不同促渗剂对右旋酮洛芬氨丁三醇水凝胶贴剂透皮吸收的影响  

Effect of Different Penetration Enhancers on the Transdermal Permeability of Dexketoprofen Trometamol Hydrogel Patch

作　　者：陈永顺[1] 杨金霞[1] 王启斌[1] CHEN Yongshun;YANG Jjinxia;WANG Qibin(Taihe Hospital·Affiliated Taihe Hospital of Hubei University of Medicine,Shiyan,Hubei,China442000)

机构地区：[1]湖北省十堰市太和医院·湖北医药学院附属太和医院,湖北十堰442200

出　　处：《中国药业》2020年第23期13-17,共5页China Pharmaceuticals

摘　　要：目的探讨不同促渗剂对右旋酮洛芬氨丁三醇(DKT)水凝胶贴剂透皮吸收的影响。方法采用改良Franz扩散池,以高效液相色谱法检测一元促渗剂及多元促渗剂对DKT水凝胶贴剂累积渗透量的影响。比较无促渗剂组和含促渗剂组在比格犬体内的药代动力学(简称药动学)参数,考察其体内促渗效果。结果体外透皮试验中,以4%氮酮联用10%丙二醇的效果最好,其促渗倍率提高至无渗透促进剂的3.22倍。在药动学试验中,含促渗剂组与无促渗剂组的药动学参数0~24 h药时曲线下面积(AUC0→24 h)分别为(26.22±1.17)mg·h/L和(10.56±0.32)mg·h/L,两者比值为2.48。结论4%氮酮联用10%丙二醇的促渗作用最好,可作为DKT水凝胶贴剂的促渗剂。Objective To investigate the effect of penetration enhancers on the transdermal permeability of dexketoprofen(DKT)trometamol hydrogel patch.Methods Modified Franz diffusion cell was used.HPLC method was adopted to detect the effect of a penetration enhancer and multiple penetration enhancers on accumulative permeation quantity of DKT trometamol in the hydrogel patch.The pharmacokinetic parameters in vivo in beagle dogs were compared between the non-penetration enhancer group and the penetration enhancer group,and the transdermal permeability of dexketoprofen trometamol hydrogel patch in vivo was studied.Results In vitro transdermal test showed that 4%azone combined with 10%propylene glycol had the best penetrative effect,and its penetration rate was the 3.22-fold enhancement of the no-penetration enhancer group.In the pharmacokinetic experiment,AUC0→24 hof DKT hydrogel patch included transdermal penetration and without transdermal penetration were(26.22±1.17)mg·h/L and(10.56±0.32)mg·h/L with the ratio of 2.48.Conclusion 4%azone combined with 10%propylene glycol has the best penetrative effect,which can be used as the enhancer for DKT trometamol hydrogel patch.

关 键 词：右旋酮洛芬氨丁三醇 水凝胶贴剂 促渗剂 透皮吸收 药代动力学 

分 类 号：R965[医药卫生—药理学] R971.1[医药卫生—药学]