电致孔技术促进瑞格列奈水凝胶经皮吸收

Preparation of repaglinide hydrogel and evaluation of its transdermal release of drug in vitro and in vivo

应用自制瑞格列奈-精氨酸复合物制备瑞格列奈水凝胶.采用Franz立式扩散池和小鼠离体皮肤,考察瑞格列奈水凝胶体外释放,其释放符合零级方程.利用HPLC法测定兔体内血药浓度,药物动力学数据表明,电致孔组兔血药浓度达峰时间缩短2 h,而药物经皮渗透量为正常组的1.8倍.相比兔皮肤直接涂敷药物水凝胶,兔皮电致孔处理后给予等剂量药物水凝胶,可促进水凝胶中药物经皮渗透.此外,瑞格列奈水凝胶的药物释放具备良好的体内外相关性.

The repaglinide hydrogel was prepared by repaglinide-arginine complex.The drug release from hydrogel through isolated skin of mice was investigated by using Franz diffusion cell in vitro.The drug release of hydrogel followed to the zero-order equation.The plasma concentration in rabbits was determined by HPLC.The pharmacokinetic data showed that the time to peak of plasma concentration in the electroporation group was shortened by 2 h,and the amount of drug through percutaneous penetration was 1.8 times of that in the normal group.Compared with repaglinide hydrogel coated with skin directly,rabbit skin using electroporation treatment and then coated with equal dose of drug hydrogel can promote the transdermal penetration of drugs.In addition,the drug release of repaglinide hydrogel showed a good correlation in vitro and in vivo.