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。
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 cumulative 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.
出处
《重庆医科大学学报》
CAS
CSCD
北大核心
2018年第1期135-138,共4页
Journal of Chongqing Medical University
基金
重庆市科委资助项目(编号:cstc2015jcyj BX0027)
关键词
吴茱萸碱
磷脂纳米复合物
纳米乳
体外释放
透析法
evodiamine
drug-phospholipid nanocomplex
nanoemulation
drug release in vitro
dialysis method
