溃康结肠靶向微丸靶向性评价研究

Evaluation of targeting property for Kuikang colon targeted pellets

目的:探索大鼠胃肠药物浓度测定评价溃康结肠靶向微丸的可行性。方法:HPLC测定黄芩苷和黄芩素的含量,比较给药3h和6 h后,靶向微丸和普通微丸在大鼠胃肠道中药物浓度差异。结果:给药3 h后,靶向微丸组大鼠胃肠道中黄芩苷原形的回收率约70%,明显高于普通微丸组(约20%),微丸形状完整,大部分集中于小肠下段,表明其释药部位为小肠下段或结肠;6 h后,药物以黄芩素形式分布于大肠,证明制剂释药完全。结论:在体测定胃肠道中黄芩苷的残余量,适用于溃康结肠靶向微丸的靶向性评价。该制剂能使药物达到结肠靶向给药效果。

Objective： To evaluate colon targeting characteristic of Knikang colon targeted pellets （KCP） with determination of residual baicalin and baicalein concentration in gastrointestinal tract （GIT） . Method： The baicalin and baicalein were assayed by HPLC. The recovery differences of the drug between KCP and conventional pellets from GIT were investigated, three and six hours after administration. Result： The baicalin recovery of KCP （70%） from rat GIT was higher than that of CP （about 20% ）. Most of KCP were intact at 3 h after oral administration, and distributed in lower ileum. It indicated that release site of KCP was in lower ileum and colon. Six hours later, a small amount of baicalin was recovered in intestime, which showed that the release of baicalin from KCP was complete. Conclusion： The determination of residual baicalin in rat GIT was feasibility for evaluating KCP. The result confirmed KCP of colon targeting property.