金属阵列微针预处理对盐酸雷莫司琼贴片经皮给药促透作用的研究  

Effect of Metallic Arraymicroneedle Pretreatment on Ramosetron Hydrochloride Paches in Transdermal Drug Delivery

作　　者：夏旭[1] 高文彦[1] 刘筱雅 沈晨[1] 叶金翠[1] XIA Xu;GAO Wen-yan;LIU Xiao-ya;SHEN Chen;YE Jin-cui(Zhejiang Academy of Medical Science,Hangzhou 310007,China)

机构地区：[1]浙江省医学科学院,杭州310007

出　　处：《中国药学杂志》2019年第2期105-109,共5页Chinese Pharmaceutical Journal

基　　金：浙江省科技厅项目资助(2014F10034;2016F50016;2017C33147);浙江省卫生高层次创新人才培养工程项目资助

摘　　要：目的探究金属阵列微针对皮肤的预处理方式对盐酸雷莫司琼贴片经皮给药促透作用的影响。方法自制盐酸雷莫司琼贴片与金属阵列微针(以下简称微针)联合应用,通过析因实验设计,考察微针类型、长度、预处理皮肤的作用力和作用时间4个主要因素对药物经离体豚鼠皮肤渗透的促进作用,并进行了影响因素的主效应和交互效应分析。结果微针长度对微针促透效果的影响最明显,微针长度由200μm提高到300μm,稳态渗透速率以及48 h累积渗透量增加明显。微针处理皮肤的作用力与微针长度对药物经皮促透效果有交互影响,当微针作用时间以及微针类型一定时,微针长度200μm,作用力在3～5 N内变化未对微针的经皮促透效果产生明显影响,微针长度为300μm时,作用力增加对药物促透效果明显。结论提示微针对皮肤的预处理方式对盐酸雷莫司琼经皮渗透效果有重要影响,预处理方式间存在交互效应,本实验为微针辅助经皮给药中的微针预处理方式选择提供参考。OBJECTIVE To evaluate the effects of different pretreatment ways on microneedle onits penetration enhancing effect for ramosetron hydrochloride paches in microneedle-assisted transdermal drug delivery.METHODS Skin penetration experiments were carried out using excised guinea pig skin.Microneedle pretreatment ways including needle type,needle length,needle acting force and acting time were taken as the influencing factors.The main effects and interaction effects of influencing factors in skin penetration enhancement were analyzed.RESULTS Microneedle length had the most significant impact on drug skin penetration.When the length changed from 200μm to 300μm,the steady-state permeation rate and the cumulative permeation amount within 48 h displayed marked increase.Additionally,there was interaction between the penetration enhancing effects of the microneedle length and acting force.When the acting time and needle type were fixed and the microneedle length was 200μm,no significantly different impacts occurred if the acting force varied between 3 and 5 N.However,if the microneedle length was 300μm,the penetration enhancing effects became more significant when increasing acting force from 3 to 5 N.CONCLUSION This studies suggeste that microneedle pretreatment ways may result in different effects on penetration of drugs through skin,and there may exist interaction effect between different microneedle pretreatment ways.This study provides a reference for the selection of microneedle pretreatment in microneedle-assisted transdermal drug delivery.

关 键 词：金属阵列微针 透皮贴片 微针预处理方式 析因设计 

分 类 号：R944.9[医药卫生—药剂学]