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Amorphous stabilization and dissolution enhancement of amorphous ternary solid dispersions: combination of polymers showing drug-polymer interaction for synergistic effects.
J Pharm Sci. 2014 Nov; 103(11):3511-3523.JP

Abstract

The purpose of this study was to understand the combined effect of two polymers showing drug-polymer interactions on amorphous stabilization and dissolution enhancement of indomethacin (IND) in amorphous ternary solid dispersions. The mechanism responsible for the enhanced stability and dissolution of IND in amorphous ternary systems was studied by exploring the miscibility and intermolecular interactions between IND and polymers through thermal and spectroscopic analysis. Eudragit E100 and PVP K90 at low concentrations (2.5%-40%, w/w) were used to prepare amorphous binary and ternary solid dispersions by solvent evaporation. Stability results showed that amorphous ternary solid dispersions have better stability compared with amorphous binary solid dispersions. The dissolution of IND from the ternary dispersion was substantially higher than the binary dispersions as well as amorphous drug. Melting point depression of physical mixtures reveals that the drug was miscible in both the polymers; however, greater miscibility was observed in ternary physical mixtures. The IR analysis confirmed intermolecular interactions between IND and individual polymers. These interactions were found to be intact in ternary systems. These results suggest that the combination of two polymers showing drug-polymer interaction offers synergistic enhancement in amorphous stability and dissolution in ternary solid dispersions.

Authors+Show Affiliations

School of Pharmacy, MCPHS University-Boston, Boston, Massachusetts 02115.School of Pharmacy and Health Professions, Creighton University, Omaha, Nebraska 68178.School of Pharmacy, MCPHS University-Boston, Boston, Massachusetts 02115. Electronic address: eman.atef@mcphs.edu.

Pub Type(s)

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

Language

eng

PubMed ID

25196860

Citation

Prasad, Dev, et al. "Amorphous Stabilization and Dissolution Enhancement of Amorphous Ternary Solid Dispersions: Combination of Polymers Showing Drug-polymer Interaction for Synergistic Effects." Journal of Pharmaceutical Sciences, vol. 103, no. 11, 2014, pp. 3511-3523.
Prasad D, Chauhan H, Atef E. Amorphous stabilization and dissolution enhancement of amorphous ternary solid dispersions: combination of polymers showing drug-polymer interaction for synergistic effects. J Pharm Sci. 2014;103(11):3511-3523.
Prasad, D., Chauhan, H., & Atef, E. (2014). Amorphous stabilization and dissolution enhancement of amorphous ternary solid dispersions: combination of polymers showing drug-polymer interaction for synergistic effects. Journal of Pharmaceutical Sciences, 103(11), 3511-3523. https://doi.org/10.1002/jps.24137
Prasad D, Chauhan H, Atef E. Amorphous Stabilization and Dissolution Enhancement of Amorphous Ternary Solid Dispersions: Combination of Polymers Showing Drug-polymer Interaction for Synergistic Effects. J Pharm Sci. 2014;103(11):3511-3523. PubMed PMID: 25196860.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Amorphous stabilization and dissolution enhancement of amorphous ternary solid dispersions: combination of polymers showing drug-polymer interaction for synergistic effects. AU - Prasad,Dev, AU - Chauhan,Harsh, AU - Atef,Eman, Y1 - 2014/09/05/ PY - 2014/04/27/received PY - 2014/07/23/revised PY - 2014/07/31/accepted PY - 2014/9/9/entrez PY - 2014/9/10/pubmed PY - 2015/6/27/medline KW - Crystallization Inhibition KW - Indomethacin KW - Interaction KW - Polymer KW - amorphous KW - poorly water-soluble drugs KW - solid dispersion KW - solubility KW - supersaturation SP - 3511 EP - 3523 JF - Journal of pharmaceutical sciences JO - J Pharm Sci VL - 103 IS - 11 N2 - The purpose of this study was to understand the combined effect of two polymers showing drug-polymer interactions on amorphous stabilization and dissolution enhancement of indomethacin (IND) in amorphous ternary solid dispersions. The mechanism responsible for the enhanced stability and dissolution of IND in amorphous ternary systems was studied by exploring the miscibility and intermolecular interactions between IND and polymers through thermal and spectroscopic analysis. Eudragit E100 and PVP K90 at low concentrations (2.5%-40%, w/w) were used to prepare amorphous binary and ternary solid dispersions by solvent evaporation. Stability results showed that amorphous ternary solid dispersions have better stability compared with amorphous binary solid dispersions. The dissolution of IND from the ternary dispersion was substantially higher than the binary dispersions as well as amorphous drug. Melting point depression of physical mixtures reveals that the drug was miscible in both the polymers; however, greater miscibility was observed in ternary physical mixtures. The IR analysis confirmed intermolecular interactions between IND and individual polymers. These interactions were found to be intact in ternary systems. These results suggest that the combination of two polymers showing drug-polymer interaction offers synergistic enhancement in amorphous stability and dissolution in ternary solid dispersions. SN - 1520-6017 UR - https://www.unboundmedicine.com/medline/citation/25196860/Amorphous_stabilization_and_dissolution_enhancement_of_amorphous_ternary_solid_dispersions:_combination_of_polymers_showing_drug_polymer_interaction_for_synergistic_effects_ L2 - https://linkinghub.elsevier.com/retrieve/pii/S0022-3549(15)30349-X DB - PRIME DP - Unbound Medicine ER -