天然产物研究与开发 ›› 2017, Vol. 29 ›› Issue (5): 856-861.doi: 10.16333/j.1001-6880.2017.5.024

• 开发研究 • 上一篇    下一篇

正交实验优化川陈皮素微乳凝胶剂促渗剂及体外释药评价

袁旭1,刘新2,郝旺青1,高倩2,林於1*   

  1. 1 重庆医科大学中医药学院;2重庆医科大学药学院,重庆 400016
  • 出版日期:2017-05-31 发布日期:2017-06-09

Optimization of Penetration Enhancer of Nabiletin Micromulision Gel by Orthogonal Test and Evaluation of Drug Release in vitro

YUAN Xu1,LIU Xin2,HAO Wang-qing1,GAO Qian2,LIN Yu1*   

  1. 1 Chinese Medicine Department; 2 Pharmacy Department,Chongqing Medical University,Chongqing 400016,China
  • Online:2017-05-31 Published:2017-06-09

摘要: 本文筛选了川陈皮素微乳凝胶剂的最佳透皮促渗剂并考察了其体外释药机制。采用正交实验设计,对离体家兔鼻粘膜进行体外渗透实验,以川陈皮素的累积渗透量及渗透速率常数为指标,优选最佳处方;采用扩散池法对川陈皮素微乳凝胶剂进行体外释药研究,并用无膜溶出法考察其释药机制。结果表明,不同促渗剂对川陈皮素的累积渗透量及渗透速率常数影响大小为:氮酮>冰片>丙二醇,且氮酮具有显著性差异(P<0.05),微乳凝胶剂12 h的累积释药率为86%,符合Higuchi方程,其溶蚀量较少且与释药率无明显线性相关(r=0.9387)。可见,2%氮酮、2%冰片和1%丙二醇可作为最佳促渗剂处方在川陈皮素微乳凝胶剂中使用,且该制剂体外释药性能良好,有一定的缓释特性。

关键词: 川陈皮素, 微乳凝胶剂, 正交实验, 促渗剂

Abstract: The penetration enhancer of nabiletin micromulision gel was optimized and its drug release mechanism in vitro was studied. Orthogonal design was employed to transdermal diffusion test in nasal mucosa of rabbits in vitro, the cumulative permeation quantity and permeation rate of nabiletin were used as indexes to optimize the prescription;Behavior of drug release was studied by modifying diffusion cell and mechanism of drug release was studied by membrane-less model. The results showed that the influence order of different penetration enhancers on cumulative permeation quantity and permeation rate of nabiletin were as follows:azone > borneol > propanediol,while azone had significant influence(P<0.05),and the cumulative release rate of microemulsion gel in 12 hours was 86% which followed the Higuchi equation,erosion rate of microemulsion gel was low and not linearly correlated with the drug release rate(r=0.9387). It was evidently that the prescription of 2% azone,2% borneol and 1% propanediol can be used as the compound penetration enhancer,it had a good property of drug release in vitro and showed controlled release property.

Key words: nobiletin, microemulsion gel, orthogonal test, penetration enhancer