Drug release in vivo and efficacy evaluation of a new colon targeted powder of total saponins of Pulsatilla
Drug release in vivo and efficacy evaluation of a new colon targeted powder of total saponins of Pulsatilla
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新型白头翁总皂苷结肠靶向粉体内释药及药效评价
DOI：
10.1016/j.biopha.2020.110376
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发表时间：
2020-09-01
影响因子：
7.5
通讯作者：
Liu, Hongning
中科院分区：
文献类型：
--
作者：
Chen, Zhenhua;Zhao, Teng;Liu, Hongning
基于白头翁总皂苷(PTS)的抗溃疡性结肠炎(UC)作用，制备了一种pH依赖的结肠靶向粉剂。以pH敏感的高分子材料Eudradit S100超细粉末为壳层，以药物为核，制备了PTS的核壳复合微粒设计粉末。PTS复合颗粒设计粉在人工结肠液中的释放量增加，在人工胃液和小肠液中的释放量减少。本文通过PTS中白头翁皂苷D的释放性能和三七总皂甙诱导的大鼠溃疡性结肠炎模型来评价PTS复合颗粒设计粉在结肠中的靶向性，结果表明，口服PTS复合颗粒设计粉后，结肠组织中白头翁皂苷D的含量显著高于原药物组。白头翁皂苷D在结肠组织中的溶解度也高于在胃和小肠中的溶解度。达峰时间延长，体内滞留时间延长，最大血药浓度降低(C-max)。PTS结肠靶向粉剂(50 mg/kg)对TNBS诱导的SD大鼠溃疡性结肠炎的抗炎作用优于原药(200 mg/kg)。因此，将PTS制成结肠靶向制剂，对于提高生物利用度、疗效、减少胃肠道刺激具有重要意义。
Based on the anti-ulcerative colitis (UC) effect of total saponins of Pulsatilla (PTS), a pH dependent colonic targeting particle design powder of PTS was prepared. The core-shell composite particle design powder of PTS was prepared with pH sensitive polymer material Eudragit S100 superfine powder as shell and the drug as core. The release of PTS composite particle design powder was increased in the artificial colon fluid and decreased in the artificial stomach and small intestine fluid.In this paper, the release performance of Pulsatilla saponin D in PTS and the ulcerative colitis model induced by TNBS in rats were used to evaluate the targeting of PTS composite particle design powder in colon.The results showed that the content of Pulsatilla saponin D in colon tissue was significantly higher than that of the original drug group after oral administration of PTS composite particle design powder. The solubility of Pulsatilla saponin D in colon tissue was also higher than that in the stomach and small intestine. The peak time and retention time in vivo were prolonged, and the maximum blood concentration was decreased (C-max). The effect of colonic targeting powder of PTS (50 mg/kg)on anti-ulcerative colitis induced by TNBS in SD rats was better than the original drug (200 mg/kg). Therefore, it is a great significance to make the PTS into colon targeted preparation for improving bioavailability, efficacy and reducing gastrointestinal stimulation.