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通过溶胶-凝胶法合成二氧化硅-聚乙二醇基质并评估双氯芬酸二乙胺盐的释放情况。

Silica-polyethylene glycol matrix synthesis by sol-gel method and evaluation for diclofenac diethyloammonium release.

作者信息

Prokopowicz Magdalena

机构信息

Division of Physical Chemistry with Instrumental Analysis Laboratory, Medical Academy of Gdansk, Gdansk, Poland.

出版信息

Drug Deliv. 2007 Mar;14(3):129-38. doi: 10.1080/10717540600812653.

Abstract

Modified silica-polyethylene glycol xerogels were prepared by the sol-gel method to explore the possibilities of using these polymers as drug delivery systems. The synthesis was performed at room temperature and under atmospheric pressure using tetraethylorthosilicate (TEOS) as a precursor, low-molecular polyethylene-glycol (600) as a modifier, and acetic acid as a catalyst. The composition in a mole ratio of the initial sols corresponds to TEOS:H(2)O:EtOH:CH(3)COOH:PEG = 1:4:6:0.005:0.147. Diclofenac diethyloammonium was used as a model drug and encapsulated in predoping sol-gel process. After 5 days of gelation time of matrices at room temperature two different forms of xerogels were obtained: monolithic form of pellet and cracked, irregular-shaped of particles. The rate of release from the both forms of xerogels was controlled by the rate of diffusion of the drug through the pores. The dissolution testing for the loaded irregular-shaped xerogels showed an initial burst release followed by sustained release. The degradation of the PEG/silica xerogels followed a zero-order kinetics.

摘要

采用溶胶-凝胶法制备了改性二氧化硅-聚乙二醇干凝胶,以探索将这些聚合物用作药物递送系统的可能性。合成在室温及大气压下进行,使用正硅酸乙酯(TEOS)作为前驱体,低分子聚乙二醇(600)作为改性剂,乙酸作为催化剂。初始溶胶的摩尔比组成对应于TEOS:H₂O:EtOH:CH₃COOH:PEG = 1:4:6:0.005:0.147。双氯芬酸二乙胺用作模型药物,并在预掺杂溶胶-凝胶过程中进行包封。在室温下基质凝胶化5天后,获得了两种不同形式的干凝胶:整体形式的丸粒和破裂的不规则形状颗粒。两种形式干凝胶的释放速率均由药物通过孔隙的扩散速率控制。对负载的不规则形状干凝胶进行的溶出度测试显示,最初有一个突释,随后是持续释放。PEG/二氧化硅干凝胶的降解遵循零级动力学。

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