土槿皮乙酸微乳的制备及体外经皮渗透性研究-天津中草药杂志社.PDF

中草药 Chinese Traditional and Herbal Drugs 第 43 卷 第 4 期 2012 年 4 月 ·683 · 土槿皮乙酸微乳的制备及体外经皮渗透性研究 * 徐 婷，葛淑敏，邓礼荷，韦敏燕，徐月红 ，吴传斌 中山大学药学院，广东 广州 510006 摘 要：目的 制备 O/W 型土槿皮乙酸（PAB ）微乳，并进行体外经皮渗透性能研究。方法 通过绘制伪三元相图确定 PAB 微乳形成的区域，以微乳的体外经皮渗透速率为指标进一步优化筛选 PAB 微乳的处方，并对微乳的外观、形态、粒径分布 等进行表征；以大鼠皮肤为渗透屏障，利用 V-C 扩散池比较了 PAB 微乳和 PAB 过饱和水溶液的体外经皮累积渗透量及皮肤 滞留量。结果 优选的 PAB 微乳处方为 IPM-Cremophor EL-Transcutol P-水（0.2 ∶0.97 ∶1.83 ∶7 ），所制备的微乳澄清透明， 透射电镜（TEM ）观察结果为均匀的球形或近球形，平均粒径为（18.7±1.9）nm 。PAB 微乳与 PAB 过饱和水溶液 24 h 累 积渗透量分别为（50.31 ±4.63 ）、（6.27 ±1.33）μg/cm2 2 ，皮肤滞留量分别为（6.28 ±0.31 ）、（0.51 ±0.13 ）μg/cm ，差异均具 有显著性（P ＜0.05 ）。结论 PAB 微乳新型给药系统可有效促进 PAB 的经皮渗透及提高其皮肤滞留量，为PAB 皮肤给药抗 真菌新制剂的设计提供了实验基础。 关键词：土槿皮乙酸；微乳；伪三元相图；经皮渗透；皮肤滞留 中图分类号：R283.6 ；286.02 文献标志码：A 文章编号：0253 - 2670(2012)04 - 0683 - 07 Preparation of pseudolaric acid B microemulsion and its transdermal penetration XU Ting, GE Shu-min, DENG Li-he, WEI Min-yan, XU Yue-hong, WU Chuan-bin School of Pharmaceutical Sciences, Sun Yat-sen University, Guangzhou 510006, China Abstract: Objective To prepare O/W microemulsion formulation containing pseudolaric acid B (PAB) and investigate its transdermal delivery ability in vitro. Methods Pseudo-ternary phase diagrams were drawn to obtain the area of PAB microemulsion, and PAB microemulsion formulations were further optimized by the rate of transdermal permeation. The microemulsion properties including appearance, form, and particle size distribution were examined. Taking rat skin as permeability barrier, the cumulative permeation amount in 24 h and retention amount of PAB in skin were determined in vitro using V-C diffusion cell fitted with rat skin. Comparison was made between the PAB microemulsion and