低分子肝素凝胶处方优化及对瘙痒模型小鼠的作用  

Formula optimization of low molecular weight heparin gel and its effect on the mouse model of pruritus

作　　者：李超[1] 金海蓉[1] 胡晋红[1] 

机构地区：[1]第二军医大学长海医院药学部,上海200433

出　　处：《药学服务与研究》2015年第2期107-110,共4页Pharmaceutical Care and Research

基　　金：国家自然科学基金(81173130)

摘　　要：目的:优化低分子肝素(low molecular weight heparin,LMWH)凝胶处方,并观察其对蛋白酶活化受体2(proteinase activated receptor 2,PAR-2)激动剂SLIGRL-NH2引起小鼠瘙痒的作用。方法:选用L9(34)正交设计,优化LMWH凝胶处方。32只BALB/c小鼠随机分成对照组、模型组、地塞米松乳膏组和LMWH凝胶组,每组8只。分别在脱毛部位给予空白凝胶、空白凝胶、复方醋酸地塞米松乳膏和LMWH凝胶各0.1g,2次/d×3d。最后一次给药后2h,除对照组小鼠用药局部皮内注射生理盐水外,其余3组小鼠皮内注射PAR-2激动剂SLIGRL-NH2。观察皮内注射后30min内小鼠的搔抓次数。结果:最佳处方是LMWH 3%、月桂氮酮5%、卡波姆1.5%。模型组小鼠搔抓次数比对照组显著增多(P<0.01);复方醋酸地塞米松乳膏组小鼠搔抓次数比模型组小鼠显著减少(P<0.05);LMWH凝胶组小鼠搔抓次数比模型组和地塞米松乳胶组小鼠均显著减少(P<0.01)。结论:LMWH凝胶能减轻PAR-2激动剂SLIGRL-NH2引起的瘙痒,其作用可能优于地塞米松乳膏。Objective：To optimize the formula of low molecular weight heparin（LMWH）gel and observe its antipruritic effects in the mouse model of pruritus induced by proteinase activated receptor-2（PAR-2）agonist,SLIGRL-NH2.Methods：L9（34）orthogonal design was used to optimize the formula of LMWH gel.Thirty-two BALB/c mice were randomly divided into the control,model,compound dexamethasone acetate cream（CDAC）and LMWH gel groups,each consisting of 8animals.Blank gel,blank gel,CDAC and LMWH gel at a dosage of 0.1g,twice a day,for 3successive days were applied directly to the skin sites of removed hair,respectively.Two hours after the last dosing,saline solution was intradermally injected in the nape of the control group,and PAR-2agonist SLIGRL-NH2 was given by intradermal injection in the nape of the remaining three groups.The scratching behavior was observed 30 min after intradermal injection.Results：The optimal formula was 3% LMWH,5% azone and 1.5% carbomer.Compared with the control group,the times of scratching significantly increased in the model group（P〈0.01）.The times of scratching decreased in the CDAC group,compared with that of the model group（P〈0.05）.The times of scratching decreased in the LMWH gel group,as compared with those of the model and CDAC groups（P〈0.01）.Conclusion：LMWH gel could relieve pruritus induced by SLIGRL-NH2,with its antipruritic effect being superior to that of CDAC.

关 键 词：低分子肝素凝胶 处方优化 透皮吸收 蛋白酶活化受体2 瘙痒 

分 类 号：R758.3[医药卫生—皮肤病学与性病学] R944.15[医药卫生—临床医学]