Kim Joo-Il, Park Sang-Wook, Lim Jhong-Jae, Sohn Se-Il, Shin Ji-Su, Park Sang Cheol, Jang Young Pyo, Chung Eun Kyoung, Lee Hong-Woo, Lee Kyung-Tae
1Department of Pharmaceutical Biochemistry, College of Pharmacy, Kyung Hee University, 26, Kyungheedae-ro Dongdaemun-gu, Seoul, 02447, Korea Republic of.
3Central Research Institute, Daewon Pharmaceutical Company, 520 Cheonho-daero, Gwangjin-gu, Seoul Republic of Korea.
Acta Pharm. 2017 Dec 20;67(4):479-494. doi: 10.1515/acph-2017-0037.
In this study, we investigated the gastroprotective effect of an isopropanol extract from the aerial parts of Artemisia princeps (IPAP) and developed a gastroretentive floating tablet of IPAP (IPAP-FR) for maximized local gastroprotective effects. Pre-treatment with IPAP ameliorated the gastric mucosal hemorrhagic lesions in ethanol/HCl- or indomethacin- treated rats. IPAP decreased mucosal hemorrhage of gastric ulcers induced by ethanol or indomethacin plus pyloric ligation in rats. The optimized floating tablet, IPAP-FR, floated on medium surface with more sustained eupatilin release compared to the non-floating control tablet. X-ray photographs in beagle dogs showed that IPAPFR was retained for > 2 h in the stomach. In the ethanol-induced gastric ulcer rat model, the gastric hemorrhagic lesion was improved more substantially with IPAP-FR compared to the non-floating control tablet. Based on these data, our data suggest that IPAP-FR has an improved therapeutic potential for the treatment of gastric ulcer.
在本研究中，我们研究了朝鲜艾蒿地上部分的异丙醇提取物（IPAP）的胃保护作用，并开发了一种IPAP胃滞留漂浮片（IPAP-FR），以实现最大程度的局部胃保护作用。用IPAP预处理可改善乙醇/盐酸或吲哚美辛处理的大鼠的胃粘膜出血性病变。IPAP可减少乙醇或吲哚美辛加幽门结扎诱导的大鼠胃溃疡的粘膜出血。与非漂浮对照片相比，优化后的漂浮片IPAP-FR漂浮在培养基表面，灯盏乙素释放更持久。比格犬的X光照片显示，IPAPFR在胃中保留超过2小时。在乙醇诱导的胃溃疡大鼠模型中，与非漂浮对照片相比，IPAP-FR对胃出血性病变的改善更为显著。基于这些数据，我们的数据表明IPAP-FR在治疗胃溃疡方面具有更高的治疗潜力。
