格列美脲水凝胶剂体内外透皮释放的评价  

Drug release evaluation of glimepiride hydrogel in vitro and in vivo

作　　者：杨文智[1] 李霞霞[1] 王树根[1] 李海鹰[1] 

机构地区：[1]河北大学药学院,河北保定071002

出　　处：《河北大学学报（自然科学版）》2015年第6期599-604,共6页Journal of Hebei University(Natural Science Edition)

基　　金：河北省自然科学基金资助项目(H2012201069;H2016201044);河北省科技计划项目(13272705)

摘　　要：采用HPLC法检测自制格列美脲水凝胶的药物含量,研究凝胶中药物的体内外透皮释放.选用小鼠鼠皮,采用Franz立式扩散仪考察水凝胶中药物的体外释放,药物体外释放接近零级释放.选用新西兰兔背敷凝胶,测定兔体内格列美脲的药-时曲线.考察超声按摩兔皮后涂敷等量药物水凝胶,药物经皮渗透的变化.药代动力学研究结果表明:对照组血药质量浓度12h达峰,ρ_(max)为7.64μg/mL,持续释药长达48h.而兔皮超声后t_(max)提前至6h,药物起效迅速.格列美脲水凝胶体内外释放呈相关性,即可通过体外释放状况预测药物体内吸收.In order to study and evaluate the release behavior of glimepiride（GM）hydrogel in vitro and in vivo,an HPLC method was used to determine the drug concentration in the hydrogel.The in vitro transdermal permeation behaviors of GM through mice skin were studied using Franz-type diffusion cell.The results showed that the drug released from hydrogel fitted with zero-order kinetic characteristics.A pharmacokinetic study of glimepiride hydrogel was carried out using New Zealand rabbits,and compared with the ultrasonic wave processing rabbit skin.It demonstrated that in the control group,the hydrogel could sustain release glimepiride for 48 h,and plasma drug mass concentration reached a peak（ρ_（max）,7.64μg/mL）after 12 h.After an ultrasonic pretreatment,there was an earlier t_（max）at 6h.It was evident that ultrasonic could promote drug permeation.There was a good correlation between in vitro skin permeation and in vivo transdermal absorption using hydrogel,and the GM release in vitro could well predict its absorption in vivo.

关 键 词：格列美脲 水凝胶 超声 体内外释放 透皮吸收 

分 类 号：O658[理学—分析化学]