吴茱萸碱水包油型复合纳米乳的体外释放和在体吸收研究

Release profile and intestinal absorption of evodiamine complex oil-in-water nanoemulation

摘要:

目的：研究吴茱萸碱磷脂复合物水包油型纳米乳（evodiamine nanocomplex oil-in-water nanoemulation，OECNE）体外释放特性和在胃肠吸收情况。方法：采用透析法建立OECNE体外模型，用模型拟合法和相似因子法（f2）考察其体外释放行为；应用大鼠单向肠灌流模型研究其吸收情况。结果：在pH 1.2盐酸溶液和pH 6.8磷酸缓冲溶液中，OECNE的累积释放率均约为EDA的3倍，释放曲线均符合Weibull方程，f2说明OECNE能促进EDA释放；其吸收速率常数在胃部、十二指肠、空肠、回肠和结肠分别为EDA的2.32、2.74、3.36、4.13和2.74倍，有效渗透系数在4个肠段中分别为EDA的4.66、3.70、4.87和3.60倍，OECNE增加了在大鼠胃和不同肠段中药物的吸收。结论：OECNE改善了EDA的释放行为；OECNE提高了EDA的吸收。

Abstract:

Objective：To study its in vitro drug release of evodiamine nanocomplex oil-in-water nanoemulation（OECNE）and to inves－tigate its intestinal absorption. Methods：The dialysis was used to evaluate release profile，and the release behavior was studied by model and similarity factor f2. Single-pass intestinal perfusion was conducted to evaluate intestinal absorption. Results：The cumula－tive releases of OECNE were both about 3-fold that of EDA in 0.1 pH 1.2 hydrochloric acid solution and in pH 6.8 phosphate buffer solution，and OECNE was in accordance with Weibull model in two different solutions，and f2 also revealed OECNE have benefit in drug release. The intestinal absorption rate constant of OECNE was 2.32-fold，2.74-fold，3.36-fold，4.13-fold and 2.74-fold than that of free EDA in stomach，duodenum，jejunum，ileum and colon. The effective permeability of OECNE was 4.66-fold，3.70-fold，4.87-fold and 3.60-fold than that of EDA. Conclusion：OECNE was successfully used to enhance the absorption of EDA.