格列本脲乳胶剂的制备及初步药效学

目的制备格列本脲乳胶剂,并观察其对正常大鼠的降血糖作用。方法采用改进的Franz扩散池,考察不同浓度二乙胺、不同有机胺和促进剂对格列本脲透皮吸收的影响,并评价优选处方对正常大鼠的降血糖作用。结果当二乙胺和氮酮的质量分数分别为0.70%和3%时,格列本脲乳胶剂的稳态渗透速率最高,并且能显著降低正常大鼠空腹血糖(P<0.01)。结论格列本脲乳胶剂的降血糖作用显著,有望成为一种治疗糖尿病的新型制剂。

Preparation and pharmacodynamic evaluation of glibenclamide emulgel in rats

Objective To prepare glibenclamide emulgel and observe its hypoglycemic effect in normal rats.Methods The effects of different concentrations of diethylamine on the permeation of glibenclamide from emulgel through rat skin were investigated using vertical diffusion cells.The influences of various organic amines and penetration enhancers on the permeation of glibenclamide from emulgel were also investigated.In addition,the glibenclamide emulgel was evaluated for its hypoglycemic activity in normal rats.Results The highest steady-state flux was observed when 0.70% diethylamine and 3% azone were added.The glibenclamide emulgel produced a significant reduction in blood glucose levels compared to the control(P<0.01).Conclusions The glibenclamide emulgel has significant hypoglycemic effect,so it may be a promising candidate for the treatment of diabetes.