摘要
目的:基于AHP-CRITIC法赋权的D-最优混料设计优化欧前胡素和5-氟尿嘧啶共载乳膏的制备处方,并考察共载乳膏的体外透皮特性。方法:在预试验的基础上,以稳定性、外观性状及延展性为考察指标。以AHP-CRITIC混合加权法确定各指标的权重并计算综合得分作为评价指标。采用D-最优混料设计法优化欧前胡素和5-氟尿嘧啶共载乳膏基质处方,并进行验证。采用改良Franz扩散池法探究共载乳膏体外透皮特性。结果:按照AHP-CRITIC混合加权法得到稳定性、外观性状及延展性3个指标的权重分别为0.6457、0.2132及0.1411。确定最优处方制备方法并通过验证。体外透皮结果显示,共载乳膏中欧前胡素24 h累积透过量52.95μg,累积透过百分比14.69%,稳态速率为2.48μg·(cm^(2)·h)^(-1),5-氟尿嘧啶24 h累积透过量为261.24μg,累积透过百分比61.35%,稳态速率为11.94μg·(cm^(2)·h)^(-1)。结论:欧前胡素和5-氟尿嘧啶共载乳膏剂具有膏体均匀,稠度适宜及易涂布等特性,具有良好的体外释放和透皮性能,是一种优良的皮肤科外用制剂。
Objective:The preparation formula for imperatorin and 5-fluorouracil co-loaded cream was optimized using the D-optimal mixture design empowered by the AHP-CRITIC method,The in vitro transdermal properties of the co-loaded cream were investigated,Methods:Based on preliminary tests,stability,appearance properties,and ductility were used as inspection indicators,The AHP-CRITIC hybrid weighting method was used to determine the weight of each indicator and calculate the comprehensive score as the evaluation indicator,The D-optimal mixture design method was used to optimize the formulation of the cream matrix co-loaded with imperatorin and 5-fluorouracil and was verified,The study employed the modified Franz diffusion cell method to investigate the in vitro transdermal properties of the co-loaded cream,Results:According to the AHP-CRITIC hybrid weighting method,the weights of the three indicators of stability,appearance properties and ductility were 0.6457,0.2132 and0.1411 respectively.The optimal formulation preparation method was determined and validated,In vitro transdermal results showed that the 24 h cumulative penetration of imperatorin in the co-loaded cream was 52.95μg,with the cumulative penetration percentage of 14.69%and the steady-state rate 2.48μg·(cm^(2)·h)^(-1),The 24 h cumulative penetration of fluorouracil was 261.24μg,with the cumulative transmission percentage of 61.35%,and the steady-state rate 11.94μg·(cm^(2)·h)^(-1),Conclusion:The cream containing imperatorin and 5-fluorouracil is a uniform paste with a suitable consistency for easy coating,It exhibits good in vitro release and transdermal properties,making it an excellent external dermatological preparation,
作者
钟文潇
袁明昊
王雨露
郭力
ZHONG Wenxiao;YUAN Minghao;WANG Yulu;GUO Li(School of Pharmacy,Chengdu University Traditional Chinese Medicine,Chengdu 611137,Sichuan)
出处
《中药与临床》
2024年第6期25-30,共6页
Pharmacy and Clinics of Chinese Materia Medica
基金
四川省科技基础条件平台项目(2019JDPT0032)
“杏林学者”学科人才科研提升计划(CXTD2018012)。
关键词
欧前胡素
5-氟尿嘧啶
乳膏
处方优化
透皮吸收
Imperatorin
5-fluorouracil
cream
prescription optimization
transdermal absorption
