右哌甲酯贴剂体外透皮特性的考察  

Investigation of in vitro Characterization of Demethyphenidate Transdermal Patches

作　　者：张成豪[1] 罗华菲[1] 林国钡[1] 武余波[1] 王浩[1] 

机构地区：[1]中国医药工业研究总院药物制剂国家工程研究中心,上海201203

出　　处：《中国医药工业杂志》2016年第4期424-429,共6页Chinese Journal of Pharmaceuticals

基　　金：国家"重大新药创制"科技重大专项(2014ZX09507006-002)

摘　　要：建立了HPLC法测定体外透皮接收液中的右哌甲酯浓度。分别考察了右哌甲酯在不同p H值介质中的稳定性和饱和溶解度。结果表明,以p H 4.5磷酸盐缓冲液为接收介质时,右哌甲酯在48 h内仅降解0.17%,且满足漏槽条件。进一步考察了不同种属皮肤和不同种类促透剂对贴剂中右哌甲酯体外透皮特性的影响。结果表明,使用大鼠和裸鼠皮肤为屏障时,9 h已有70%的药物透过,因此选用最难透过的巴马香猪皮肤;1,3-丙二醇、油酸、月桂氮酮、聚乙二醇400和N-甲基吡咯烷酮在5%浓度下均能略增强右哌甲酯的渗透性,但均无显著差异(P>0.05),而薄荷醇呈现出阻碍右哌甲酯渗透的作用。An HPLC method was established to determine the concentration of demethyphenidate in the receive liquid. The stability and saturation solubility of demethyphenidate in media with different p H values were investigated. The results showed that the degradation rate of demethyphenidate in p H 4.5 phosphate buffer was only 0.17% within 48 h and this medium could also maintain the sink conditions based on the results of solubility test. The effects of skin species and enhancer types on in vitro permeation behavior of demethyphenidate from the patches were further investigated. The results showed that the cumulative amount of demethyphenidate were both over 70% within 9 h with SD rat skin and nude mice skin as barriers. So, Bama miniature pig skin was chosen as the barrier because of its poor permeation. With 1,3-propanediol, oleic acid, azone, polyethylene glycol 400 or N-methylpyrrolidone as a enhancer at concentration of 5%, the cumulative amount of demethyphenidate were all slightly improved（P0.05）, while menthol at the same concentration obstruct the permeation of demethyphenidate.

关 键 词：右哌甲酯 透皮贴剂 体外透皮 促透剂 

分 类 号：R944.9[医药卫生—药剂学]