中国药理学通报2018，Vol.34Issue(5)：724-728,5.DOI:10.3969/j.issn.1001-1978.2018.05.026
吴茱萸碱丁酰基衍生物固体脂质纳米粒的体外释放及在体胃肠吸收研究
In vitro release and in situ gastrointestinal absorption of evodiamine butyryl derivative-loaded solid lipid nanoparticles
摘要
Abstract
Aim To prepare evodiamine butyryl deriva-tive (EBD) and evodiamine butyryl derivative-loaded solid lipid nanoparticles (EBDLN), and study its re-lease in vitro,and to investigate its in situ gastrointesti-nal absorption. Methods EBD was prepared by a one-step synthetized method, and then EBDLN was prepared by a film dispersion method. Dynamic dialy-sis was used to evaluate drug release in vitro,and sin-gle-pass gastrointestinal perfusion was employed to study the gastrointestinal absorption of EDM,EBD and EBDLN. Results In identical release media, there were identical drug release tendencies of EBD and EB-DLN, but the release rate of EBDLN was faster than EBD. Compared with EDM and EBD, the Kavalues and Pappvalues of EBDLN in every perfusion segment increased significantly. The Kaof EBDLN in stomach, duodenum, jejunum, ileum and colon was 110.14-fold,56.70-fold,51.23-fold,45.70-fold and 127.23-fold of free EDM respectively. The Pappvalue of EB-DLN was 9.74-fold, 4.48-fold, 3.82-fold and 11.3-fold of that of free EDM. Conclusion EBDLN has sustained effect and can enhance the gastrointestinal absorption of EDM and EBD.关键词
吴茱萸碱/吴茱萸碱丁酰衍生物/固体脂质纳米粒/体外释放/在体胃肠吸收/吸收速率常数/表观渗透系数Key words
evodiamine/evodiamine butyryl deriva-tive/solid lipid nanoparticles/in vitro release/in situ gastrointestinal absorption/absorption rate constant/apparent permeability coefficient分类
医药卫生引用本文复制引用
杨兰,万坤,杨建波,晏声蕾,张奇娆,张景勍,胡雪原..吴茱萸碱丁酰基衍生物固体脂质纳米粒的体外释放及在体胃肠吸收研究[J].中国药理学通报,2018,34(5):724-728,5.基金项目
国家自然科学基金资助项目(No 30973645) （No 30973645）
重庆市研究生科研创新项目资助(No CYS 17172) （No CYS 17172）
重庆医科大学大学生科学研究与创新实验项目(No 201724) （No 201724）
