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Glass Transition Dynamics and Physical Stability of Amorphous Griseofulvin in Binary Mixtures with Low-Tg Excipients.
Mol Pharm. 2019 08 05; 16(8):3626-3635.MP

Abstract

Amorphization of drug formulations containing active pharmaceutical ingredients (APIs) and excipients has been proven to be an effective strategy to improve their poor aqueous solubility. The excipients can also impact the physical stability of the prepared amorphous forms. Generally, researchers are more apt to select excipients that have high values of glass transition temperature (Tg) because of the antiplasticization effect of the additives on APIs. In this article, we studied the glass transition dynamics as well as crystallization behavior in binary blends composed of griseofulvin (GSF) and two low-Tg additives, octaacetylmaltose (acMAL) and polyvinyl acetate (PVAc), with a particular focus on the plasticization effect. Effectively suppressed crystallization of GSF is observed in both systems when higher excipient contents are used. Our finding aims to encourage the use of specifically developed protocols in which suitable plasticizers are used as excipients for stabilizing the amorphous state of a drug.

Authors+Show Affiliations

Institute of Physics , University of Silesia , 75 Pułku Piechoty 1a , 41-500 Chorzow , Poland. SMCEBI , 75 Pułku Piechoty 1a , 41-500 Chorzow , Poland.Institute of Physics , University of Silesia , 75 Pułku Piechoty 1a , 41-500 Chorzow , Poland. SMCEBI , 75 Pułku Piechoty 1a , 41-500 Chorzow , Poland.Institute of Physics , University of Silesia , 75 Pułku Piechoty 1a , 41-500 Chorzow , Poland. SMCEBI , 75 Pułku Piechoty 1a , 41-500 Chorzow , Poland.Institute of Physics , University of Silesia , 75 Pułku Piechoty 1a , 41-500 Chorzow , Poland. SMCEBI , 75 Pułku Piechoty 1a , 41-500 Chorzow , Poland.

Pub Type(s)

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

Language

eng

PubMed ID

31287704

Citation

Tu, Wenkang, et al. "Glass Transition Dynamics and Physical Stability of Amorphous Griseofulvin in Binary Mixtures With Low-Tg Excipients." Molecular Pharmaceutics, vol. 16, no. 8, 2019, pp. 3626-3635.
Tu W, Knapik-Kowalczuk J, Chmiel K, et al. Glass Transition Dynamics and Physical Stability of Amorphous Griseofulvin in Binary Mixtures with Low-Tg Excipients. Mol Pharm. 2019;16(8):3626-3635.
Tu, W., Knapik-Kowalczuk, J., Chmiel, K., & Paluch, M. (2019). Glass Transition Dynamics and Physical Stability of Amorphous Griseofulvin in Binary Mixtures with Low-Tg Excipients. Molecular Pharmaceutics, 16(8), 3626-3635. https://doi.org/10.1021/acs.molpharmaceut.9b00476
Tu W, et al. Glass Transition Dynamics and Physical Stability of Amorphous Griseofulvin in Binary Mixtures With Low-Tg Excipients. Mol Pharm. 2019 08 5;16(8):3626-3635. PubMed PMID: 31287704.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Glass Transition Dynamics and Physical Stability of Amorphous Griseofulvin in Binary Mixtures with Low-Tg Excipients. AU - Tu,Wenkang, AU - Knapik-Kowalczuk,Justyna, AU - Chmiel,Krzysztof, AU - Paluch,Marian, Y1 - 2019/07/23/ PY - 2019/7/10/pubmed PY - 2020/6/26/medline PY - 2019/7/10/entrez KW - amorphous pharmaceuticals KW - crystallization KW - dielectric spectroscopy KW - griseofulvin KW - molecular mobility KW - physical stability KW - plasticization effect SP - 3626 EP - 3635 JF - Molecular pharmaceutics JO - Mol. Pharm. VL - 16 IS - 8 N2 - Amorphization of drug formulations containing active pharmaceutical ingredients (APIs) and excipients has been proven to be an effective strategy to improve their poor aqueous solubility. The excipients can also impact the physical stability of the prepared amorphous forms. Generally, researchers are more apt to select excipients that have high values of glass transition temperature (Tg) because of the antiplasticization effect of the additives on APIs. In this article, we studied the glass transition dynamics as well as crystallization behavior in binary blends composed of griseofulvin (GSF) and two low-Tg additives, octaacetylmaltose (acMAL) and polyvinyl acetate (PVAc), with a particular focus on the plasticization effect. Effectively suppressed crystallization of GSF is observed in both systems when higher excipient contents are used. Our finding aims to encourage the use of specifically developed protocols in which suitable plasticizers are used as excipients for stabilizing the amorphous state of a drug. SN - 1543-8392 UR - https://www.unboundmedicine.com/medline/citation/31287704/Glass_Transition_Dynamics_and_Physical_Stability_of_Amorphous_Griseofulvin_in_Binary_Mixtures_with_Low_Tg_Excipients_ L2 - https://doi.org/10.1021/acs.molpharmaceut.9b00476 DB - PRIME DP - Unbound Medicine ER -