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盐酸阿夫唑嗪多颗粒药物传递系统的开发和优化。

Development and optimization of multiparticulate drug delivery system of alfuzosin hydrochloride.

机构信息

Shri Neminath Jain Brahmacharyashram's, Shriman Sureshdada Jain College of Pharmacy (PG Course), Neminagar, Chandwad, Dist. Nashik 423 101, Maharashtra, India.

出版信息

Colloids Surf B Biointerfaces. 2013 Feb 1;102:171-7. doi: 10.1016/j.colsurfb.2012.08.035. Epub 2012 Sep 1.

DOI:10.1016/j.colsurfb.2012.08.035
PMID:23010113
Abstract

The purpose of present research was to develop and optimize sustained release floating pellets of alfuzosin hydrochloride which has narrow absorption window in proximal intestine to improve patient compliance and therapeutic efficacy in the treatment of benign prostatic hyperplasia. The system was designed to provide drug loaded pellets coated with three successive coatings over Celphere(®) (microcrystalline cellulose pellets) - drug layer, effervescent layer (HPMC and sodium bicarbonate) and gas entrapped polymeric membrane (Kollicoat(®) SR 30D). A 3(2) factorial design was employed with HPMC:sodium bicarbonate and Kollicoat(®) SR 30D concentration as independent variables while drug release and floating lag time were the dependent variables. Regression analysis was performed to identify best formulation conditions. Scanning electron microscopy was used to study pellet morphology. The floating ability and in vitro drug release of the system were dependent on amount of sodium bicarbonate layered onto pellets and coating level of Kollicoat(®) SR 30D.

摘要

本研究旨在开发和优化盐酸阿夫唑嗪的缓控释漂浮微丸,以改善其在近端肠道狭窄的吸收窗,提高患者顺应性和治疗良性前列腺增生症的疗效。该系统设计为用三层连续包衣(Celphere ® 载药微丸-药物层、泡腾层(HPMC 和碳酸氢钠)和气体包埋聚合物膜(Kollicoat ® SR 30D))对载药微丸进行包衣。采用 3(2) 因子设计,以 HPMC:碳酸氢钠和 Kollicoat ® SR 30D 浓度为自变量,药物释放和漂浮滞后时间为因变量。进行回归分析以确定最佳配方条件。扫描电子显微镜用于研究微丸的形态。该系统的漂浮能力和体外药物释放取决于碳酸氢钠在微丸上的包衣量和 Kollicoat ® SR 30D 的包衣水平。

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