基于遥控释药胶囊的卡马西平肠吸收药动学研究
首发时间:2011-01-26
摘要:文章研究了卡马西平在健康志愿者近端小肠吸收的药代动力学,了解其定位吸收的体内分布、消除规律。并用自主研制的遥控释药胶囊系统,将200mg卡马西平定位释放于志愿者的近端小肠内。用TDx测定卡马西平的血药浓度,3P87程序拟合房室模型并计算药代动力学参数。结果表明健康志愿者近端小肠定点吸收卡马西平的药-时曲线符合一室开放模型,主要药动学参数:Cmax为(2.1±0.3 )mg.L-1;Tmax为(8.6±2.4)h;T1/2为(6.9±1.6)h;AUC(0-36) 为(33±8)mg.L-1.h-1。卡马西平在志愿者近端小肠定点释放后吸收速率缓慢,吸收总量较好。
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Study on pharmacokinetics of Carbamzepine in the small intestine based on remote controlled capsule
Abstract:To investigate the pharmacokinetics of carbamzepine in the proximal small intestine of healthy volunteers and obtain the standard pharmacokinetic parameters.200mg Carbamzepine was delivered in the proximal small intestine of healthy volunteers by remote controlled capsule system, which made by our work group. The concentration of Carbamzepine in serum was determined by TDx. The main parameters were calculated by 3P87 pharmacokinetic program.The Carbamzepine pharmacokinetics conforms to a one-compartment open model after a single delivered dose of Carbamzepine (200mg) in upper small intestine of healthy volunteers.The main parameters were as follows: Cmax was (2.1±0.3) mg.L-1 ,Tmax was (8.6±2.4)h,T1/2 was (6.9±1.6)h,AUC(0-36) was (33±8 )mg.L-1.h-1,Ka was (0.15±0.06)h and Ke was (0.10±0.04)h.The pharmacokinetics of Carbamzepine showed that there were slow and good absorption in upper small intestine of healthy volunteers.
Keywords: remote control delivery capsule carbamazepine enteral absorption pharmacokinetics
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No.4407713564944129****
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