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[摘要]
目的 优化三七跌打软膏剂基质处方并对其体外透皮特性进行研究。方法 在预试验的基础上,采用Box-Behnken法,以外观性状、高温实验、低温实验、离心实验评分为指标优化三七跌打软膏基质最优处方,采用改良Franz扩散池法,以血竭素、人参皂苷Rg1、川续断皂苷VI、人参皂苷Rb1为评价指标,考察不同薄荷醇促渗剂对软膏体外透皮渗透量的影响。结果 三七跌打软膏最优处方为十二烷基硫酸钠-硬脂醇-凡士林(1.61:26.72:27.10);不同浓度的促渗剂对血竭素、人参皂苷Rg1、川续断皂苷VI、人参皂苷Rb1促渗效果均较好,3%的促渗剂对指标成分促渗效果及制剂稳定性较好,体外透皮速率依次为3.971、6.368、0.415、2.780 μg/(cm2∙h)。结论 优化的三七跌打软膏剂膏体均匀,稠度适宜,易涂布,具有较好的释药性和透皮性,透皮行为符合零级动力学过程。
[Key word]
[Abstract]
Objective To prepare Sanqi Traumatic Ointment (STO) and study its transdermal permeation properties in vitro. Methods In this paper, the appearance description, high-temperature test, low-temperature test and centrifugal test were taken as indexes. Based on the result of a single factor experiment, the formula for the STO was optimized by Box-Behnken test. Franz diffusing cells method was chosen to investigate the tansdermal infiltration capacity of ointment with different mentha camphor penetration enhancers' in vitro, taking dracorhodin, ginsenoside Rg1, asperosaponi VI, and ginsenoside Rb1 as index components. Results The optimal ratio of the prescription was as follows:lauryl sodium sulfate-stearyl alcohol-vaseline (1.61:26.72:27.10). The promoting effect of different concentration of penetration enhancers on dracorhodin, ginsenoside Rg1, ginsenoside VI, and asperosaponin Rb1 penetration were better; The promoting effect of 3% concentration for index component was better, and this preparation had good stability; The transdermal rates of dracorhodin, ginsenoside Rg1, asperosaponi VI, and ginsenoside Rb1 were 3.971, 6.368, 0.415, and 2.780 μg/(cm2∙h). Conclusion STO had a good release and transdermal properties, and transdermal actions were consistent with zero-order kinetics.
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[基金项目]
重庆市科委应用开发重大项目(cstc2014yykfC10006)