期刊
EUROPEAN JOURNAL OF PHARMACEUTICS AND BIOPHARMACEUTICS
卷 119, 期 -, 页码 243-252出版社
ELSEVIER SCIENCE BV
DOI: 10.1016/j.ejpb.2017.06.021
关键词
Amorphous drug; Two-phase solid dispersion; Glucose; lndomethacin; Low solubility, immiscible, ultrasound
资金
- SEP-CONACyT program [255135]
- School of Engineering and Sciences from Institute Tecnologico y de Estudios Superiores de Monterrey
Amorphization of active pharmaceutical ingredients (APIs) and the preparation of solid dispersions are strategies that can be synergized to improve the solubility of oral drugs. Immiscibility between an API and a carrier in the molten state that could be perceived as a problem in the preparation of solid dispersions, may actually introduce an advantage. In the present work, a two-phase amorphous-amorphous solid dispersion (AASD) was prepared by ultrasonicating a molten immiscible mixture of indomethacin (IND) and glucose (GLU) prior quenching. By introducing this novel ultrasound assisted method, the immiscible API particles were uniformly dispersed as microscopic glassy clusters of the drug in the solid amorphous GLU matrix; particle sizes of IND in the AASD range from 600 nm to 1.4 um. As a result of the amorphization and particle size reduction of IND, its aqueous solubility increased to reach almost 40 ppm (8 times more soluble compared to indomethacin in its crystalline state). In addition, the oral bioavailability and its resistance against crystallization were also enhanced; AASD samples have remained amorphous for more than two years of storage. (C) 2017 Elsevier B.V. All rights reserved.
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