5-单硝酸异山梨酯缓释片剂的药动学及相对生物利用度研究

PHARMACOKINETICS AND RELATIVE BIOAVAILABILITYOF ISOSORBIDE 5MONONITRATE SUSTAINEDRELEASE TABLETS

采用毛细管气相色谱－电子捕获法测定１８名键康男性志愿者多剂量交叉口服４０ｍｇ５－单硝酸异山梨醇酯缓释制剂（国产片和进口胶囊）后的血药浓度变化情况。单剂量研究结果表明：片与胶囊的ｋａ分别为０．２４７９、０．２５０４ｈ－１，ｋｅ为０．１４０３、０．１３７９ｈ－１，ｔｍａｘ为５．３５、５．３６ｈ，Ｃｍａｘ为３７７．０９、３５１．９８ｎｇ／ｍｌ；缓释片的相对生物利用度为１０６．２８％。多剂量研究结果表明片与胶囊的波动系数分别为１．９７与１．８６。

The isosorbide5mononitrate ( 1 ) concentration in plasma was determined by CGCECD method following an oral multidose of domestic 1 sustained release tablets and imported 1 sustained release capsules given to 18 healthy male volunteers in an open randomized crossover test.The monodose test showed that k\-a was 0.2479 and 0.2504 h\+\{-1\},k\-e 0.1403 and 0.1379 h\+\{-1\},tmax 5.35 and 5.36 h,Cmax 377.09 and 351.98 ng/ml respectively.The relative bioavailability of 1 sustained release tablets was 106.28%.And the multidose test showed that the fluctuation index of the tablets and the capsules was 1.97 and 1.86 respectively.