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.
作者
陈永顺
杨金霞
王启斌
CHEN Yongshun;YANG Jjinxia;WANG Qibin(Taihe Hospital·Affiliated Taihe Hospital of Hubei University of Medicine,Shiyan,Hubei,China442000)
出处
《中国药业》
CAS
2020年第23期13-17,共5页
China Pharmaceuticals
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
dexketoprofen trometamol
hydrogel patch
penetration enhancer
transdermal penetration
pharmacokinetics
