摘要
目的:考察羟丙基-β-环糊精(HP-β-CD)在辣椒碱凝胶剂中作为增溶剂和促渗剂的作用。方法:以相溶解度法考察辣椒碱与HP-β-CD的相互作用。制备含HP-β-CD的辣椒碱凝胶剂和含月桂氮酮、乙醇的凝胶剂,并以上市辣椒碱软膏Zostrix为阳性对照,分别比较其经皮渗透率、镇痛作用、抗炎作用以及对皮肤的刺激性。结果:辣椒碱与HP-β-CD包合的表观稳定性常数为1 061.7 L/mol;与Zostrix软膏和含月桂氮酮、乙醇的凝胶相比,HP-β-CD使辣椒碱的透皮吸收显著提高(P<0.01);抗炎、镇痛的效果依次为含HP-β-CD凝胶≈Zostrix软膏>月桂氮酮乙醇凝胶。皮肤刺激性实验结果为月桂氮酮乙醇凝胶>HP-β-CD凝胶≈Zostrix软膏。结论:HP-β-CD能与辣椒碱发生较强相互作用,在辣椒碱凝胶中作为增溶剂和促渗剂,可以显著促进辣椒碱的皮肤渗透性,提高辣椒碱的抗炎、镇痛效果,且不会对家兔的完整皮肤产生刺激性。
Objective：To investigate the role of hydroxypropyl-β-cyclodextrin（HP-β-CD） as solubilizer and penetration enhancer in capsaicin hydrogel.Methods：Phase-solubility technique was used to study the interaction of capsaicin and HP-β-CD.Capsaicin hydrogels were prepared with HP-β-CD,azone and ethanol as solubilizer and penetration enhancer,respectively,and then the in vitro percutaneous penetration behavior,anti-inflammatory effect,analgesic effect and skin irritation of these formulations were examined.Results：The apparent stability constant（Ks） of capsaicin and HP-β-CD was 1 061.7 L/tool. Percutane-ous absorption of capsaicin hydrogel with HP-β-CD as enhancer was increased significantly compared with that of Zostrix cream and hydrogel prepared with azone and ethanol （P〈0.01）. The results of anti-inflammatory and analgesic tests showed similar tendency： HP-β-CD gel≈Zostrix cream〉azone and ethanol gel, while the order of skin irritation was azone and ethanol gel〉 HP-β-CD gel≈Zostrix cream. Conclusion：As a solubilizer and penetration enhancer, HP-β-CD can interact with capsaicin strong ly,promote the percutaneous penetration and improve the anti-inflammatory and analgesic effects of capsaicin with little irritation to intact skin of rabbit.
出处
《药学服务与研究》
CAS
CSCD
2009年第5期363-366,共4页
Pharmaceutical Care and Research
关键词
辣椒碱
羟丙基-Β-环糊精
经皮吸收
凝胶类
capsaicin
hydroxypropyl-β-cyclodextrin
percutaneous penetration
gels
