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以天然多糖作为释放调节剂的控释球体的研制。

Development of controlled release spheroids using natural polysaccharide as release modifier.

作者信息

Kulkarni Giriraj T, Gowthamarajan K, Dhobe Rohan R, Yohanan Fenni, Suresh B

机构信息

Department of Pharmaceutics, J.S.S. College of Pharmacy, Tamilnadu, India.

出版信息

Drug Deliv. 2005 Jul-Aug;12(4):201-6. doi: 10.1080/10717540590952537.

Abstract

A polysaccharide hydrogel was isolated from the seeds of Tamarindus indica (tamarind) and was used as release modifier for the preparation of diclofenac sodium spheroids, using extrusion-spheronization technique. The process was studied for the effect of variables to arrive at spheroids with satisfactory particle shape, size and size-distribution. The prepared spheroids were characterized for surface morphology, qualitative surface porosity, friability, bulk density, and flow properties. The in vitro release studies exhibited a zero-order release kinetics that was confirmed by Higuchi's and Peppas' models. A credible correlation was obtained among swelling index, viscosity, surface roughness of the polysaccharide, and in vitro dissolution profile of the spheroids. In the comparative bioavailability study, we found that the developed spheroids were able to sustain the drug release over 8 hr and could improve the extent of absorption and bioavailability of the drug.

摘要

从罗望子(酸豆)种子中分离出一种多糖水凝胶,并将其用作制备双氯芬酸钠球体的释放调节剂,采用挤出滚圆法。研究了该工艺中变量的影响,以获得具有令人满意的颗粒形状、尺寸和尺寸分布的球体。对制备的球体进行了表面形态、定性表面孔隙率、脆碎度、堆密度和流动性质的表征。体外释放研究显示出零级释放动力学,这通过Higuchi模型和Peppas模型得到证实。在多糖的溶胀指数、粘度、表面粗糙度与球体的体外溶出曲线之间获得了可靠的相关性。在比较生物利用度研究中,我们发现所开发的球体能够在8小时内持续释放药物,并能提高药物的吸收程度和生物利用度。

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