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The stabilization of amorphous zopiclone in an amorphous solid dispersion

Authors :
10196226 - Liebenberg, Wilna
24888923 - Milne, Marnus
11927860 - Aucamp, Marique Elizabeth
Milne, Marnus
Liebenberg, Wilna
Aucamp, Marique
10196226 - Liebenberg, Wilna
24888923 - Milne, Marnus
11927860 - Aucamp, Marique Elizabeth
Milne, Marnus
Liebenberg, Wilna
Aucamp, Marique
Publication Year :
2015

Abstract

Zopiclone is a poorly soluble psychotherapeutic agent. The aim of this study was to prepare and characterize an amorphous form of zopiclone as well as the characterization and performance of a stable amorphous solid dispersion. The amorphous form was prepared by the well-known method of quenchcooling of the melt. The solid dispersion was prepared by a solvent evaporation method of zopiclone, polyvinylpyrrolidone-25 (PVP-25), and methanol, followed by freeze-drying. The physico-chemical properties and stability of amorphous zopiclone and the solid dispersion was studied using differential scanning calorimetry (DSC), infrared spectroscopy (FT-IR), thermogravimetric analysis (TGA), scanning electron microscopy (SEM), hot-stage microscopy (HSM), X-ray diffractometry (XRD), solubility, and dissolution studies. The zopiclone amorphous solid-state form was determined to be a fragile glass; it was concluded that the stability of the amorphous form is influenced by both temperature and water. Exposure of amorphous zopiclone to moisture results in rapid transformation of the amorphous form to the crystalline dihydrated form. In comparison, the amorphous solid dispersion proved to be more stable with increased aqueous solubility

Details

Database :
OAIster
Notes :
English
Publication Type :
Electronic Resource
Accession number :
edsoai.on1139716717
Document Type :
Electronic Resource