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速尿从聚乙二醇固体分散体中的溶出速率。

Dissolution rate of furosemide from polyethylene glycol solid dispersions.

作者信息

Ozdemir N, Ordu S

机构信息

Department of Pharmaceutical Technology, Faculty of Pharmacy, University of Ankara, Tandoğan, Türkiye.

出版信息

Farmaco. 1997 Oct;52(10):625-9.

PMID:9507675
Abstract

In this study, by preparing the solid dispersions of furosemide, a substance that is poor-soluble in water, with polyethylene glycol 6000, 10,000 and 20,000, the enhancement of the dissolution rate of furosemide has been aimed. Solid dispersions were prepared by the fusion method in proportions of 1:4, 1:6 and 1:10 (active material/polymer). The formation of solid dispersion was tested by the techniques of X-ray diffraction, differential calorimetry (DSC) and infrared spectroscopy (IR). The release rate of active material from the solid dispersions prepared was examined by using the flow through cell method. Also, the effect of particle size of the complexes obtained, on the dissolution rate and the stabilities of these complexes were studied. It was determined that the dissolution rate of furosemide was markedly increased along with the formation of the complex and that a better dissolution profile was obtained even in the physical mixtures prepared for the purposes of comparison. It was found that the molecular weights of different kinds of polyethylene glycols and the various proportions of active material/polymer complexes as well as the particle sizes of the solid dispersions were not efficient in the release rate of active material. It was concluded that the increase of the dissolution rate was being a result of both wettability and solubility enhancing effects of polyethylene glycols.

摘要

在本研究中,通过将难溶于水的速尿与聚乙二醇6000、10000和20000制备固体分散体,旨在提高速尿的溶解速率。采用熔融法按1:4、1:6和1:10(活性物质/聚合物)的比例制备固体分散体。通过X射线衍射、差示量热法(DSC)和红外光谱法(IR)技术测试固体分散体的形成。采用流通池法考察所制备固体分散体中活性物质的释放速率。此外,研究了所得复合物的粒径对溶解速率和这些复合物稳定性的影响。结果表明,随着复合物的形成,速尿的溶解速率显著提高,甚至在为比较目的而制备的物理混合物中也获得了更好的溶解曲线。发现不同种类聚乙二醇的分子量、活性物质/聚合物复合物的不同比例以及固体分散体的粒径对活性物质的释放速率没有影响。得出的结论是,溶解速率的提高是聚乙二醇的润湿性和溶解性增强作用共同作用的结果。

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