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在体微透析技术研究低相对分子质量肝素凝胶经皮给药大鼠体内药动学特征
  • ISSN号:1001-2494
  • 期刊名称:《中国药学杂志》
  • 时间:0
  • 分类:R758.3[医药卫生—皮肤病学与性病学;医药卫生—临床医学] R944.15[医药卫生—药剂学;医药卫生—药学]
  • 作者机构:[1]第二军医大学长海医院药学部,上海200433
  • 相关基金:国家自然科学基金(81173130)
中文摘要:

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。

英文摘要:

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.

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期刊信息
  • 《中国药学杂志》
  • 中国科技核心期刊
  • 主管单位:中国科学技术协会
  • 主办单位:中国药学会
  • 主编:桑国卫
  • 地址:北京市朝阳区建外大街四号建外SOHO九号楼18层
  • 邮编:100022
  • 邮箱:zgyxzz@cpa.org.cn
  • 电话:010-58698009
  • 国际标准刊号:ISSN:1001-2494
  • 国内统一刊号:ISSN:11-2162/R
  • 邮发代号:2-232
  • 获奖情况:
  • 首届国家期刊奖,第一、二届全国优秀科技期刊一等奖,中国期刊方阵“双高”期刊
  • 国内外数据库收录:
  • 美国国际药学文摘,美国化学文摘(网络版),荷兰文摘与引文数据库,荷兰医学文摘,日本日本科学技术振兴机构数据库,中国中国科技核心期刊,中国北大核心期刊(2004版),中国北大核心期刊(2008版),中国北大核心期刊(2011版),中国北大核心期刊(2014版),英国英国皇家化学学会文摘,中国北大核心期刊(2000版)
  • 被引量:54982