期刊
EUROPEAN JOURNAL OF PHARMACEUTICS AND BIOPHARMACEUTICS
卷 79, 期 3, 页码 559-565出版社
ELSEVIER
DOI: 10.1016/j.ejpb.2011.07.006
关键词
alpha-Glucosyl hesperidin; Dry grinding; Nanoparticle; Glibenclamide; Dissolution rate; Blood glucose level
资金
- Ministry of Education, Culture, Sports, Science and Technology, Japan [22790041]
- Grants-in-Aid for Scientific Research [22790041] Funding Source: KAKEN
The effectiveness of alpha-glucosyl hesperidin (Hsp-G) as a novel grinding aid for the preparation of drug nanoparticles by dry grinding was investigated. Poorly water-soluble drugs and Hsp-G were mixed at a weight ratio of 1/5 and ground for 60 min by a vibrational ball mill. It was evident that all poorly water-soluble drugs used in this study formed nanoparticles after the ground mixtures were dispersed into distilled water. The dissolution profile of glibenclamide from the ground mixtures of glibenclamide/Hsp-G showed dramatic improvement from that of untreated drug crystals. Administration of the ground mixture of glibenclamide/Hsp-G to rats resulted in a significantly higher rate of decrease in blood glucose levels than that of untreated glibenclamide. The area above the time-curve of plasma-glucose concentrations using the ground mixture of glibenclamide/Hsp-G was 6-fold higher than that using untreated glibenclamide. The improved dissolution rate due to nanoparticle formation of glibenclamide, induced by co-grinding with Hsp-G, was responsible for this improvement. (C) 2011 Elsevier B.V. All rights reserved.
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