The roles of acidifiers in solid dispersions and physical mixtures

Tran, TT-D, Tran, Ha Lien Phuong, Choi, H-G, Han, H-K and Lee, B-J 2010, The roles of acidifiers in solid dispersions and physical mixtures, International journal of pharmaceutics, vol. 384, no. 1-2, pp. 60-66, doi: 10.1016/j.ijpharm.2009.09.039.

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Title The roles of acidifiers in solid dispersions and physical mixtures
Author(s) Tran, TT-D
Tran, Ha Lien PhuongORCID iD for Tran, Ha Lien Phuong orcid.org/0000-0001-8463-7516
Choi, H-G
Han, H-K
Lee, B-J
Journal name International journal of pharmaceutics
Volume number 384
Issue number 1-2
Start page 60
End page 66
Total pages 7
Publisher Elsevier
Place of publication Amsterdam, The Netherlands
Publication date 2010-01
ISSN 1873-3476
Keyword(s) Chemistry, Pharmaceutical
Citric Acid
Crystallization
Dosage Forms
Pharmaceutical Preparations
Solubility
Science & Technology
Life Sciences & Biomedicine
Pharmacology & Pharmacy
Weakly basic poorly water-soluble drug
Solid dispersion
Physical mixture
Acidifier release
Micro-environmental pH
Drug crystallinity
WEAKLY BASIC DRUG
MICROENVIRONMENTAL PH
MATRIX TABLETS
CONTROLLED-RELEASE
DISSOLUTION
FORMULATIONS
MECHANISM
Summary The roles of acidifiers in polyvinylpyrrolidone-based solid dispersions and physical mixtures were originally investigated on dissolution rate of drug, acidifier release, structural crystallinity and micro-environmental pH. A poorly water-soluble and weakly basic isradipine was used as a model drug. The solid dispersion and physical mixtures were prepared with drug and polyvinylpyrrolidone without or with pH modifiers using the solvent evaporation method and then compressed into tablet. The dissolution rate of drug from solid dispersions containing acidifiers were more pronounced when compared to physical mixtures. The dissolution rate of isradipine from solid dispersion was ranked by acidifiers in a decreasing order: fumaric acid, citric acid, glycolic acid and malic acid. In contrast, the acidifiers in physical mixtures had no significant difference in drug dissolution rate. It was attributed by the rank of acidifiers leading to the decrease of micro-environmental pH and slower release rate of acidifier as well as the maintenance of structural amorphousness. The selection of acidifiers with optimal micro-environmental pH, retarded release rate and maintaining structural amorphousness of drug could maximize the dissolution rate of weakly basic drug in solid dispersion.
Language eng
DOI 10.1016/j.ijpharm.2009.09.039
Field of Research 1115 Pharmacology And Pharmaceutical Sciences
HERDC Research category C1.1 Refereed article in a scholarly journal
Copyright notice ©2009, Elsevier
Persistent URL http://hdl.handle.net/10536/DRO/DU:30119548

Document type: Journal Article
Collections: Faculty of Health
School of Medicine
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