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Drug release from compacted single inert matrix agglomerates
Uppsala University, Disciplinary Domain of Medicine and Pharmacy, Faculty of Pharmacy, Department of Pharmacy.
Uppsala University, Disciplinary Domain of Medicine and Pharmacy, Faculty of Pharmacy, Department of Pharmacy.
Uppsala University, Disciplinary Domain of Medicine and Pharmacy, Faculty of Pharmacy, Department of Pharmacy.
2007 (English)In: Journal of Drug Delivery Science and Technology, ISSN 1773-2247, Vol. 17, no 4, 273-277 p.Article in journal (Refereed) Published
Abstract [en]

The effect of compaction on the drug release from single, sodium chloride loaded, microcrystalline cellulose agglomerates of different porosities was investigated in this study. The drug release from uncompacted agglomerates and from agglomerates regained from tablets compacted at a range of different compaction pressures was monitored measuring the conductivity of the dissolution medium in a recirculation flow-through system. The drug release profiles were described using the mean dissolution time (MDT), the variation of dissolution time (VDT) and the relative dispersion coefficient (RD). It was found that depending on physical structure changes of the matrix, the drug release rate of compacted agglomerates could be enhanced or retarded in comparison with uncompacted agglomerates. The retardation is suggested to be due to a densification of the matrix and the enhancement due to a crack formation in the external surface of the matrix.

Place, publisher, year, edition, pages
2007. Vol. 17, no 4, 273-277 p.
National Category
Pharmaceutical Sciences
Identifiers
URN: urn:nbn:se:uu:diva-95424ISI: 000250032200007OAI: oai:DiVA.org:uu-95424DiVA: diva2:169621
Available from: 2007-02-01 Created: 2007-02-01 Last updated: 2011-01-22Bibliographically approved
In thesis
1. Identification and Variation of some Functionality Related Characteristics of Pharmaceutically Relevant Solid Materials and their Effect on Product Performance
Open this publication in new window or tab >>Identification and Variation of some Functionality Related Characteristics of Pharmaceutically Relevant Solid Materials and their Effect on Product Performance
2007 (English)Doctoral thesis, comprehensive summary (Other academic)
Abstract [en]

The aim of this thesis was to identify some functionality related characteristics of pharmaceutically relevant solid materials and to study the effect of their variation on processing behaviour and product performance. For this purpose, particles with different characteristics were prepared under a variety of conditions by crystal agglomeration, wet granulation and spray drying. The effect of particle size distribution on the evolution of the tablet microstructure during and after compression was investigated. The compression behaviour of particles with different nominal strength and degrees of agglomeration was studied and the influence of the surfactant concentration of amorphous particles on the compression behaviour was examined. The response of the powders to compression was described with the help of various techniques characterising the microstructure and tensile strength of the tablets produced.

Furthermore, a method suitable for observing drug release from single matrix granules was developed and used to study the effect of granule porosity and compaction pressure on the drug release process.

The particle size distribution did not influence the evolution of the tablet porosity or the tensile strength during compression, but it could have an effect on the evolution of the tablet microstructure during short-term storage, depending on the instability mechanism. The compression behaviour of particles prepared by crystal agglomeration and wet granulation was dependent on their degree of agglomeration and their failure strength. For particles with similar solid state properties and compression behaviour, the surface energy appears to have an effect on the bonding strength of adsorption bonds acting at interparticulate junctions. Using the method developed to observe the drug release from single matrix granules, reproducible data was obtained enabling the drug release process to be characterised. Depending on the type of matrix and the compaction pressure, the drug release rate could be enhanced or retarded.

Place, publisher, year, edition, pages
Uppsala: Acta Universitatis Upsaliensis, 2007. 92 p.
Series
Digital Comprehensive Summaries of Uppsala Dissertations from the Faculty of Pharmacy, ISSN 1651-6192 ; 47
Keyword
Pharmaceutics, Particle size distribution, Degree of agglomeration, Amorphous lactose, Matrix agglomerates, Drug release, Compactability, Tablet tensile strength, Particle fracture strength, Surfactant, Compression, Galenisk farmaci
Identifiers
urn:nbn:se:uu:diva-7462 (URN)978-91-554-6789-0 (ISBN)
Public defence
2007-02-23, B 41, BMC, Husargatan 3, Uppsala, 09:15
Opponent
Supervisors
Available from: 2007-02-01 Created: 2007-02-01Bibliographically approved

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Fichtner, FraukeFrenning, GöranAlderborn, Göran

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