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铁交联琥珀酸壳聚糖和铁交联异羟肟酸琥珀酸壳聚糖的合成及其作为口服茶碱缓释微丸潜在基质材料的体外评价

Synthesis of iron-crosslinked chitosan succinate and iron-crosslinked hydroxamated chitosan succinate and their in vitro evaluation as potential matrix materials for oral theophylline sustained-release beads.

作者信息

Aiedeh K, Taha M O

机构信息

Department of Pharmaceutical Technology and Pharmaceutics, Faculty of Pharmacy, University of Jordan, Amman, Jordan.

出版信息

Eur J Pharm Sci. 2001 May;13(2):159-68. doi: 10.1016/s0928-0987(00)00217-7.

DOI:10.1016/s0928-0987(00)00217-7
PMID:11297900
Abstract

Chitosan succinate (CS) and hydroxamated chitosan succinate (HCS) were prepared. The generated semisynthetic polymers were employed in the formation of drug-loaded, iron(III)-crosslinked polymeric beads. Infrared spectroscopy was employed to prove the crosslinking. The produced beads were evaluated in vitro as drug prolonging and potentially orally administered delivery system. Theophylline was used as the loaded model drug. The generated beads proved to be successful in prolonging drug release. Iron leaching from the generated beads was minimal (<2%), and it only took place under acidic conditions (pH 1).

摘要

制备了琥珀酸壳聚糖(CS)和琥珀酸异羟肟酸壳聚糖(HCS)。所生成的半合成聚合物用于形成载药的、铁(III)交联的聚合物珠粒。采用红外光谱法证明交联。对所制备的珠粒进行体外评价,作为药物缓释且可能口服给药的递送系统。使用茶碱作为载药模型药物。所生成的珠粒在延长药物释放方面被证明是成功的。从所生成的珠粒中浸出的铁极少(<2%),且仅在酸性条件(pH 1)下发生。

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