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胰岛素-壳聚糖制剂的直肠和阴道给药:家兔实验研究

Rectal and vaginal administration of insulin-chitosan formulations: an experimental study in rabbits.

作者信息

Değim Zelihagül, Değim Tuncer, Acartürk Füsun, Erdoğan Deniz, Ozoğul Candan, Köksal Mete

机构信息

Department of Pharmaceutical Technology, Faculty of Pharmacy, Gazi University, 06330-Etiler, Ankara, Turkey.

出版信息

J Drug Target. 2005 Dec;13(10):563-72. doi: 10.1080/10611860500441933.

Abstract

Insulin is a polypeptide drug and it is degraded by gastrointestinal enzymes, therefore, it cannot be used via oral route readily. There are only parenteral forms available in the market. The aim of this study was to investigate the effect of rectal and vaginal administration of various insulin gel formulations on the blood glucose level as alternative routes in rabbits. Chitosan gel (CH-gel) was used as a carrier; the penetration enhancing effect of sodium taurocholate and dimethyl-beta-cyclodextrin (DM-betaCD) was also investigated. CH-gel provided longer insulin release. The maximum decreasing effect on blood glucose level was observed with insulin-CH-gel containing 5% DM-betaCD. In conclusion, our results indicate that insulin may penetrate well through the rectal and vaginal mucosae from the CH-gel. DM-betaCD was also found to be a useful agent to enhance the penetration of insulin through rectal and vaginal membranes.

摘要

胰岛素是一种多肽药物,会被胃肠道酶降解,因此不能轻易通过口服途径使用。市场上只有注射剂型。本研究的目的是探讨在兔身上将各种胰岛素凝胶制剂经直肠和阴道给药作为替代途径对血糖水平的影响。壳聚糖凝胶(CH-凝胶)用作载体;还研究了牛磺胆酸钠和二甲基-β-环糊精(DM-βCD)的促渗透作用。CH-凝胶可实现胰岛素的长效释放。含5% DM-βCD的胰岛素-CH-凝胶对血糖水平的降低作用最大。总之,我们的结果表明,胰岛素可从CH-凝胶中很好地穿透直肠和阴道黏膜。还发现DM-βCD是增强胰岛素穿透直肠和阴道膜的有效制剂。

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