泼尼松龙前体药物的结肠定位研究

目的：探讨以葡聚糖为载体的泼尼松龙前体药物大鼠体内是否具结肠定位性。方法：将前体药物按30μmol.kg^-1的剂量给大鼠灌胃,用HPLC检测大鼠胃肠道不同部位内容物中,药物浓度的变化以及血药浓度的变化,并与游离泼尼松龙作用比较,结果：前体药物主要是在盲肠和结肠释放出泼尼松龙和泼尼松龙半酯,而游离泼尼松龙主要是在上消化道释放药物,前体药物的血药浓度比游离泼尼松龙低,且达峰时间晚。结论,泥尼松龙前体药物具一定结肠定位性,有可能成为一种具有应用前景的结肠炎治疗药物。

The Investigation of a Prednisolone Prodrug for Colon-Specific Drug Delivery

Aim To evaluate colon delivery effects of dextran-prednisolone,a prodrug of prednisolone,in rats.Method The prodrug was given by ig at the dosage of 30μmol·kg-1.The contents of released prednisolone in different parts of rat gastrointestinal tract and in plasma were determined by HPLC,and compared with free dexamethasone.Result We found that prednisolone and prednisolone-hemisuccinate was mainly released in cecum and colon after oral administration of prednisolone prodrug.But free prednisolone is mainly distributed in upper digestive tract.The prednisolone concentration in plasma determinated from prodrug is lower than that from free prednisolone,and the peak time og drug in plasma from prodrug is later than that from free prednisolone.Conclusion The results show that prednisolone can be delivered to large intestine by synthesized prednisolone prodrug,which has a potential in treatment of colitis.