果胶钙包被放射性核素制剂在结肠内释放的研究

The Study of Release of Coated Radionuclide Preparation with Pectic Calcium from Colonic Application

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。

The radionuclide coated with pectic cacium had been prepared in tablet,which was tested in the simulated human digestive tract.The sample of the digestive juice which was collected every hour within 12 hours was counted by the scintillation counter.The delivery rate based on the counts of the samples could be developed a time-delivery rate curve.The expiremental results demonstrated that the pectic calcium coated tablet was not destroyed in the stomach or small intestine,but in the colon the tablet was broken down to deliver radionuclide labelling-drug which was influened by the pectic enzyme.The same expirement was carried out in two volunteers,the gamma scintilgraphic studies displayed the kinetics of the radionuclide labelled-drug and its delivery process colon.The preliminary results indicated that a colonic drug delivery system with pectic calcium has developed a broad prospect of local application of drugs.