麦冬多糖口服吸收促进剂的研究

Oral absorption enhancers of Ophiopogon japonicas polysaccharides

目的:研究适用于麦冬多糖(OJP)的口服吸收促进剂,为寻求利用吸收促进剂来实现OJP口服给药提供依据。方法:通过Caco-2细胞模型,对薄荷油、丁香油、冰片、三七花皂苷、麦冬皂苷、人参皂苷Rg1、三七皂苷R1和癸酸钠的吸收促进作用和细胞毒性进行评价。通过大鼠在体肠段试验,对OJP在各肠段的吸收情况以及癸酸钠对吸收的促进作用进行研究。结果:癸酸钠是既有效又安全的吸收促进剂,而丁香油、薄荷油、麦冬皂苷的吸收促进作用与细胞毒性高度相关。OJP在十二指肠、回肠和结肠段中均有少量吸收,其中在十二指肠中的吸收情况最好,回肠次之,而在结肠段最差。在使用癸酸钠之后,各肠段对OJP的吸收均有显著提高,尤以结肠段最为明显。结论:吸收促进剂的吸收促进作用往往与其细胞毒作用相关,选用安全而有效的吸收促进剂来增加麦冬多糖的口服吸收是有效且具有应用价值的一种方法。

Objective： To investigate suitable oral absorption enhancer （s） for Ophiopogon japonicas polysaccharides （OJP） and provide bases of utilizing the absorption enhancer to realize the oral administration of OJP. Method： The absorption enhancement effects and cytotoxicity of clove oil, peppermint oil, borneol, Sanqi saponins, Maidong saponins, Ginseng saponin Rgl, Sanqi saponin R1 and sodium caprate （SC） were evaluated via Caco-2 cell culture model. The absorption of OJP from rat intestinal segments and the absorption enhancement effect of SC were investigated by in situ experiments of rat intestinal segments. Result： SC was an effective and safe absorption enhancer. However, the absorption enhancement effects of clove oil, peppermint oil and Maidong saponins were highly correlated with their cytotoxieity. OJP alone was poorly absorbed from all the rat intestinal segments. It was rapidly absorbed when coadministered with SC, and the absorption increase was significant and the best absorption enhancing site of SC for OJP was colon. Conclusion： The absorption enhancement effects of absorption enhancers are often correlated with their cytotoxicity. Co-administrating a powerful and safe absorption enhancer is an effective and valuable method of enhancing oral absorption of OJP.