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阿苯达唑固体分散体的制备、理化性质表征及药物释放研究。

Preparation, physicochemical characterization and drug release studies of albendazole solid dispersions.

作者信息

Mallick S, Sahoo A, Mitra S S

机构信息

Division of Pharmaceutics, Seemanta Institute of Pharmaceutical Sciences, Jharpokharia, Mayurbhanj, Orissa, India.

出版信息

Boll Chim Farm. 2003 May;142(4):180-6.

Abstract

Albendazole (ALB) solid dispersions were prepared by codissolvation and solvent evaporation technique using water soluble carrier such as polyethylene glycol (PEG) and polyvinylpyrrolidone (PVP) to improve the aqueous solubility of the drug and thus enhancing its bioavailability. The physicochemical characteristics of these solid dispersions were performed by scanning electron microscopy (SEM), X-ray diffraction (XRD), fourier-transform infrared (FT-IR) spectroscopy and dissolution rate analyses. SEM was used to clarify the surface and shape characteristics of the different samples. All characteristic bands of albendazole are seen in the FT-IR spectra of solid dispersions. Basically no significant changes in the frequency and shape of albendazole were noticed which leads to the conclusion that no strong interaction between the drug and the polymer exists in the solid dispersion (SD) particles. The degree of crystallinity of ALB decreased and also differed with the SD of different polymers. Dissolution rate and percent dissolution efficiency were significantly increased in the solid dispersions in comparison with drug alone. The drug release kinetics was ascertained by using F-test statistics using kinetic models of zero order, first order, Higuchi and Hixson-Crowell. Albendazole formed solid dispersions with water soluble polymers like PVP and PEG and the dissolution rate of the drug in the SD system was faster when the ratio of polymer to drug was greater. First order model may be used for explaining the kinetics of drug release from all the SD formulations as suggested by F-test.

摘要

采用共溶解和溶剂蒸发技术,使用聚乙二醇(PEG)和聚乙烯吡咯烷酮(PVP)等水溶性载体制备阿苯达唑(ALB)固体分散体,以提高药物的水溶性,从而提高其生物利用度。通过扫描电子显微镜(SEM)、X射线衍射(XRD)、傅里叶变换红外(FT-IR)光谱和溶出速率分析对这些固体分散体的物理化学特性进行了研究。SEM用于阐明不同样品的表面和形状特征。在固体分散体的FT-IR光谱中可以看到阿苯达唑的所有特征谱带。基本上,阿苯达唑的频率和形状没有明显变化,这表明在固体分散体(SD)颗粒中药物与聚合物之间不存在强烈相互作用。ALB的结晶度降低,并且因不同聚合物的SD而有所不同。与单独的药物相比,固体分散体中的溶出速率和溶出效率百分比显著提高。通过使用零级、一级、Higuchi和Hixson-Crowell动力学模型的F检验统计来确定药物释放动力学。阿苯达唑与PVP和PEG等水溶性聚合物形成固体分散体,当聚合物与药物的比例更大时,药物在SD系统中的溶出速率更快。如F检验所建议的,一级模型可用于解释所有SD制剂中药物释放的动力学。

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