黄芩苷外用温敏凝胶的处方设计及优化

Optimization and Evaluation of Baicalin Thermosensitive Gels for External Application

目的:通过不同数学模型及评价指标优选黄芩苷外用温敏凝胶的处方。方法:以泊洛沙姆407,188为凝胶基质,以胶凝温度为指标比较全样本多元线性模型及星点设计-效应面法优选的黄芩苷外用温敏凝胶处方。以胶凝时间及凝胶长度为评价指标进行处方优化。结果:星点设计-效应面法优选的处方置信度较高。黄芩苷外用温敏凝胶的最优处方为1%黄芩苷,17%泊洛沙姆407和1.5%泊洛沙姆188;胶凝温度、胶凝时间及凝胶长度分别为(30.3±0.1)℃,(18.9±1.9)s,(0.7±0.6)cm。结论:制备的黄芩苷外用温敏凝胶符合局部迅速富集、提高患者顺应性的要求,指标评价应以人体测定的结果为准,为外用温敏凝胶的处方优选提供参考。

Objective： To prepare baicalin thermosensitive gels for external application through different mathematical models and evaluation indexes. Method： Taking poloxamer 407 （P407） and poloxamer 188 （P188） as gel matrices, gelation temperature was applied as a target to compare formulations of baicalin thermosensitive gels, which were optimized by all sample multiple linear regression model and central composite design-response surface methodology （CCD-RSM） , while combination of gelation time and length were adopted to optimize formulation. Result： Counting on high reliability of CCD-RSM. Gels formulation was finally confirmed as 1% baicalin, 17% P407 and 1.5% P188; gelation temperature, time and length were （30.3 ± 0.1） ℃, （18.9 ± 1.9 ） s, （ 0. 7 ± 0. 6 ） cm, respectively. Conclusion： Baiealin thermosensitive gels for external application is consistent with external requests for rapid enrichment at the local and elevated compliance, index evaluation should he based on results of human determination, references are offered to filter prescriptions of external thermosensitive gels scientifically and reasonably.