【摘要】 目的:研究氯氮平缓释片在小猎兔犬（Beagle犬）体内的药动学特征及其口服相对生物利用度。方法:6条Beagle犬随机分成2组,采用自身对照交叉实验设计,分别单次口服氯氮平缓释片和普通片各100mg,用RP-HPLC法检测血药浓度。药动学参数用统计矩法计算。结果:氯氮平缓释片和普通片的tmax分别为（7.3±s 1.0）和（3.3±0.8）h;Cmax分别为（986±274）和（1388±346）μg·L^-1,t_1/2分别为（8.1±1.4）和（9.5±1.0）h;AUC_0-t分别为（17452±5618）和（14174±3420）μg·h·L^-1。以AUC_0-t计算,与普通片相比,氯氮平缓释片的相对生物利用度为（120±28）％。2种制剂的主要药动学参数经统计学检验,两者差异有显著意义（P<0.05）。结论:氯氮平缓释片具有一定缓释特性,生物利用度优于普通制剂。更多还原

【Abstract】 AIM:To study the oral relative bioavailability and pharmacokinetics of clozapine sustained release tablets in Beagle dogs.METHODS:The self-crossover design was conducted in 6 Beagle dogs.A single dose of clozapine sustained release tablets 100mg and clozapine generic tablets 100 mg were taken orally in group A and B,respectively.Plasma clozapine levels were determined by a reversed-phase HPLC method.The pharmacokinetic parameters were analyzed by non-compartmental method.RESULTS:The pharmacokinetic parameters were as follows:tmax,Cmxa,t_1/2and AUC_0-1were（7.3±s1.0）h,（986±274）μg.L^-1,（8.1±1.4） h,（17452±5618）μg.h.L^-1for clozapine sustained-release tablets and（3.3±0.8）h,（1388±346）μg·L^-1,（9.5±1.0）h,（14174±3420）μg.h.L^-1for clozapine generic tablets.Compare with clozapine generic tablets,relative bioavailability of clozapine sustained-release tablets was（120±28）% based on AUC_0-1.There was significant difference between two preparations（P<0.05）.CONCLUSION:Clozapine sustained-release tablet shows prolonged-action characteristics and its bioavailability is better than clozapine generic tablet.更多还原