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固体分散体系统的药物应用:灰黄霉素-聚乙二醇6000系统的X射线衍射及水溶性研究

Pharmaceutical applications of solid dispersion systems: X-ray diffraction and aqueous solubility studies on griseofulvin-polyethylene glycol 6000 systems.

作者信息

Chiou W L

出版信息

J Pharm Sci. 1977 Jul;66(7):989-91. doi: 10.1002/jps.2600660722.

DOI:10.1002/jps.2600660722
PMID:886463
Abstract

The X-ray diffraction method was used to characterize physiochemical properties of griseofulvin dispersed in polyethylene glycol 4000 and 6000. Results indicate a negligible or very limited solid solubility of griseofulvin in the pulverized solid dispersions. Pulverization and aging had pronounced effects on the X-ray diffraction spectrum. Results from aqueous solubility studies of griseofulvin in various concentrations of polyethylene glycol 6000 further indicate weak or insignificant interactions between the drug and the carrier. Mechanisms are postulated to account for the reported marked enhancement of dissolution rates and oral adsorption of griseofulvin dispersed in these carriers.

摘要

采用X射线衍射法表征了分散于聚乙二醇4000和6000中的灰黄霉素的理化性质。结果表明,灰黄霉素在粉碎的固体分散体中的固溶度可忽略不计或非常有限。粉碎和老化对X射线衍射光谱有显著影响。灰黄霉素在不同浓度聚乙二醇6000中的水溶性研究结果进一步表明,药物与载体之间的相互作用较弱或不显著。推测了这些机制,以解释所报道的分散于这些载体中的灰黄霉素溶解速率和口服吸收显著提高的现象。

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