阿奇霉素固体分散片的制备及溶解法体外、体内表征

Pawan Kumar, R. Mazumder
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引用次数: 1

摘要

http://dx.doi.org/10.21276/IJRDPL.227 8-0238.2017.6(5)。摘要:阿奇霉素是一种环状结构的大环内酯类药物,具有持久的抗菌、抗炎和免疫调节作用。阿奇霉素属于BCSⅱ类药物,即溶解度差、渗透性好的药物。这种药物的主要问题是它在生物液体中的溶解度很差,导致口服给药后的生物利用度很差。本研究的目的是研制提高难溶性阿奇霉素溶出度的制剂。以PEG 6000为载体,采用熔融法制备了阿奇霉素固体分散体。采用固体分散制剂配制片剂,并与不含载体的纯药物配制片剂进行比较。体外溶出率明显提高,并与动物体内溶出率进行了比较。药物的溶解增强是由药物的结晶性质转变为无定形性质引起的。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
Preparation and in vitro and in vivocharacterization of Solid Dispersions tablets of Azithromycin by melting method
http://dx.doi.org/10.21276/IJRDPL.227 8-0238.2017.6(5).2769-2772 ABSTRACT:Azithromycin is a cyclic-structure macrolide, shows prolonged antibacterial, anti-inflammatory and immunomodulatory effects. Azithromycin belongs to BCS class II drug i.e. drug with poor solubility and good permeability. The major problems with this drug is its very poor solubility in biological fluids that results into poor bioavailability after oral administration. The objectives of the present research work were to develop the formulation with enhanced dissolution rate of poorly soluble azithromycin. The solid dispersion of azithromycin was prepared using carrier PEG 6000 by melting method. Tablets were formulated containing solid dispersion products and compared with tablet formulated by pure drug without any carrier. The in vitro dissolution studied showed improved dissolution rate and it was compared with in vivo studied using animal model. Dissolution enhancement of the drug being caused by change in crystalline nature of drug in to amorphous nature.
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