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Titolo:
Investigation of thermal properties of glassy itraconazole: identificationof a monotropic mesophase
Autore:
Six, K; Verreck, G; Peeters, J; Binnemans, K; Berghmans, H; Augustijns, P; Kinget, R; Van den Mooter, G;
Indirizzi:
Katholieke Univ Leuven, Lab Farmacotechnol & Biofarm, Louvain, Belgium Katholieke Univ Leuven Louvain Belgium hnol & Biofarm, Louvain, Belgium Janssen Res Fdn, B-2340 Beerse, Belgium Janssen Res Fdn Beerse Belgium B-2340 en Res Fdn, B-2340 Beerse, Belgium Katholieke Univ Leuven, Lab Coordinatiechem, Louvain, Belgium Katholieke Univ Leuven Louvain Belgium oordinatiechem, Louvain, Belgium Katholieke Univ Leuven, Lab Polymeerchem, Louvain, Belgium Katholieke UnivLeuven Louvain Belgium b Polymeerchem, Louvain, Belgium
Titolo Testata:
THERMOCHIMICA ACTA
fascicolo: 2, volume: 376, anno: 2001,
pagine: 175 - 181
SICI:
0040-6031(20010907)376:2<175:IOTPOG>2.0.ZU;2-S
Fonte:
ISI
Lingua:
ENG
Keywords:
itraconazole; liquid crystals; MTDSC; glassy drugs;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Physical, Chemical & Earth Sciences
Citazioni:
10
Recensione:
Indirizzi per estratti:
Indirizzo: Van den Mooter, G Katholieke Univ Leuven, Lab Farmacotechnol & Biofarm, Louvain, Belgium Katholieke Univ Leuven Louvain Belgium uvain, Belgium
Citazione:
K. Six et al., "Investigation of thermal properties of glassy itraconazole: identificationof a monotropic mesophase", THERMOC ACT, 376(2), 2001, pp. 175-181

Abstract

The purpose of the present work is the elucidation of two endothermic transitions at 74 and 90 degreesC, respectively, observed during differential scanning calorimetry of glassy itraconazole. Modulated temperature DSC (MTDSC), hot-stage microscopy (HSM), HPLC and high temperature X-ray diffraction(HT-X ray) were used to examine the thermal properties of glassy itraconazole. It was found that the preparation mode of the glass does not seem to influence the appearance of both endothermic transitions since they were present during heating of glassy itraconazole which was prepared by cooling the melt or by rapid solvent evaporation of an itraconazole solution. These observations suggest that the appearance of the two endothermic transitions require the liquid state prior to glass formation. The transitions are not due to impurities in the starting material, nor are they caused by thermal decomposition. This was further confirmed by HPLC-analysis. HSM showed structure formation following cooling of the melt, at approximately 87 degreesC; cooling the product further showed a second change in optical contrast. HT-X ray confirmed and identified the formation of a nematic mesophase. The appearance of the two endothermic signals during scanning of glassy itraconazole points to the formation of a mesophase. Due to the nature of itraconazole, it appears as a chiral nematic phase of which the mobility is frozen into a glass upon cooling below 59 degreesC thereby impeding further crystallization. (C) 2001 Elsevier Science B.V. All rights reserved.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 08/07/20 alle ore 07:04:16