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Use of crospovidone as pelletization aid as alternative to microcrystalline cellulose: effects on pellet properties.
MedLine Citation:
PMID:  19832632     Owner:  NLM     Status:  In-Process    
Abstract/OtherAbstract:
BACKGROUND: Microcrystalline cellulose (MCC) is the most important pelletization aid in extrusion/spheronization. Because of known disadvantages, the search for substitutes is ongoing. In this context, crospovidone has proven to offer substantial advantages as pelletization aid because of its ability to turn low-soluble active ingredients into fast-dissolving stable pellets. METHOD: Pellets from crospovidone with different amounts of paracetamol, hydrochlorothiazide, and spironolactone as model drugs were prepared by extrusion/spheronization. For comparison, pellets with MCC as extrusion aid were also produced. The pellets of different formulations were evaluated in terms of yield, aspect ratio, mean Feret diameter, 10% interval fraction, tensile strength, disintegration, and drug release profile. RESULTS: Only crospovidone types exhibiting small particle sizes are suitable as pelletization aid. While maintaining the pharmaceutical quality aspects, it was possible to incorporate up to 60% (w/w) active pharmaceutical ingredients (API) into pellets with crospovidone. The most distinguished differences between pellets based on crospovidone and MCC are the disintegration and drug release behavior. The pellets containing binary mixtures of the low-soluble APIs and crospovidone resulted in fast release in contrast to the pellets with MCC as pelletization aid, which exhibited a slow release. CONCLUSION: Crospovidone shows an excellent behavior as pelletization aid and produces fast-releasing pellets even with low-soluble APIs.
Authors:
P Verheyen; K-J Steffens; P Kleinebudde
Publication Detail:
Type:  Journal Article    
Journal Detail:
Title:  Drug development and industrial pharmacy     Volume:  35     ISSN:  1520-5762     ISO Abbreviation:  Drug Dev Ind Pharm     Publication Date:  2009 Nov 
Date Detail:
Created Date:  2009-10-16     Completed Date:  -     Revised Date:  -    
Medline Journal Info:
Nlm Unique ID:  7802620     Medline TA:  Drug Dev Ind Pharm     Country:  England    
Other Details:
Languages:  eng     Pagination:  1325-32     Citation Subset:  IM    
Affiliation:
Rottendorf Pharma GmbH, Ennigerloh, Germany.
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