北京中医药大学学报
北京中醫藥大學學報
북경중의약대학학보
JOURNAL OF BEIJING UNIVERSITY OF TRADITIONAL CHINESE MEDICINE
2015年
4期
253-259
,共7页
章烨雯%王琼%于竞新%李辉%康倩%张庆%谭鹏%吴清
章燁雯%王瓊%于競新%李輝%康倩%張慶%譚鵬%吳清
장엽문%왕경%우경신%리휘%강천%장경%담붕%오청
微乳%凝胶膏%星点设计-效应面法%阿魏酸%欧前胡素%体外释放%透皮率
微乳%凝膠膏%星點設計-效應麵法%阿魏痠%歐前鬍素%體外釋放%透皮率
미유%응효고%성점설계-효응면법%아위산%구전호소%체외석방%투피솔
microemulsion%cataplasm%central composite design-response surface design methodology%ferulic acid%imperatorin%release capability in vitro%transdermal permeability
目的:探讨微乳技术对凝胶膏中药物释放及透皮性能的影响。方法以初黏力、180°剥离强度和综合感官评分为指标,结合单因素实验与星点设计-效应面法优选止痛微乳凝胶膏处方。采用改良Franz扩散池法,以有效成分阿魏酸和欧前胡素为指标,对比微乳凝胶膏和普通凝胶膏体外释放和经皮渗透性能。结果最终优选出基质配方为NP700,卡波姆-941,卡波姆-934,铝化合物,酒石酸,丙三醇(1∶0.1∶0.25∶0.04∶0.04∶6)。2种凝胶膏中有效成分的体外释放均符合零级动力学方程,具有扩散和溶蚀的双重机制。微乳凝胶膏和普通凝胶膏中阿魏酸的透皮速率分别为1.92、0.97μg/( h·cm2),欧前胡素的透皮速率分别为0.28、0.09μg/( h·cm2)。与普通凝胶膏相比,微乳凝胶膏中有效成分的累积透过率成倍数增加。结论微乳技术能促进凝胶膏中药物的经皮渗透。
目的:探討微乳技術對凝膠膏中藥物釋放及透皮性能的影響。方法以初黏力、180°剝離彊度和綜閤感官評分為指標,結閤單因素實驗與星點設計-效應麵法優選止痛微乳凝膠膏處方。採用改良Franz擴散池法,以有效成分阿魏痠和歐前鬍素為指標,對比微乳凝膠膏和普通凝膠膏體外釋放和經皮滲透性能。結果最終優選齣基質配方為NP700,卡波姆-941,卡波姆-934,鋁化閤物,酒石痠,丙三醇(1∶0.1∶0.25∶0.04∶0.04∶6)。2種凝膠膏中有效成分的體外釋放均符閤零級動力學方程,具有擴散和溶蝕的雙重機製。微乳凝膠膏和普通凝膠膏中阿魏痠的透皮速率分彆為1.92、0.97μg/( h·cm2),歐前鬍素的透皮速率分彆為0.28、0.09μg/( h·cm2)。與普通凝膠膏相比,微乳凝膠膏中有效成分的纍積透過率成倍數增加。結論微乳技術能促進凝膠膏中藥物的經皮滲透。
목적:탐토미유기술대응효고중약물석방급투피성능적영향。방법이초점력、180°박리강도화종합감관평분위지표,결합단인소실험여성점설계-효응면법우선지통미유응효고처방。채용개량Franz확산지법,이유효성분아위산화구전호소위지표,대비미유응효고화보통응효고체외석방화경피삼투성능。결과최종우선출기질배방위NP700,잡파모-941,잡파모-934,려화합물,주석산,병삼순(1∶0.1∶0.25∶0.04∶0.04∶6)。2충응효고중유효성분적체외석방균부합령급동역학방정,구유확산화용식적쌍중궤제。미유응효고화보통응효고중아위산적투피속솔분별위1.92、0.97μg/( h·cm2),구전호소적투피속솔분별위0.28、0.09μg/( h·cm2)。여보통응효고상비,미유응효고중유효성분적루적투과솔성배수증가。결론미유기술능촉진응효고중약물적경피삼투。
Objective To investigate the influence of microemulsion technology on release capability and transdermal permeability of components in cataplasm. Methods With the initial bonding strength, 180 degree force strength and sensory evaluation scores as indicators, the formula of the analgesic microemul-sion cataplasm matrix was optimized by using single factor experiment combined with central composite de-sign-response surface design methodology. Modified Franz diffusion cell was used to compare the release capability and transdermal permeability between analgesic microemulsion cataplasm ( MEC) and analgesic common cataplasm ( CC) with indicators of ferulic acid and imperatorin. Results Optimized matrix formu-la was NP700, carbomer 941, carbomer 934, aluminum compounds, tartaric acid and glycerin with the rati-o of 1∶0. 1∶0. 25∶0. 04∶0. 04∶6 . The release capability in vitro of ferulic acid and imperatorin in MEC and CC conformed to zero-order kinetic equation with a dual mechanism of diffusion and dissolution. The stead-y-state permeation rate of ferulic acid in MEC was 1. 92 μg/( h·cm2 ) and that in CC was 0. 97 μg/( h· cm2);that of imperatorin in MEC was 0. 28 μg/(h·cm2), while in CC was 0. 09 μg/(h·cm2). Com-pared with CC, the cumulative release rate of effective components multiplied. Conclusion Microemul-sion technology can significantly promote the transdermal permeability of components in cataplasm.