异丁司特缓释片在正常人体内的药代动力学和相对生物利用度  

Pharmacokinetics and Relative Bioavailability of KC-404 Sustained Release Tablets in Healthy Volunteers

作　　者：李铜铃[1] 庞怡诺[1] 王志霄[1] 贾玉蓉[1] 程强[2] 孙健[1] 

机构地区：[1]四川大学华西药学院临床药学教研室,成都610041 [2]四川抗菌素研究所

出　　处：《四川大学学报（医学版）》2003年第3期541-543,共3页Journal of Sichuan University(Medical Sciences)

摘　　要：目的　研究异丁司特缓释片和缓释胶囊在健康人体内的药物动力学和生物利用度。方法　采用高效液相色谱法测定 19名健康男性志愿受试者单剂量口服 2 0 m g异丁司特缓释片或 2 0 m g异丁司特缓释胶囊后 ,血浆中异丁司特浓度的变化。结果　经 3 P87药动学程序处理 ,以异丁司特计其 AUC0→∞ 分别为 ( 740 .12 ng· h) / ml和 ( 72 4.0 4ng· h) / ml,tmax分别为 5 .3 7h和 5 .11h,Cmax分别为 46.98ng/ ml和 46.2 9ng/ m l,T1 / 2 分别为 7.4h和7.0 h,MRT0→∞ 分别为 14.78h和 14.3 9h。配对 t检验结果表明 ,两种异丁司特制剂的 AUC、tmax、Cmax、T1 / 2 及MRT0→∞ 无显著性差异 ( P>0 .0 5 )。双单侧 t检验 AUC、tmax、Cmax及 T1 / 2 的 90 %置信区间位于有效置信区间范围内。以异丁司特缓释胶囊为标准参比制剂 ,异丁司特缓释片的相对生物利用度为 10 2 .6%。Objective To study the pharmacokinetics and relative bioavailability of KC-404 sustained release tablets and capsules in healthy volunteers. Methods The concentration of KC-404 in serum was determined by HPLC method after a single oral dose (20 mg) of tablet or capsule was administered to 19 healthy male volunteers respectively in an open randomized cross-over test. Results After being processed by 3P87 pharmacokinetics program, the experiment data showed that the pharmacokinetic parameters of the tablets and the capsules were AUC 0→∞: 740.12 ng·h/ml and 724.04 ng·h/ml; t max: 5.37 h and 5.11 h; C max: 46.98 ng/ml and 46.29 ng/ml; T 1/2: 7.4 h and 7.0 h; MRT 0→∞: 14.78 h and 14.39 h respectively. There were no significant differences in AUC, t max, C max, T 1/2 and MRT 0→∞ between these two preparations(P>0.05). The relative bioavailability of KC-404 sustained release tablets was 102.6%. Conclusion These two preparations are bioequivalent.

关 键 词：异丁司特缓释片 人体内 药代动力学 相对生物利用度 

分 类 号：R969[医药卫生—药理学]