The interactions of trimethoprim, sulphadiazine and sulphamethoxazole with natural (alpha-, beta-, gamma-) and amorphous (RAMEB) or crystalline (DIMEB) methylated beta-cyclodextrins were investigated both in aqueous solution (using phase-solubility analysis) and in the solid state (using DSC supported by X-ray analysis). In particular, DSC studies enabled determination of the relative degree of crystallinity of each drug in its physical and ground mixtures with the different cyclodextrins on the basis of the variation of its heat of fusion in comparison with that of the pure drug. In all cases, the host cavity size was a prevalent factor for the inclusion complexation in liquid state. On the contrary, it had a negligible effect on solid-state interactions in terms of drug amorphization. DIMEB and RAMEB exhibited similar performances in aqueous solution, showing that the presence of methyl-groups improved the complexing and solubilizing properties of beta-cyclodextrin. However, DSC studies revealed that RAMEB was clearly more active in performing solid-state interactions, i.e. drug amorphization, and as stabilizing agent for the amorphous state brought forth.

Differential Scanning calorimetry as an analytical tool in the study of drug-cyclodextrin interactions / P. MURA; F. MAESTRELLI; M. CIRRI; S. FURLANETTO; S. PINZAUTI. - In: JOURNAL OF THERMAL ANALYSIS AND CALORIMETRY. - ISSN 1388-6150. - STAMPA. - 73(2003), pp. 635-646.

Differential Scanning calorimetry as an analytical tool in the study of drug-cyclodextrin interactions

MURA, PAOLA ANGELA;MAESTRELLI, FRANCESCA;CIRRI, MARZIA;FURLANETTO, SANDRA;PINZAUTI, SERGIO
2003

Abstract

The interactions of trimethoprim, sulphadiazine and sulphamethoxazole with natural (alpha-, beta-, gamma-) and amorphous (RAMEB) or crystalline (DIMEB) methylated beta-cyclodextrins were investigated both in aqueous solution (using phase-solubility analysis) and in the solid state (using DSC supported by X-ray analysis). In particular, DSC studies enabled determination of the relative degree of crystallinity of each drug in its physical and ground mixtures with the different cyclodextrins on the basis of the variation of its heat of fusion in comparison with that of the pure drug. In all cases, the host cavity size was a prevalent factor for the inclusion complexation in liquid state. On the contrary, it had a negligible effect on solid-state interactions in terms of drug amorphization. DIMEB and RAMEB exhibited similar performances in aqueous solution, showing that the presence of methyl-groups improved the complexing and solubilizing properties of beta-cyclodextrin. However, DSC studies revealed that RAMEB was clearly more active in performing solid-state interactions, i.e. drug amorphization, and as stabilizing agent for the amorphous state brought forth.
73
635
646
P. MURA; F. MAESTRELLI; M. CIRRI; S. FURLANETTO; S. PINZAUTI
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Utilizza questo identificativo per citare o creare un link a questo documento: http://hdl.handle.net/2158/308662
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