Jiangxi Province Key Laboratory of Drug Design and Evaluation, School of Pharmacy, Jiangxi Science and Technology Normal University, Nanchang 330013, PR China.
Jiangxi Province Key Laboratory of Drug Design and Evaluation, School of Pharmacy, Jiangxi Science and Technology Normal University, Nanchang 330013, PR China.
Biomed Pharmacother. 2020 Sep;129:110376. doi: 10.1016/j.biopha.2020.110376. Epub 2020 Jun 18.
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). 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.
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 依赖性结肠靶向粒子设计的 PTS 粉末。以 pH 敏感聚合物材料 Eudragit S100 超细粉末为壳,药物为核,制备 PTS 核壳复合粒子设计粉末。PTS 复合粒子设计粉末在人工结肠液中的释放增加,在人工胃液和小肠液中的释放减少。本文采用白头翁皂苷 D 在 PTS 中的释放性能和三硝基苯磺酸(TNBS)诱导的大鼠溃疡性结肠炎模型,评价 PTS 复合粒子设计粉末在结肠中的靶向性。结果表明,口服 PTS 复合粒子设计粉末后,结肠组织中白头翁皂苷 D 的含量明显高于原药组。白头翁皂苷 D 在结肠组织中的溶解度也高于胃和小肠。体内的峰时间和保留时间延长,最大血药浓度降低(C)。PTS(50mg/kg)结肠靶向粉末对 SD 大鼠 TNBS 诱导的溃疡性结肠炎的作用优于原药(200mg/kg)。因此,将 PTS 制成结肠靶向制剂对于提高生物利用度、疗效和减少胃肠道刺激具有重要意义。