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Citation
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HERO ID
1249959
Reference Type
Journal Article
Title
Preparation and Characterization of Tablet Formulation based on Solid Dispersion of Glimepiride and Poly(ester amide) Hyperbranched Polymer
Author(s)
Reven, S; Homar, M; Peternel, L; Kristl, J; Zagar, E
Year
2013
Is Peer Reviewed?
1
Journal
Pharm Dev Technol
ISSN:
1083-7450
Volume
18
Issue
2
Page Numbers
323-332
Language
English
PMID
21812524
DOI
10.3109/10837450.2011.598164
Web of Science Id
WOS:000313682400003
URL
http://www.tandfonline.com/doi/full/10.3109/10837450.2011.598164
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Abstract
The feasibility of incorporating a solid dispersion containing poorly soluble antidiabetic drug glimepiride and poly(ester amide) hyperbranched polymer into a tablet using a direct-compression tabletting technique was investigated. Tablet cores were additionally coated with hydroxypropyl methylcellulose phthalate in order to protect the extremely hygroscopic solid dispersion from atmospheric moisture. Preliminary stability studies show that glimepiride, which is in amorphous form within solid dispersion, is chemically stable, even if tablets are exposed to elevated temperature and/or moisture. In-vitro dissolution studies show some impact of storage conditions on the tablet cores disintegration time and, consequently, drug release rate. Glimepiride solubility also deteriorates somewhat, most probably due to its partial recrystallization. Storage conditions much less affect the physical stability of coated tablets, which was ascribed to reduced tablet hygroscopicity due to the presence of protecting coating. The hyperbranched polymers are rather new and complex macromolecules. Therefore, we addressed also the biocompatibility of hyperbranched polymer, i.e., its impact on haemolysis of the red blood cells. The concentration required for the haemolytic effect on the red blood cells is around 100-times higher than its expected gastrointestinal luminal concentration, which makes the occurrence of hyperbranched polymer mediated cytotoxicity very unlikely.
Keywords
Biocompatibility; dissolution; preformulation; morphology; solubilization; stability
Tags
•
Phthalates – Targeted Search for Epidemiological Studies
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Source – no date limit through June 2013 (Private)
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Source - Dec 2013 Update (Private)
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Source - Jun 2014 Update (Private)
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