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用放射性核素标记或与底药混合,利用果胶钙包被底药制成片剂,将这种片剂进入体外模拟消化道环境实验中,12小时内,每小时取样,测定消化液中放射性计数,计算其药物释放率得到时间—释放率曲线。结果表明果胶钙片剂不被胃、小肠酶破坏,只在结肠果胶酶作用下释放底药。在2名志愿者体内实验,照相显像证实了此点,且显示药物移动、释放过程。由此证明果胶钙制剂在结肠内释放底药,对于结肠内局部给药,开辟了一条新途径。
Radionuclide labeled or mixed with the bottom of the drug, the use of pectin-coated calcium-coated tablets made of this tablet into the simulated gastrointestinal environment in vitro experiments within 12 hours, sampling every hour to determine the digestive juice Radioactive count, calculate the drug release rate obtained time - release rate curve. The results show that calcium pectin tablets are not stomach, small intestine enzyme damage, only under the action of the colon pectinase release bottom. In two volunteers in vivo experiments, photo imaging confirmed this point, and shows the drug movement, release process. This proves that the pectin calcium preparation releases the prodrug in the colon, opening up a new way for local administration in the colon.