通窍散瘀方微乳的制备及评价

Preparation and evaluation of Tongqiao Sanyu microemulsion

关键词:  通窍散瘀方  微乳  伪三元相图  刺激性  载药量

Key words:  Tongqiao Sanyu prescription  microemulsion  pseudo-ternary phase diagram  irritation  drug loading

摘要:

[目的] 该实验制备通窍散瘀方微乳，并对其含量、理化性质、刺激性进行评价。[方法] 实验以葛根素溶解度为指标，筛选出合适的乳化剂、助乳化剂、油相。再通过伪三元相图，优化微乳处方。[结果] 得到制剂处方为EL35，2丙二醇-IPM-水，四者比例为29.23∶29.23∶5.18∶36.34（W∶W∶W∶W）。得到的O/W型微乳，外观澄清透明，PH均值约为5.31。透射电镜下观察，圆整、均匀。激光粒径测定仪测定平均粒径约为17.86 nm，Zeta电位约为-4.90。葛根素载药量约为：68.64 mg/g，芍药苷载药量约为26.96 mg/g。通过大鼠鼻中隔切片，研究通窍散瘀微乳和通窍散瘀溶液对鼻黏膜的刺激性、损伤性作用及可逆性。[结论] 结果显示通窍散瘀微乳能显著提高难溶性药物葛根素的载药量，并且形成均一稳定的体系。可为通窍散瘀方给药提供新的剂型。微乳的刺激性小于溶液，且微乳损伤是可逆的。

Abstract:

[Objective] The experiment is to prepare Tongqiao Sanyu microemulsion, and investigate its content, physical,chemical properties and irritation.[Methods] Use the solubility of puerarin as an index, investigate the appropriate emulsifier, co-emulsifier and oil phase. And then through the pseudo ternary phase diagram, optimize the microemulsion prescription.[Results] The formulation is EL35-1, 2-propanediol-IPM-water, and the ratio is 29.23:29.23:5.18:36.34 (W:W:W:W). System of Tongqiao Sanyu microemulsion for the O/W microemulsion, the appearance of clear and transparent, The pH is 5.31. Placed under the transmission electron microscope observation, round, uniform.. The average particle size was 17.86 nm and the zeta potential was -4.90 by laser particle size analyzer. The dose of Puerarin was 68.64 mg/g, and paeoniflorin was 26.96 mg/g.Toad palate cilia irritation test results show that the drug suspension and microemulsion preparations are certain irritation.[Conclusion] Results show that Tongqiao Sanyu microemulsion can significantly improve the insoluble drug puerarin drug loading, and the formation of uniform and stable system. Tongqiao Sanyu microemulsion can provide a new dosage form for Tongqiao Shuyu recipe. The irritation of microemulsion is less than that of the solution, and the damage of microemulsion is reversible