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姜酚油结肠靶向微丸治疗溃疡性结肠炎的研究。

Investigations of the gingerol oil colon targeting pellets for the treatment of ulcerative colitis.

机构信息

Department of Pharmacy, Changzhou University. Changzhou, China.

Department of Pharmacy, Changzhou University. Changzhou, China.

出版信息

Fitoterapia. 2023 Sep;169:105607. doi: 10.1016/j.fitote.2023.105607. Epub 2023 Jul 12.

DOI:10.1016/j.fitote.2023.105607
PMID:37442485
Abstract

The clinical treatment of ulcerative colitis (UC) faces great challenges due to lifetime medication. In this study, Gingerol oil was extracted and purified by the process easily scale-up and cost effective, with productivity 2.72 ± 0.38% (w/w, versus crude drugs). The quality control of gingerol oil was fully established by HPLC fingerprint with 4 common peaks identified as 6-gingerol, 8-gingerol, 6-shogaol and 10-gingerol. The similarities of 6 batches of gingerol oil are within 0.931-0.999. The protective effects of gingerol oil are equivalent to or even stronger than that of 6-gingerol on inflammation and oxidative stress of HT-29 cells induced by lipopolysaccharide and HO, as well as on UC in mice caused by dextran sulfate sodium salt (DSS). Our research conclusions coincide well with the holistic view of Traditional Chinese Medicine and network pharmacology. The absorption kinetics of gingerol oil were conducted using the in situ intestinal perfusion in rats and comparable absorption were achieved in the jejunum, ileum and colon segments within 2 h. Thus, gingerol oil colon targeting pellets were prepared by extrusion-spherization technique. The cumulative dissolution behaviors and mechanisms were observed and analyzed by fitting to dissolution model. Our studies provided reliable theoretical and experimental support for the gingerol oil as reliable therapeutic choice of UC.

摘要

姜烯酚油的提取和纯化工艺简单、易于放大且成本效益高,产率为 2.72±0.38%(w/w,相对于原料药),溃疡性结肠炎(UC)的临床治疗由于需要终身用药而面临巨大挑战。本研究中。姜烯酚油的提取和纯化工艺简单、易于放大且成本效益高,产率为 2.72±0.38%(w/w,相对于原料药)。通过高效液相色谱指纹图谱对姜烯酚油的质量控制进行了全面建立,共鉴定出 4 个共有峰,分别为 6-姜酚、8-姜酚、6-姜辣素和 10-姜辣素。6 批姜烯酚油的相似度在 0.931-0.999 之间。姜烯酚油对脂多糖和 HO 诱导的 HT-29 细胞炎症和氧化应激以及葡聚糖硫酸钠(DSS)诱导的 UC 小鼠的保护作用与 6-姜酚相当或更强。我们的研究结论与中药整体观和网络药理学相吻合。采用大鼠在体肠灌流法研究了姜烯酚油的吸收动力学,在 2 h 内,姜烯酚油在空肠、回肠和结肠段的吸收相当。因此,采用挤出-造球技术制备了姜烯酚油结肠靶向微丸。通过拟合溶解模型观察和分析了累积溶解行为和机制。我们的研究为姜烯酚油作为 UC 的可靠治疗选择提供了可靠的理论和实验依据。

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