盐酸倍他洛尔片在健康人体的药代动力学和相对生物利用度  

Pharmacokinetics and relative bioavailability of betaxolol hydrochloride tablets in Chinese healthy volunteers

作　　者：郜娜[1] 乔海灵[1] 田鑫[1] 贾琳静[1] 郭玉忠[1] 张莉蓉[1] 

机构地区：[1]郑州大学临床药理研究所,郑州450052

出　　处：《中国临床药理学杂志》2007年第3期191-194,共4页The Chinese Journal of Clinical Pharmacology

摘　　要：目的研究盐酸倍他洛尔(抗高血压药)在健康人体内药代动力学和相对生物利用度。方法18名男性健康受试者单剂量交叉口服盐酸倍他洛尔片进口制剂和被试制剂40mg后,用高效液相色谱-荧光法测定不同时间血药浓度。所得药-时数据经3P97软件处理。结果2制剂药-时曲线均符合一房室开放模型,tmax分别为(4.6±1.4),(4.1±1.1)h;Cmax分别为(51.45±9.21),(53.69±10.58)μg·L-1;t1/2ke分别为(17.16±2.27),(16.47±2.80)h;AUC0-60h分别为(1007±165),(1145±218)μg·h·L-1;AUC0-∞分别为(1165±214),(1281±250)μg·h·L-1。与进口制剂相比,国产制剂的相对生物利用度F0-t为(89.4±15.0)%,F0-∞为(92.6±18.0)%。结论2种制剂具有生物等效性。Objective To study pharmacokinetics and relative bioavai - lability of betaxolol hydrochloride in young healthy volunteers. Methods A single oral dose（40 mg） of the standard formulation and the test formulation were given to 18 volunteers in randomized cross - over test. The betaxolol concentrations in plasma were determined by HPLC - fluorescence method. Results The concentration - time curves of two formulations fitted to a one - compartment open model. The tmax were （4.6 ± 1.4）h and （4.1 ± 1.1 ） h, Cmax were （51.45 ± 9.21 ） μg · L^-1 and （53.69±10.58） μg·L^-1, t1/2ke were （17. 16±2.27） h and （16.47 ±2.80） h,AUC0-∞ were （1007 ±165） μg · h · L^-1 and （1145 ±218） μg · h · L^-1,AUC0-∞ were（1165 ±214） μg · h · L^-1 and （1281 ± 250） μg · h · L^-1, respectively. The pharmacokinetic parameters ob- tained from our studies showed no significant difference between two formulations（P 〉 0.05 ）. The relative bioavailability F0-t was （ 89.4 ± 15.0）% ,F0-∞ was （92.6 ± 18.0）% of testd formulation. Conclusion The results of statistical analysis suggest that the two formulations were bioequivalent.

关 键 词：盐酸倍他洛尔片 高效液相色谱-荧光法 药代动力学 相对生物利用度 

分 类 号：R969.1[医药卫生—药理学] R972.4[医药卫生—药学]