Chemical and Pharmaceutical Bulletin
Online ISSN : 1347-5223
Print ISSN : 0009-2363
ISSN-L : 0009-2363
Some Physicochemical Properties of Glassy Indomethacin
EIHEI FUKUOKAMIDORI MAKITASHIGEO YAMAMURA
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Keywords: dissolution rate
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1986 Volume 34 Issue 10 Pages 4314-4321

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Abstract

Glassy indomethacin was prepared by cooling the melt, and the glassy state was confirmed by the jump of heat capacity and the anomalous endothermic park (heat capacity maximum) in the differential scanning calorimetry (DSC) curve. The influences of the cooling rate of the melt and the heating rate of the glass formed on the glass transition temperature (Tg) were examined, and the apparent activation energy of glass transition was calculated to be 212.5kJ/mol. The relaxation process below Tg was traced in terms of the area under the anomalous endothermic park of the DSC curve and the rate of relaxation during annealing was found to reach the maximum at about 303 K. The rate of dissolution of glassy indomethacin was far greater than that of crystalline indomethacin. Although indomethacin remained as a glass for 2 years at room temperature, pulverized glassy indomethacin was found to crystallize, and the rate of crystallization was determined by the X-ray diffraction method. The degree of crystallization was determined by Hermans' method, and was found to reach a maximum of 60% after 2 months. The process of crystallization followed first-order kinetics.

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© The Pharmaceutical Society of Japan
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