基于葡聚糖-瑞舒伐他汀缀合物的微球的制备、表征及体外释放。

Preparation, characterization and in vitro release of microparticles based on dextran-rosuvastatin conjugate.

机构信息

College of Chemistry and Materials Engineering, Wenzhou University, Wenzhou 325027, China.

出版信息

Carbohydr Polym. 2013 Jul 1;96(1):156-62. doi: 10.1016/j.carbpol.2013.03.094. Epub 2013 Apr 6.

DOI:10.1016/j.carbpol.2013.03.094

Abstract

A novel conjugate for rosuvastatin has been prepared by a coupling reaction between rosuvastatin and dextran. The dextran-rosuvastatin conjugates (DRC) were characterized by FT-IR, NMR, and XRD. And the resulting DRC self-assembled into microparticles by controlled slow exchange of solvents applying dialysis. The size and morphology of DRC microparticles could be controlled through the solvents and pH selection. Particles with different shape and size of microspheres, micro-blocks, micro-flakes or three-dimensional network structure were obtained by adjusting the pH from 9.0 to 13.0. Multiple morphologies of nano- or microparticles were collected in different organic solvents. In vitro release studies suggested that these DRC microparticles had a sustained release manner and the release behavior could be controlled by adjusting their morphology.

摘要

已通过将瑞舒伐他汀与葡聚糖偶联反应制备了瑞舒伐他汀的一种新缀合物。葡聚糖-瑞舒伐他汀缀合物（DRC）通过傅里叶变换红外光谱（FT-IR）、核磁共振（NMR）和 X 射线衍射（XRD）进行了表征。通过控制溶剂的缓慢交换应用透析，所得 DRC 自组装成微粒。通过选择溶剂和 pH 值，可以控制 DRC 微粒的尺寸和形态。通过将 pH 值从 9.0 调节至 13.0，可以获得具有不同形状和尺寸的微球、微块、微片或三维网络结构的颗粒。在不同的有机溶剂中收集到具有多种形态的纳米或微粒。体外释放研究表明，这些 DRC 微粒具有缓释方式，并且可以通过调节其形态来控制释放行为。