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为了探讨以葡聚糖 (平均分子质量 2 0 0 0 0 )为载体合成的地塞米松前体药物在大鼠胃肠道内的转运及活性药物的释放情况 ,以 5μmol·kg-1地塞米松给大鼠 ig,采用高效液相色谱法监测该前体药物在大鼠胃肠道不同部位释放出地塞米松的情况及血药浓度变化 ,并与地塞米松相对比较 .结果表明 ,地塞米松前体药物 ig后 ,地塞米松主要集中在盲肠和结肠内释放 ,吸收显著减少 .其血浆药峰浓度为1 1 0 μg·L-1,达峰时间 6.3h.而地塞米松 ig后 ,其大量出现在胃 ,小肠近端及远端内容物中 ,并被迅速吸收入血 ,其血浆药峰浓度高达 2 .1 2 mg· L-1,达峰时间为 2 .2 h;上述结果表明 ,以葡聚糖为载体合成的地塞米松前体药具有良好的结肠定位转释作用 ,有可能成为一种具有应用前景的结肠炎治疗药物
In order to explore the transport of dexamethasone prodrug synthesized in dextran (average molecular weight 2000) in the gastrointestinal tract of rats and the release of active drug, 5μmol · kg-1 dexamethasone To rats ig, using high performance liquid chromatography to monitor the prodrug release of dexamethasone in different parts of the gastrointestinal tract of rats and changes in plasma concentrations, and compared with dexamethasone.The results show that the dexamethasone Dexamethasone was mainly released in the cecum and colon after ig of the prednisolone, and its absorption was significantly reduced.The peak plasma concentration was 110 microg x L (-1) and peak time was 6.3 h, while dexamethasone , Which appeared in the stomach, proximal and distal contents of the small intestine, and was quickly absorbed into the blood, the plasma concentration peak as high as 2.12 mg · L-1, the peak time was 2.2 h; The results showed that dexamethasone-based prodrugs synthesized with dextran had good colon-specific translocation and release potential and could become a promising colitis treatment drug