非索伪麻缓释片在健康人体中的药代动力学

Single and multiple dose pharmacokinetics of fexofenadine/peudoephedrine sustained release tablet in healthy volunteers

目的研究中国健康志愿者单次和多次口服非索伪麻缓释片后的药代动力学行为,并评价非索非那定、伪麻黄碱的单次和多次给药药代动力学参数差异。方法 12名健康志愿者单次,多次口服非索伪麻缓释片1片(含盐酸非索非那定60 mg和盐酸伪麻黄碱120 mg),qd,连用8 d,测定给药前和给药后48 h内的血药浓度,用DAS 2.1.1软件计算药代动力学参数。结果单次和多次口服非索伪麻缓释片后药代动力学参数如下,非索非那定的t1/2分别为(10.88±5.67),(7.94±1.80)h,tmax分别为(2.83±0.58),(2.08±0.67)h,cmax分别为(316.42±171.34),(316.50±158.37)ng.mL-1,AUC0-t分别为(1816.33±904.83),(1726.25±741.16)ng.h-1.mL-1;伪麻黄碱的t1/2分别为(6.56±1.04),(8.71±2.38)h,tmax分别为(5.67±2.23),(6.00±2.52)h,cmax分别为(193.58±52.40),(186.17±35.90)ng.mL-1,AUC0-t分别为(3056.92±982.46),(2722.25±602.77)ng.h-1.mL-1。结论单次和多次口服非索伪麻缓释片后,除非索非那定的tmax和伪麻黄碱的t1/2剂量间差异有统计学意义,其他差异均无统计学意义。单次给药后伪麻黄碱的CL/F性别间差异有统计学意义,多次给药后非索非那定的CL/F、AUC0-t性别间差异有统计学意义,其他参数性别间差异无统计学意义。

Objective To study the pharmacokinetics of single and multiple dose fexofenadine/peudoephedrine sustained release tablet in healthy subjects, and assess single and multiple dose pharmacokinetic differences of fexofenadine and peudoephedrine. Methods Twelve healthy subjects took single and multiple oral administrations of fexofenadine / peudoephedrine sustained release tablet. Plasma concentrations were determined before and after administration of 48 h. The pharmacokinetic parameters were analyzed by DAS 2. 1.1 sofeware. Results The pharmacokinetic parameters of single and multiple fexofenadine as follows： t1/2 were （ 10. 88 ± 5.67 ）, （ 7.94 ± 1.80 ） h, tmax were （ 2.83 ± 0. 58 ）, （2.08 ±0. 67） h, cmax were （316. 42 ± 171.34）, （316. 50 ± 158.37） ng.mL-1, AUC0-1 were （1816.33 ±904.83）, （1726.25 ±741.16） ng.h-1.mL-1. The parameters of eudoephehrine as follows： t1/2 were （6.56±1.04）, （8.71 ±2.38） h, tmax were （5.67 ±2.23）,（6.00 ± 2.52） h, cmax were （ 193.58 ±52. 40）, （ 186. 17 ±35.90） ng.mL-1, AUC0-t were （3056. 92 ± 982. 46 ）, （ 2722. 25 ± 602.77 ） ng.h-1.mL-1. Conclusion After single and multiple oral dose of fexofenadine/pseudoephedrine sustained release tablets, differences in the pharmacokinetic tically significant, but differences in t of fexofenadine and t1/2 of peudoephedrine was statistically significant. There were significant differences between genders in CL/F of pseudoephedrine after single dose administration and CL/F, AUC0-1, of fexofenadine after multiple dose administration, other parameters showed no statistical difference.