在体循环肠灌流模型研究小檗碱及其磷脂固体分散体的肠吸收特性

Intestinal absorption characteristics of berberine and berberine hydrochloride phospholipid solid dispersions by rat recirculating perfusion model

目的:比较研究小檗碱及其磷脂固体分散体的肠吸收特点,探讨磷脂固体分散体技术提高小檗碱生物利用度的作用机制。方法:采用大鼠循环灌流模型,以酚红为标示物,HPLC法测定在体灌流小檗碱的浓度变化,比较分析小檗碱及其磷脂固体分散体的肠吸收数据。结果:小檗碱肠吸收较差,磷脂固体分散技术可显著促进小檗碱各肠段的吸收,主要促进吸收部位为十二指肠和空肠。结论:小檗碱及其磷脂固体分散体的肠吸收机制主要为被动扩散,磷脂固体分散技术促吸收机制与小檗碱与P-gp亲和力降低或/和小檗碱膜渗透性提高有关。

OBJECTIVE To compare intestinal absorption characteristics of berberine hydrochloride（BBH）and berberine hydrochloride phospholipid solid dispersions（BBH-PSD）by rat recirculating perfusion model,explore berberine bioavailability increasing mechanism by phospholipid solid dispersion technology.METHODS The recirculating perfusion model was established in rats.With phenol red as the indicator,the concentrations of berberine in intestinal perfusion were determined by HPLC,intestinal absorption data of BBH and its phospholipid solid dispersions were analyzed.RESULTS Berberine in the intestinal absorption was poor.BBH-PSD enhanced the absorption of berberine significantly in various intestinal segments.Duodenum and jejunum were the main absorption parts.CONCLUSION The intestinal absorption mechanism of BBH and BBHPSD is mainly passive diffusion,the promoting absorption mechanism of BBH-PSD is concerned with reducing P-gp substrate properties and/or improving the membrane permeability of BBH.