Agglomeration of Mesoporous Silica by Melt and Steam Granulation. Part II: Screening of Steam Granulation Process Variables Using a Factorial Design

The objectives of this study were to identify the key process parameters during steam granulation of disordered mesoporous silica material Syloid® 244 FP (244) and to compare two different binders: polyvinylpyrrolidone (PVP) K25 and hydroxypropylmethyl cellulose (HPMC). Itraconazole (ITZ) was select...

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Published in:Journal of pharmaceutical sciences 2013-11, Vol.102 (11), p.3978-3986
Main Authors: Vialpando, Monica, Albertini, Beatrice, Passerini, Nadia, Heyden, Yvan Vander, Rombaut, Patrick, Martens, Johan A., Mooter, Guy Van Den
Format: Article
Language:English
Subjects:
Antifungal Agents - administration & dosage
compaction
compression
Drug Compounding - methods
Excipients - chemistry
factorial design
formulation
Hypromellose Derivatives
Itraconazole - administration & dosage
Methylcellulose - analogs & derivatives
Methylcellulose - chemistry
physical stability
polyvinylpyrrolidone
poorly water-soluble drugs
Povidone - chemistry
powder technology
Silicon Dioxide - chemistry
solid dosage form
Tablets
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Summary:The objectives of this study were to identify the key process parameters during steam granulation of disordered mesoporous silica material Syloid® 244 FP (244) and to compare two different binders: polyvinylpyrrolidone (PVP) K25 and hydroxypropylmethyl cellulose (HPMC). Itraconazole (ITZ) was selected as the model compound for the development of an oral dosage form for enhanced release. Six factors: binder content, steam amount, mixing time, impeller speed, spray pause time, and filler content were investigated using a two-level quarter-fraction factorial design of experiment (DOE) for each binder type. As experimental responses, characteristics correlating to both granules and tablets were selected. Granules prepared from PVP resulted in an overall higher bulk density, granule size, increased flow properties, and better compression and compaction behavior. Although granulation with PVP resulted in the most ITZ to extract from the pores during processing, the premature drug release was less than 5%. The results of the DOE indicate that the risk of extracting the drug from the pores during processing is governed both by the process parameters and the binder properties. Centerpoint replicates of granules prepared with HPMC were highly variable. © 2013 Wiley Periodicals, Inc. and the American Pharmacists Association J Pharm Sci 102:3978–3986, 2013
ISSN:0022-3549
1520-6017
DOI:10.1002/jps.23699