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目的 观察强的松龙·葡聚糖 (平均 Mr5 0万 )连接物的结肠定向释放特性 .方法 通过将所合成的强的松龙·葡聚糖连接物与大鼠胃肠道不同部位内容物稀释液一起孵育 ,观察强的松龙的释放情况 .结果 在 1 6 0 min的孵育过程中 ,强的松龙·葡聚糖连接物在胃肠道上部内容物中水解释放出少量强的松龙及强的松龙琥珀酸半酯 ,最大释放量小于3μm ol·L- 1 ;而在胃肠道下部内容物中水解释放出大量强的松龙及强的松龙琥珀酸半酯 ,最大释放量为 1 4μmol· L- 1 .结论 葡聚糖可保护其与强的松龙相连接的酯键免受胃肠道上部酯酶的水解 ,使强的松龙集中在结肠释放 .强的松龙·葡聚糖连接物可为一种能在结肠定向转释的药物 .
OBJECTIVE To observe the directional release characteristics of the colon of the prednisolone-dextran (average Mr 500,000) conjugate.Methods The contents of the different parts of the gastrointestinal tract Diluents were incubated together to observe the release of prednisolone.Results During the 160 min incubation, the prednisolone-dextran conjugates hydrolyzed in the upper part of the gastrointestinal tract to release a small amount of prednisone Long and strong prednisolone succinate half ester, the maximum release of less than 3μmol·L- 1; and in the lower part of the gastrointestinal tract content release a large number of prednisolone and prednisolone succinate half ester, the largest Release amount of 14μmol · L- 1. Conclusion dextran can protect the ester bond with the prednisolone from the hydrolysis of the upper esterase in the gastrointestinal tract so that prednisone concentrated in the colon release strong Pineel-dextran conjugates can be a type of drug that can be released in the colon.