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Enhancement of amorphous celecoxib stability by mixing it with octaacetylmaltose: the molecular dynamics study.
Mol Pharm. 2012 Apr 02; 9(4):894-904.MP

Abstract

In this paper, we present a novel way of stabilization of amorphous celecoxib (CEL) against recrystallization by preparing binary amorphous celecoxib-octaacetylmaltose (CEL-acMAL) systems by quench-cooling of the molten phase. As far as we know this is the first application of carbohydrate derivatives with acetate groups to enhance the stability of an amorphous drug. We found that CEL in the amorphous mixture with acMAL is characterized by a much better solubility than pure CEL. We report very promising results of the long-term measurements of stability of the CEL-acMAL binary amorphous system with small amount of stabilizer during its storage at room temperature. Moreover, we examined the effect of adding acMAL on molecular dynamics of CEL in the wide temperature range in both the supercooled liquid and glassy states. We found that the molecular mobility of the mixture of CEL with 10 wt % acMAL in the glassy state is much more limited than that in the case of pure CEL, which correlates with the better stability of the amorphous binary system. By dielectric measurements and theoretical calculations within the framework of density functional theory (DFT), we studied the role of acMAL in enhancing the stability of amorphous CEL in mixtures and postulated which interactions between CEL and acMAL molecules can be responsible for preventing devitrification.

Authors+Show Affiliations

Institute of Physics, University of Silesia, ul. Uniwersytecka 4, 40-007 Katowice, Poland. katarzyna.grzybowska@us.edu.plNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo 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

22384922

Citation

Grzybowska, K, et al. "Enhancement of Amorphous Celecoxib Stability By Mixing It With Octaacetylmaltose: the Molecular Dynamics Study." Molecular Pharmaceutics, vol. 9, no. 4, 2012, pp. 894-904.
Grzybowska K, Paluch M, Wlodarczyk P, et al. Enhancement of amorphous celecoxib stability by mixing it with octaacetylmaltose: the molecular dynamics study. Mol Pharm. 2012;9(4):894-904.
Grzybowska, K., Paluch, M., Wlodarczyk, P., Grzybowski, A., Kaminski, K., Hawelek, L., Zakowiecki, D., Kasprzycka, A., & Jankowska-Sumara, I. (2012). Enhancement of amorphous celecoxib stability by mixing it with octaacetylmaltose: the molecular dynamics study. Molecular Pharmaceutics, 9(4), 894-904. https://doi.org/10.1021/mp200436q
Grzybowska K, et al. Enhancement of Amorphous Celecoxib Stability By Mixing It With Octaacetylmaltose: the Molecular Dynamics Study. Mol Pharm. 2012 Apr 2;9(4):894-904. PubMed PMID: 22384922.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Enhancement of amorphous celecoxib stability by mixing it with octaacetylmaltose: the molecular dynamics study. AU - Grzybowska,K, AU - Paluch,M, AU - Wlodarczyk,P, AU - Grzybowski,A, AU - Kaminski,K, AU - Hawelek,L, AU - Zakowiecki,D, AU - Kasprzycka,A, AU - Jankowska-Sumara,I, Y1 - 2012/03/21/ PY - 2012/3/6/entrez PY - 2012/3/6/pubmed PY - 2012/8/2/medline SP - 894 EP - 904 JF - Molecular pharmaceutics JO - Mol. Pharm. VL - 9 IS - 4 N2 - In this paper, we present a novel way of stabilization of amorphous celecoxib (CEL) against recrystallization by preparing binary amorphous celecoxib-octaacetylmaltose (CEL-acMAL) systems by quench-cooling of the molten phase. As far as we know this is the first application of carbohydrate derivatives with acetate groups to enhance the stability of an amorphous drug. We found that CEL in the amorphous mixture with acMAL is characterized by a much better solubility than pure CEL. We report very promising results of the long-term measurements of stability of the CEL-acMAL binary amorphous system with small amount of stabilizer during its storage at room temperature. Moreover, we examined the effect of adding acMAL on molecular dynamics of CEL in the wide temperature range in both the supercooled liquid and glassy states. We found that the molecular mobility of the mixture of CEL with 10 wt % acMAL in the glassy state is much more limited than that in the case of pure CEL, which correlates with the better stability of the amorphous binary system. By dielectric measurements and theoretical calculations within the framework of density functional theory (DFT), we studied the role of acMAL in enhancing the stability of amorphous CEL in mixtures and postulated which interactions between CEL and acMAL molecules can be responsible for preventing devitrification. SN - 1543-8392 UR - https://www.unboundmedicine.com/medline/citation/22384922/Enhancement_of_amorphous_celecoxib_stability_by_mixing_it_with_octaacetylmaltose:_the_molecular_dynamics_study_ L2 - https://dx.doi.org/10.1021/mp200436q DB - PRIME DP - Unbound Medicine ER -