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Roller compaction of different pseudopolymorphic forms of theophylline: Effect on compressibility and tablet properties.
Int J Pharm. 2010 Aug 30; 396(1-2):53-62.IJ

Abstract

The effect of roller compaction on disintegration time, dissolution rate and compressibility of tablets prepared from theophylline anhydrate powder, theophylline anhydrate fine powder and theophylline monohydrate was studied. In addition, the influence of adding microcrystalline cellulose, a commonly used excipient, in mixtures with these materials was investigated. Theophylline anhydrate powder was used as a model drug to investigate the influence of different compaction pressures on the tablet properties. Tablets with same porosity were prepared by direct compaction and by roller compaction/re-compaction. Compressibility was characterized by Heckel and modified Heckel equations. Due to the property of polymorphic materials to change their form during milling and compression, X-ray diffraction analysis of theophylline anhydrate powder, theophylline anhydrate fine powder and theophylline monohydrate powders and granules was carried out. After roller compaction the disintegration time and the dissolution rate of the tablets were significantly improved. Compressibility of theophylline anhydrate powder and theophylline anhydrate fine powder was decreased, while theophylline monohydrate showed higher compressibility after roller compaction. Microcrystalline cellulose affected compressibility of theophylline anhydrate powder, theophylline anhydrate fine powder and theophylline monohydrate whereby the binary mixtures showed higher compressibility than the individual materials. X-ray diffraction analyses confirmed that there were no polymorphic/pseudopolymorphic changes after roller compaction.

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Publisher Full Text (DOI)

Authors+Show Affiliations

Hadzović E
Industrial Pharmacy Lab, Department of Pharmaceutical Sciences, University of Basel, Klingelbergstr. 50, 4056 Basel, Switzerland.
Betz G
No affiliation info available
Hadzidedić S
No affiliation info available
El-Arini SK
No affiliation info available
Leuenberger H
No affiliation info available

MeSH

CelluloseChemistry, PharmaceuticalCompressive StrengthCrystallizationCrystallography, X-RayKineticsMicroscopy, Electron, ScanningModels, ChemicalParticle SizePorosityPowdersPressureSolubilitySurface PropertiesTabletsTechnology, PharmaceuticalTheophyllineWater

Pub Type(s)

Comparative Study
Journal Article

Language

eng

PubMed ID

20600735

Citation

Hadzović, Ervina, et al. "Roller Compaction of Different Pseudopolymorphic Forms of Theophylline: Effect On Compressibility and Tablet Properties." International Journal of Pharmaceutics, vol. 396, no. 1-2, 2010, pp. 53-62.
Hadzović E, Betz G, Hadzidedić S, et al. Roller compaction of different pseudopolymorphic forms of theophylline: Effect on compressibility and tablet properties. Int J Pharm. 2010;396(1-2):53-62.
Hadzović, E., Betz, G., Hadzidedić, S., El-Arini, S. K., & Leuenberger, H. (2010). Roller compaction of different pseudopolymorphic forms of theophylline: Effect on compressibility and tablet properties. International Journal of Pharmaceutics, 396(1-2), 53-62. https://doi.org/10.1016/j.ijpharm.2010.06.009
Hadzović E, et al. Roller Compaction of Different Pseudopolymorphic Forms of Theophylline: Effect On Compressibility and Tablet Properties. Int J Pharm. 2010 Aug 30;396(1-2):53-62. PubMed PMID: 20600735.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Roller compaction of different pseudopolymorphic forms of theophylline: Effect on compressibility and tablet properties. AU - Hadzović,Ervina, AU - Betz,Gabriele, AU - Hadzidedić,Seherzada, AU - El-Arini,Silvia Kocova, AU - Leuenberger,Hans, Y1 - 2010/06/19/ PY - 2010/04/09/received PY - 2010/05/31/revised PY - 2010/06/01/accepted PY - 2010/7/6/entrez PY - 2010/7/6/pubmed PY - 2010/11/3/medline SP - 53 EP - 62 JF - International journal of pharmaceutics JO - Int J Pharm VL - 396 IS - 1-2 N2 - The effect of roller compaction on disintegration time, dissolution rate and compressibility of tablets prepared from theophylline anhydrate powder, theophylline anhydrate fine powder and theophylline monohydrate was studied. In addition, the influence of adding microcrystalline cellulose, a commonly used excipient, in mixtures with these materials was investigated. Theophylline anhydrate powder was used as a model drug to investigate the influence of different compaction pressures on the tablet properties. Tablets with same porosity were prepared by direct compaction and by roller compaction/re-compaction. Compressibility was characterized by Heckel and modified Heckel equations. Due to the property of polymorphic materials to change their form during milling and compression, X-ray diffraction analysis of theophylline anhydrate powder, theophylline anhydrate fine powder and theophylline monohydrate powders and granules was carried out. After roller compaction the disintegration time and the dissolution rate of the tablets were significantly improved. Compressibility of theophylline anhydrate powder and theophylline anhydrate fine powder was decreased, while theophylline monohydrate showed higher compressibility after roller compaction. Microcrystalline cellulose affected compressibility of theophylline anhydrate powder, theophylline anhydrate fine powder and theophylline monohydrate whereby the binary mixtures showed higher compressibility than the individual materials. X-ray diffraction analyses confirmed that there were no polymorphic/pseudopolymorphic changes after roller compaction. SN - 1873-3476 UR - https://www.unboundmedicine.com/medline/citation/20600735/Roller_compaction_of_different_pseudopolymorphic_forms_of_theophylline:_Effect_on_compressibility_and_tablet_properties_ DB - PRIME DP - Unbound Medicine ER -