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HERO ID
532383
Reference Type
Journal Article
Title
Dissolution enhancement of fenofibrate by micronization, cogrinding and spray-drying: Comparison with commercial preparations
Author(s)
Vogt, M; Kunath, K; Dressman, JB
Year
2008
Is Peer Reviewed?
1
Journal
European Journal of Pharmaceutics and Biopharmaceutics
ISSN:
0939-6411
EISSN:
1873-3441
Volume
68
Issue
2
Page Numbers
283-288
Language
English
PMID
17574403
DOI
10.1016/j.ejpb.2007.05.010
Web of Science Id
WOS:000253304700015
Abstract
Several techniques were compared for improving the dissolution of fenofibrate, a poorly soluble drug. Particle size reduction was realized by jet milling (micronization; cogrinding with lactose, polyvinylpyrrolidone or sodium lauryl sulphate) and by media milling using a bead mill (nanosizing) with subsequent spray-drying. Solid state characterization by X-ray diffraction and Differential Scanning Calorimetry verified the maintenance of the crystalline state of the drug after dry milling and its conversion to the amorphous state during spray-drying. Micronization of fenofibrate enhanced its dissolution rate in biorelevant media (8.2% in 30 min) compared to crude material (1.3% in 30 min). Coground mixtures of the drug increased the dissolution rate further (up to 20% in 30 min). Supersaturated solutions were generated by nanosizing combined with spray-drying, this process converted fenofibrate to the amorphous state. Fenofibrate drug products commercially available on the German and French markets dissolved similarly to crude or micronized fenofibrate, but significantly slower than the coground or spray-dried fenofibrate mixtures. The results suggest that cogrinding and spray-drying are powerful techniques for the preparation of rapidly dissolving formulations of fenofibrate, and could potentially lead to improvements in the bioavailability of oral fenofibrate products. (c) 2007 Elsevier B.V. All rights reserved.
Keywords
biorelevant media; cogrinding; dissolution rate enhancement; fenofibrate; jet milling; micronization; particle size reduction; spray-drying; water-soluble drugs; particle-size; solid dispersion; crystal-growth; polyvinylpyrrolidone; bioavailability; improvement; systems; nanosuspensions; indomethacin
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