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Titre du document / Document title

Solid-state characterization of fluconazole

Auteur(s) / Author(s)

ALKHAMIS Khouloud A. (1) ; OBAIDAT Aiman A. (1) ; NUSEIRAT Adi F. (1) ;

Affiliation(s) du ou des auteurs / Author(s) Affiliation(s)

(1) Faculty of Pharmacy, Jordan University of Science and Technology, Irbid, JORDANIE

Résumé / Abstract

Two polymorphs and three solvates of fluconazole were isolated and characterized by x-ray powder diffractometry, IR spectroscopy, differential scanning calorimetry (DSC), thermogravimetry, and their dissolution rates. The different forms were prepared by crystallization of the original powder in different solvents at different cooling rates. X-ray diffraction patterns of the five solid modifications exhibited substantial differences in both the intensity and position of the peaks. FTIR spectra ofthe five different solid-state modifications also exhibited differences in the peaks' positions and intensities. DSC thermogram of anhydrate form I showed a single melting point at 139.2°C. Anhydrate form II showed two endothermic peaks at 136.5 and 139.2°C and one exothermic peak in between. The DSC thermogram of acetone 1/4 solvate exhibited two endothermic peaks at 75.5 and 139.2°C. Benzene 1/7 solvate exhibited two endothermic peaks at 131.5 and 138.8°C. Hydrate E exhibited two endothermic peaks at 102.7 and 139.2°C. The DSC thermogram of anhydrate form II showed that this form is sensitive to the application of a mechanical force. The solubility study showed that anhydrate form II and acetone 1/4 solvate have higher solubilities than anhydrate form I while benzene 1/7 solvate and monohydrate have lower solubilities than anhydrate form I. The intrinsic dissolution study confirmed these results.

Revue / Journal Title

Pharmaceutical development and technology    ISSN  1083-7450 

Source / Source

2002, vol. 7, no4, pp. 491-503 [13 page(s) (article)] (12 ref.)

Langue / Language

Anglais

Editeur / Publisher

Informa Healthcare, New York, NY, ETATS-UNIS  (1996) (Revue)

Mots-clés anglais / English Keywords

Triazole derivatives

;

Dosage form

;

Tablet

;

Crystallization

;

Polymorphism

;

Solubility

;

Dissolution

;

Solid state

;

Antifungal agent

;

Fluconazole

;

Mots-clés français / French Keywords

Triazole dérivé

;

Forme pharmaceutique

;

Comprimé

;

Cristallisation

;

Polymorphisme

;

Solubilité

;

Dissolution

;

Etat solide

;

Antifongique

;

Fluconazole

;

Mots-clés espagnols / Spanish Keywords

Triazol derivado

;

Forma farmacéutica

;

Tableta

;

Cristalización

;

Polimorfismo

;

Solubilidad

;

Disolución

;

Estado sólido

;

Antifúngico

;

Fluconazol

;

Localisation / Location

INIST-CNRS, Cote INIST : 26544, 35400010563907.0100

Nº notice refdoc (ud4) : 14386224



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