得理多与两种国产卡马西平片在人体内生物利用度研究

Comparative bioavailability of tegretol and two domestic carbamazepine tablets in normal volunteers

目的：比较两种国产卡马西平（Ｃａｒｂａｍａｚｅｐｉｎｅ，ＣＢＺ）片（Ｂ，Ｃ）与北京ＣＩＢＡ－ＧＥＩＧＹ产得理多（Ｔｅｇｒｅｔｏｌ）片（Ａ）的人体相对生物利用度。方法：采用ＦＰＩＡ测定人血清ＣＢＺ浓度。１２名健康志愿者口服３００ｍｇＣＢＺ片，采用随机单盲同体交叉试验，进行Ｂ，Ｃ与Ａ人体相对生物利用度研究。结果：Ｂ，Ｃ对Ａ的相对生物利用度分别为（１００．７±２０．９）％，（１１０．２±２３．１）％；Ａ，Ｂ，Ｃ的Ｋａ分别为（０．１５±０．１１），（５．３±６．６）和（８．０±１５．３）ｈ－１，达峰时间（Ｔｍａｘ）分别为（１６．３±５．４），（３．４±３．８）和（２．３±１．９）ｈ；消除半衰期（Ｔ１／２）分别为（４２．０±９．９），（４２．１±１３．９）和（４１．６±１３．４）ｈ；血药浓度曲线下面积（ＡＵＣ０→∞）分别为（２６５．２±５９．４），（２６５．６±８２．３）和（２８６．１±７３．６）ｍｇ．ｈ．Ｌ－１。经统计学分析Ｂ，Ｃ与Ａ的Ｔｍａｘ，Ｋａ差异有极显著性（Ｐ＜０．０１），其余各参数差异均无显著性（Ｐ＞０．０５）。单次给药后，ＣＢＺ血药浓度－时间曲线出现双峰或多峰现象。结论：Ｂ，Ｃ生物等效。

Objective:To compare the relative bioavailability of tegretol and two domestic carbamazepine tablets in human.Methods:Carbamazepine serum concentration was determined by FPIA. A single oral dose of 300 mg Carbamazepine tablet was given respectively to 12 volunteers in a randomized, single blind, cross over study for comparison of relative bioavailability in human. Results:The relative bioavailability of two domestic Carbamazepine tablets was ( 100.72 ± 20.93 ),( 110.21 ± 23.07 )%。Absorption rate constant (Ka) was significantly smaller for Tegrelol( 0.1460 ± 0.1077 )h -1 than that for two domestic Carbamazepine tablets ( 5.2931 ± 6.5778 ),( 7.9617 ± 15.2934 )h -1 . The mean time to maximum concentration(T max ) was significantly greater after Tegretol ( 16.28 ± 5.37 )h than that after two domestic Carbamazepine tablets ( 3.35 ± 3.82 ),( 2.26 ± 1.86 )h. After single dosing,the serum level time curves appeared double or multiple peaks.Conclusion:The processes of two domcstic Carbamazepine tablets in human body are similar, but both of them are different to that of Tegretol.