索他洛尔人体药代动力学和相对生物利用度研究

THE PHARMACOKINETICS AND RELATIVE BIOAVAILABITY OF SOTALOL

目的：以英国施贵宝公司的索他洛尔片剂为对照，研究德国基诺公司研制的索他洛尔片剂的相对生物利用度和药代动力学。方法：以１２名男性健康志愿者为研究对象，采用自身对照法交叉口服单剂量索地洛尔１６０ｍｇ，ＨＰＬＣ法测定服药后不同时间血清中索他洛尔的药物浓度。结果：药物的体内过程经药代动力学程序拟合后，符合二室模型，其主要药代动力学参数如下：Ｃｍａｘ（１．１８±０．１９）ｍｇ／Ｌ；Ｔｍａｘ（３．０４±０．７５）ｈ；Ｔ１／２β（９．４６±２．４８）ｈ；ＡＵＣ０～∞（１３．３０±１．６０）（ｍｇ·ｈ）／Ｌ；相对生物利用度Ｆ＝（１０１．９６±１３．４１）％。结论：经统计学检验证实两种制剂生物等效。

OBJECTIVE :To study the pharmacokinetics and relative bioavailability of sotalol HCl(DarobKnoll)in comparision with Sotacor(Squibb's sotalol HCI). METHODS :The crossover selfcontrolled study was conducted in 12 healthy volunteers.After a single dose of 160 mg drug was given,blood drug concentrations were measured by HPLC. RESULTS :The pharmacokinetic parameters of Darobwere:Cmax (1.180.19)mg/L;Tmax (3.040.75)h;t1/2 (9.462.48)h;AUC0 (13.301.60)(mgh)/L. The relative bioavailability was(101.9613.41)%.No statistical significant difference was found between Daroband Sotacor. CONCLUSION :The two tablets are bioequivalent.