Influence of soluble and insoluble cyclodextrin polymers on drug release from hydroxypropyl methylcellulose tablets

Background: The influence of β-cyclodextrin (β-CD) polymers on drug release from hydroxypropyl methylcellulose (HPMC) matrices has not been reported in the literature. Aim: The influence of monomeric β-CD and both soluble and insoluble β-CD polymers on drug release from tablets containing either 30%...

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Bibliographic Details
Published in:	Drug development and industrial pharmacy Vol. 35; no. 10; pp. 1264 - 1270
Main Authors:	Zugasti, Maria Esther, Zornoza, Arantza, del Mar Goñi, María, Isasi, José Ramón, Vélaz, Itziar, Martín, Carmen, Sánchez, Miguel, Martínez-Ohárriz, María Cristina
Format:	Journal Article
Language:	English
Published:	Colchester Informa UK Ltd 01-10-2009 Taylor & Francis
Subjects:	Anti-Inflammatory Agents, Non-Steroidal - administration & dosage Anti-Inflammatory Agents, Non-Steroidal - chemistry beta-Cyclodextrins - chemistry Biological and medical sciences Chemistry, Pharmaceutical - methods Delayed-Action Preparations Differential Thermal Analysis Diflunisal - administration & dosage Diflunisal - chemistry Drug Carriers - chemistry drug release Excipients - chemistry General pharmacology HPMC Hypromellose Derivatives Kinetics Medical sciences Methylcellulose - analogs & derivatives Methylcellulose - chemistry Pharmaceutical technology. Pharmaceutical industry Pharmacology. Drug treatments solid state Solubility soluble and insoluble β-cyclodextrin polymers Spectrophotometry, Infrared Tablets X-Ray Diffraction β-Cyclodextrin Drug Pharmaceutical technology Oligosaccharide Polymer Solid state β-Cyclodextrin Cyclodextrin soluble and insoluble β-cyclodextrin polymers Dosage form Tablet drug release Inclusion compound Hypromellose Release HPMC
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Summary:	Background: The influence of β-cyclodextrin (β-CD) polymers on drug release from hydroxypropyl methylcellulose (HPMC) matrices has not been reported in the literature. Aim: The influence of monomeric β-CD and both soluble and insoluble β-CD polymers on drug release from tablets containing either 30% or 50% hydroxypropyl methylcellulose has been studied using diflunisal (DF) as model drug. Method: The DF-β-CD inclusion complex (1:1 M) was prepared by coevaporation and characterised using X-ray diffraction, differential thermal analysis, and IR spectroscopy. The dissolution assays were performed according to the USP paddle method. Results: The incorporation of β-CD in the complexed form increases drug release from hydroxypropyl methylcellulose tablets in comparison with the physical mixture because of the better solubilization of the drug. The soluble polymer promotes drug release to a higher extent than the physical mixture with monomeric β-CD, but the insoluble polymer, which is itself a hydrogel, gives rise to the most retarded release profile, probably by retention of the drug in its structure. The formulations containing physical mixtures with either β-CD or the soluble polymer present an optimum adjustment to zero-order release kinetics, and the inclusion complex followed non-Fickian diffusion according to the Korsmeyer-Peppas model. Conclusion: The release profile of DF from a HPMC matrix can be modulated in different ways by the use of either monomeric or polymeric β-CD.
Bibliography:	ObjectType-Article-1 SourceType-Scholarly Journals-1 ObjectType-Feature-2 content type line 23
ISSN:	0363-9045 1520-5762
DOI:	10.1080/03639040902882306