萘丁美酮凝胶中透皮促进剂配方研究  

Study on the formulation of penetration enhancers in nabumetone gel

作　　者：曾明辉[1] 彭颖 邱建平[1] 黄娟[1] 李旭[1] ZENG Ming-hui;PENG Ying;QIU Jian-ping;HUANG Juan;LI Xu(Department of Pharmacy,Medical Center Hospital of Qionglai City,Chengdu 611530,Sichuan,China)

机构地区：[1]邛崃市医疗中心医院药学部,四川成都611530

出　　处：《川北医学院学报》2022年第8期974-977,982,共5页Journal of North Sichuan Medical College

基　　金：四川省成都市医学科研项目(2019120);四川省邛崃市经济科技和信息化局科技项目(qlsjkjkjhm202017)。

摘　　要：目的:评价萘丁美酮凝胶剂中不同配方的透皮促进剂对萘丁美酮经皮渗透性的影响。方法:以卡波姆为凝胶基质,采用析因设计法,选用四种不同配方的透皮促进剂制备萘丁美酮凝胶剂样品;采用Franz皮肤渗透实验装置,以HPLC法测定凝胶剂中萘丁美酮在12 h内的累积渗透量,并计算其稳态流量和渗透系数。结果:5组样品中萘丁美酮在12 h内的累积渗透量分别为291.64、587.33、564.66、709.51及503.94μg/cm^(2),其中透皮促进剂以2.0%氮酮+1.0%川芎挥发油比例配方时,萘丁美酮经皮累积渗透量最高(709.51μg/cm^(2)),稳态流量及渗透系数也均高于其它样品组,且萘丁美酮的渗透过程亦符合Higuchi方程。结论:以卡波姆为凝胶基质时,氮酮与川芎挥发油联用对萘丁美酮透皮特性具有协同增效作用,两者最佳配方浓度为2.0%氮酮+1.0%川芎挥发油。Objective:To optimize the formula of nabumetone gel by studying the effects of different doses of penetration enhancers on the penetration of nabumetone through skin in vitro.Methods:With carbopol as the gel base,the factorial design method was used to choose the optimal formulation of penetration enhancers among four different formulations to prepare nabumetone gels.The release rate of nabumetone in the release media was detected by HPLC with Franz diffusion cells method,and the steady percutaneous speed,the permeability coefficient and the accumulative permeation quantity in 12 h were calculated.Results:The accumulative permeation quantity in 12 h of nabumetone from the nabumetone gels made with the 5 different test groups were 291.64,587.33,564.66,709.51 and 503.94μg/cm^(2),respectively.The gel with 1.0% Chuanxiong aetherolea and 2.0% azone as penetrationenhancers had the maximum value of The accumulative permeation quantity of nabumetone,it was 709.51μg/cm^(2),its penetration process conformed to Higuchi equation,and the steady percutaneous speed and the permeability coefficient were also higher than the other experimental groups.Conclusion:With carbopol as the gel base,Chuanxiong aetherolea and azone have a synergistic effect on the percutaneous penetration of nabumetone gels,and the best formulation is 1.0%Chuanxiong aetherolea and 2.0% azone.

关 键 词：萘丁美酮 卡波姆 氮酮 川芎挥发油 透皮促进剂 透皮吸收 凝胶剂 析因设计 

分 类 号：R944[医药卫生—药剂学]