传明酸传递体的制备及其性质考察-天津中草药杂志社.pdfVIP

中草药 Chinese Traditional and Herbal Drugs 第 44 卷 第 22 期 2013 年 11 月 ·3141 · 传明酸传递体的制备及其性质考察 李莎莎，宋艳丽，危红华，张朵朵，吴艳丽，郝保华* 西北大学生命科学学院，陕西 西安 710069 摘 要：目的 采用星点设计-效应面法优化传明酸传递体的处方。方法 逆向旋蒸法制备传明酸传递体；通过考察膜材比、 脂药比及脱氧胆酸钠用量对包封率、载药量的影响，并对结果进行二项式方程拟合，用效应面法预测最佳处方，并对其稳定 性进行研究。结果 确定最优处方为膜材比 2 ∶1、脂药比 6 ∶1、脱氧胆酸钠用量为 20 mg ；以该处方制备所得传明酸传递 体的包封率为（81.28 ±1.06）%、载药量为（4.67 ±0.28 ）%、平均粒径为（105.3±7.2 ）nm 、Zeta 电位为（−38.5 ±2.3 ）mV ， 且实测值与预测值的偏差较小。结论 星点设计-效应面优化法筛选传明酸传递体是一种简便、可行的实验设计方法。 关键词：传明酸；传递体；星点设计；效应面法；制备工艺 中图分类号：R283.6 文献标志码：A 文章编号：0253 - 2670(2013)22 - 3141 - 06 DOI: 10.7501/j.issn.0253-2670.2013.22.010 Preparation of tranexamic acid transfersomes and investigation on their characteristics LI Sha-sha, SONG Yan-li, WEI Hong-hua, ZHANG Duo-duo, WU Yan-li, HAO Bao-hua College of Life Science, Northwest University, Xi’an 710069, China Abstract: Objective To optimize the formulation and prepration of tranexamic acid (TA) transfersomes by central composite design-response surface method. Methods The transfersomes were prepared using the reverse rotary evaporation method. The effects of phosphatidylcholine (SPC)-cholesterol (CH) ratio, SPC-drug ratio, and the concentration of sodium deoxycholic acid on the entrapment efficiency (EE) were investigated, the results were fitted with binomial equation, and the optimal formulation was predicted by response surface method. Results The preparation conditions were optimized as SPC-CH (2 ∶1), SPC-drug (6 ∶1), and the concentration of sodium deoxycholic acid 20 mg. Under these conditions, the evaluated EE, drug-loading, average partical size, and Zeta potential of TA transfersomes were (81.28 ± 1.06)%, (4.67 ± 0.28)%, (105.3 ± 7.2) nm, and (−38.5 ± 2.3) mV. The deviation of measured and predicated values was smaller. Conclusion The central composite design-response surface method is appl