多剂量口服西替伪麻缓释片的人体药动学  

Pharmacokinetics of single-dose and multi-dose of oral cetirizine-pseudoephedrine substained-release tablets in healthy volunteers

作　　者：陈伟力[1] 戴佩芳[1] 储楠楠[1] 李雪宁[1] 徐红蓉[1] 诸骏仁[1] 

机构地区：[1]复旦大学附属中山医院临床药理室,上海200032

出　　处：《中国新药杂志》2008年第6期518-522,共5页Chinese Journal of New Drugs

摘　　要：目的：评价单剂量和多剂量口服西替伪麻缓释片的药动学特征。方法：10名健康志愿者单剂量和多剂量口服西替伪麻缓释片后,用LC-MS/MS法同时测定血浆中盐酸西替利嗪和盐酸伪麻黄碱的浓度。结果：盐酸西替利嗪和盐酸伪麻黄碱的主要药动学参数如下：单剂量Cmax分别为（249.50±55.81）和（433.40±86.29）ng.mL-1,Tmax分别为（1.35±1.06）和（4.00±1.00）h,AUC0-t分别为（2 393.11±684.31）和（5 131.96±1 327.18）ng.h.mL-1;多剂量达稳态：Cav分别为（199.91±59.03）和（366.73±126.78）ng.mL-1,Tmax分别为（1.35±1.08）和（3.95±0.60）h,AUCss分别为（2 398.90±708.32）和（4 400.72±1 521.38）ng·h·mL^-1,DF分别为（112.35±23.22）%和（86.68±38.38）%。结论：西替伪麻缓释片在中国健康人体内安全耐受性良好,盐酸伪麻黄碱具有缓释特征,多剂量给药后药物在体内无明显蓄积现象。Objective：To evaluate the pharmacokinetics of single-dose and multi-dose of oral cetirizinepseudoephedrine substained-release tablets in healthy volunteers. Methods： Ten healthy volunteers were selected to receive single-dose and multi-doses of cetirizine-pseudoephedrine substained-release tablets. The plasma concentrations of both drugs were determined by LC-MS/MS method. Results： The pharmacokinetic parameters of cetirizine hydrochloride and pseudoephedrine hydrochloride after single-dose were as follows： the Cmax were （249.50 ± 55.81） and （433.40±86.29）ng·mL^-1; T were （1.35 ±1.06） and （4.00±1.00） h; AUC0-1were （2393.11± 684.31 ） and （5 131.96± 1 327.18）ng·h· mL^-1, respectively. The parameters on 8th day after multi-doses： C,, were （199.91±59.03） and （366.73 ±126.78） ng·mL^-1; Tmax were （1.35 ±1.08） and （3.95 ±0.60）h; AUCss were （2 398.90 ± 708.32） and （4 400.72 ± 1 521.38 ） ng· h· mL^- 1 ; degree of flunctuation （ DF% ） were （112.35 ± 23.22）% and （86.68 ± 38.38）%, respectively. Multi-doses of the tablets were well tolerated in healthy volunteers. Conclusion： Pseudoephedrine hydrochloride has the characteristics of substained release. There is no accumulation of cetirizine hydrochloride and pseudoephedrine hydrochloride after multi-doses in healthy volunteers.

关 键 词：西替伪麻缓释片 药动学 LC-MS/MS 

分 类 号：R969.1[医药卫生—药理学] R978[医药卫生—药学]