格列吡嗪乳胶处方筛选及初步药动-药效学Preparation and pharmacodynamic-pharmacokinetic evaluation of glipizide emulgel
谭喆,方亮,张晶颖
TAN Zhe,FANG Liang,ZHANG Jing-ying(School of Pharmacy
摘要(Abstract):
目的制备格列吡嗪乳胶,考察其体外经皮渗透性及其药动-药效学。方法采用改良Franz扩散池,研究6种不同的有机胺、不同的油相和促进剂对格列吡嗪经皮渗透性的影响,并选择最佳处方进行药动-药效学考察。结果当有机胺为二乙胺和油相为肉豆蔻酸异丙脂且在不含促进剂的条件下,格列吡嗪的药物累积透过量最大;在12 h内,含药质量分数为0.5%和0.125%的乳胶均随着血药浓度的不断上升血糖值下降,但是降糖效果无显著差异(P>0.05)。结论格列吡嗪乳胶降糖作用明显,值得进一步的深入研究,制成一种治疗糖尿病的新剂型。
Objective To prepare glipizide emulgel and evaluate its in vitro transdermal permeability,and observe its pharmacodynamic-pharmacokinetics in vivo.Methods The effects of different organic amines,oils and enhancers on the permeations of glipzide from emulgel through rat skin were investigated using vertical diffusion cells.Results The highest cumulative amount of glipzide was observed when diethylamine(DA)and IPM were added,without enhancer.In 12 h,the blood glucose were decreased with the increase of the drug plasma concentration when the emulgel with glipizide of 0.5% and 0.125% was given,but there were no significant differences between the two dosages in the reduction of the blood glucose level(P>0.05).Conclusions The glipizide emulgel has marked hypoglycemic effect and is worthy for further investigation.
关键词(KeyWords):
格列吡嗪;乳胶剂;经皮吸收;降血糖作用
glipizide;emulgel;skin permeation;hypoglycemic activity
基金项目(Foundation):
作者(Author):
谭喆,方亮,张晶颖
TAN Zhe,FANG Liang,ZHANG Jing-ying(School of Pharmacy
DOI: 10.14066/j.cnki.cn21-1349/r.2010.03.011
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