乳状溶剂蒸发法制备格列本脲缓释微球及评价

Rashmi R Kokardekar, Yogesh S. Chaudhari, Suresh D. Kumavat, H. Pawar
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引用次数: 13

摘要

口服格列本脲似乎通过刺激胰腺胰岛素的释放而急剧降低血糖。格列本脲在人体内的胃肠道吸收均匀、快速且基本完全,单次口服后1-3小时血药浓度达到峰值,正常受试者的半衰期为3小时。本研究的目的是用乳液-溶剂蒸发法制备格列本脲微球并对其进行评价。以乙基纤维素N100为原料制备了微球,并对其微球性能、粒径和包封效率进行了表征。体外释放研究采用pH 1.2 (0.1N HCL)缓冲液进行,显示药物持续释放达24小时。SEM研究表明,微球呈球形,具有多孔性。在健康家兔身上进行了体内研究,以分析微球的漂浮效率。成功制备了格列本脲微球,可以帮助更好地控制II型糖尿病的并发症。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
Development and Evaluation of Sustained Release Microspheres of Glibenclamide by Emulsion Solvent Evaporation Method
Oral administration of Glibenclamide appears to lower the blood glucose acutely by stimulating the release of insulin from the pancreas. Gastro intestinal absorption of Glibenclamide in man is uniform, rapid and essentially complete having peak plasma concentration 1-3 hours after single oral dose and half-life of elimination three hours in normal subjects. The objective of the present investigation was to formulate and evaluate microspheres of Glibenclamide by emulsion – solvent evaporation method. Microspheres were prepared using Ethyl Cellulose N100 and characterized for their micromeritic properties, particle size and encapsulation efficiency. The in-vitro release studies were performed using pH 1.2 (0.1N HCL) buffer revealed that the drug release was sustained up to 24 hours. SEM studies showed that the microspheres were spherical and porous in nature. In-vivo studies were performed in healthy rabbits to analyze the floating efficiency of microspheres. Microspheres of glibenclamide were prepared successfully and could help to manage better the complications involved in Type II diabetes.
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