Preparation and in vitro evaluation of Eudragit microspheres containing acetazolamide

Preparation and in vitro evaluation of Eudragit microspheres containing acetazolamide
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DOI:
10.1016/j.ijpharm.2003.09.015
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发表时间:
2004-01-09
影响因子:
5.8
通讯作者:
Dortunç, B
Dortunç, B
中科院分区:
医学2区
文献类型:
--
作者:
Haznedar, S;Dortunç, B

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本研究的目的是制备和评价乙酰唑胺丙烯酸树脂(RS和RL)微球。以丙酮/液体石蜡为溶剂,采用溶剂挥发法制备微球。考察了搅拌速度、聚合物与药物比例、聚合物类型、聚合物组合比例等因素对微球粒径、包封率和体外释放特性的影响。所有处方的微球制备收率和包封率均较高。通过改变聚合物:药物比例或系统的搅拌速度来改变平均粒径。尽管乙酰唑胺从Eudragit RS微球的释放速率对于所有制剂都非常缓慢且不完全,但它们从Eudragit RL微球的释放速率很快。当将Eudragit RS加入到Eudragit RL微球制剂中时,释放速率减慢并实现适合于口服给药的释放曲线。(C)2003 Elsevier B.V保留所有权利。
The aim of this study was to prepare and evaluate Eudragit (RS and RL) microspheres containing acetazolamide. Microspheres were prepared by solvent evaporation method using acetone/liquid paraffin system. The influence of formulation factors (stirring speed, polymer:drug ratio, type of polymer, ratio of the combination of polymers) on particle size, encapsulation efficiency and in vitro release characteristics of the microspheres were investigated. The yields of preparation and the encapsulation efficiencies were high for all formulations the microspheres were obtained. Mean particle size changed by changing the polymer:drug ratio or the stirring speed of the system. Although acetazolamide release rates from Eudragit RS microspheres were very slow and incomplete for all formulations, they were fast from Eudragit RL microspheres. When Eudragit RS was added to Eudragit RL microsphere formulations, release rates slowed down and achieved the release profile suitable for peroral administration. (C) 2003 Elsevier B.V All rights reserved.