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Influence of copolymer composition on the phase behavior of solid dispersions.
Mol Pharm. 2014 Nov 03; 11(11):4189-98.MP

Abstract

The incorporation of poorly soluble active pharmaceutical ingredients (APIs) into excipients (e.g., polymers) to formulate an amorphous solid dispersion is a promising strategy to improve the oral bioavailability of the API. The application of copolymer excipients allows access to combinations of different monomers and thus to the design of excipients to improve solid-dispersion properties. In this work, the thermodynamic phase behavior of solid dispersions was investigated as a function of the API, type of monomer, and copolymer composition. The glass-transition temperatures and API solubilities in the solid dispersions of naproxen and indomethacin in polyvinylpyrrolidone, polyvinyl acetate, and copolymers with different weight fractions of vinylpyrrolidone and vinyl actetate were investigated. It is shown that the thermodynamic phase behavior of API/copolymer solid dispersions is a function of monomer type and copolymer composition. This effect was also predicted by using the perturbed-chain statistical associating fluid theory (PC-SAFT). The glass-transition temperature of the solid dispersions was calculated with the Gordon-Taylor equation.

Authors+Show Affiliations

Department of Biochemical and Chemical Engineering, Laboratory of Thermodynamics, TU Dortmund , Emil-Figge-Str. 70, D-44227 Dortmund, Germany.No affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info available

Pub Type(s)

Journal Article
Research Support, Non-U.S. Gov't

Language

eng

PubMed ID

25295846

Citation

Prudic, Anke, et al. "Influence of Copolymer Composition On the Phase Behavior of Solid Dispersions." Molecular Pharmaceutics, vol. 11, no. 11, 2014, pp. 4189-98.
Prudic A, Kleetz T, Korf M, et al. Influence of copolymer composition on the phase behavior of solid dispersions. Mol Pharm. 2014;11(11):4189-98.
Prudic, A., Kleetz, T., Korf, M., Ji, Y., & Sadowski, G. (2014). Influence of copolymer composition on the phase behavior of solid dispersions. Molecular Pharmaceutics, 11(11), 4189-98. https://doi.org/10.1021/mp500412d
Prudic A, et al. Influence of Copolymer Composition On the Phase Behavior of Solid Dispersions. Mol Pharm. 2014 Nov 3;11(11):4189-98. PubMed PMID: 25295846.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Influence of copolymer composition on the phase behavior of solid dispersions. AU - Prudic,Anke, AU - Kleetz,Tobias, AU - Korf,Marcel, AU - Ji,Yuanhui, AU - Sadowski,Gabriele, Y1 - 2014/10/21/ PY - 2014/10/9/entrez PY - 2014/10/9/pubmed PY - 2015/7/15/medline KW - PC-SAFT KW - copolymer KW - indomethacin KW - naproxen KW - phase behavior KW - poorly soluble pharmaceutical KW - thermodynamic model SP - 4189 EP - 98 JF - Molecular pharmaceutics JO - Mol Pharm VL - 11 IS - 11 N2 - The incorporation of poorly soluble active pharmaceutical ingredients (APIs) into excipients (e.g., polymers) to formulate an amorphous solid dispersion is a promising strategy to improve the oral bioavailability of the API. The application of copolymer excipients allows access to combinations of different monomers and thus to the design of excipients to improve solid-dispersion properties. In this work, the thermodynamic phase behavior of solid dispersions was investigated as a function of the API, type of monomer, and copolymer composition. The glass-transition temperatures and API solubilities in the solid dispersions of naproxen and indomethacin in polyvinylpyrrolidone, polyvinyl acetate, and copolymers with different weight fractions of vinylpyrrolidone and vinyl actetate were investigated. It is shown that the thermodynamic phase behavior of API/copolymer solid dispersions is a function of monomer type and copolymer composition. This effect was also predicted by using the perturbed-chain statistical associating fluid theory (PC-SAFT). The glass-transition temperature of the solid dispersions was calculated with the Gordon-Taylor equation. SN - 1543-8392 UR - https://www.unboundmedicine.com/medline/citation/25295846/Influence_of_copolymer_composition_on_the_phase_behavior_of_solid_dispersions_ L2 - https://doi.org/10.1021/mp500412d DB - PRIME DP - Unbound Medicine ER -