Interaction products of metformin hydrochloride (MF·HCl), an oral anti-hyperglycaemic agent highly soluble in water, with triacetyl-- cyclodextrin (TACyD), a hydrophobic CyD derivative practically insoluble inwater, were prepared to evaluate their suitability for the development of a sustained-release dosage form of the drug. Equimolar MF·HCl–TACyD solid compounds were obtained by different techniques, i.e., physical mixing, kneading, co-grinding, sealed-heating, and spray-drying, in order to investigate and compare their effectiveness and influence on the physical–chemical properties of the final products. Differential scanning calorimetry, X-ray powder diffractometry, Fourier transform infrared spectroscopy and scanning electron microscopy were used for the solid-state characterization of the different MF·HCl–TACyD systems, whereas their in vitro dissolution properties were determined according to the dispersed amount method. According to the results of solid-state studies, the ability of the different preparation methods to promote effective interactions between drug and CyD varied in the order: spray-drying > cogrinding > kneading > sealed-heating≈physical mixing. The same effectiveness rank order was observed also in dissolution studies. In fact the time to dissolve 100% drug varied increased from 1 min, for pure drug, to 3, 7, 40, 120 up to 420 min for physically mixed, sealed-heated, kneaded, co-ground and spray-dried products, respectively. Thus the drug–TA(CyD products obtained by spray drying and co-grinding were selected as the best candidates for the future development of a suitable prolonged-release oral dosage form of MF·HCl.

Physical chemical characterization of binary systems of metformin hydrochloride with triacetyl-β-cyclodextrin / G.Corti; G.Capasso; F. Maestrelli; M.Cirri; P. Mura. - In: JOURNAL OF PHARMACEUTICAL AND BIOMEDICAL ANALYSIS. - ISSN 0731-7085. - ELETTRONICO. - 45:(2007), pp. 480-486. [10.1016/j.jpba.2007.07.018]

Physical chemical characterization of binary systems of metformin hydrochloride with triacetyl-β-cyclodextrin

MAESTRELLI, FRANCESCA;CIRRI, MARZIA;MURA, PAOLA ANGELA
2007

Abstract

Interaction products of metformin hydrochloride (MF·HCl), an oral anti-hyperglycaemic agent highly soluble in water, with triacetyl-- cyclodextrin (TACyD), a hydrophobic CyD derivative practically insoluble inwater, were prepared to evaluate their suitability for the development of a sustained-release dosage form of the drug. Equimolar MF·HCl–TACyD solid compounds were obtained by different techniques, i.e., physical mixing, kneading, co-grinding, sealed-heating, and spray-drying, in order to investigate and compare their effectiveness and influence on the physical–chemical properties of the final products. Differential scanning calorimetry, X-ray powder diffractometry, Fourier transform infrared spectroscopy and scanning electron microscopy were used for the solid-state characterization of the different MF·HCl–TACyD systems, whereas their in vitro dissolution properties were determined according to the dispersed amount method. According to the results of solid-state studies, the ability of the different preparation methods to promote effective interactions between drug and CyD varied in the order: spray-drying > cogrinding > kneading > sealed-heating≈physical mixing. The same effectiveness rank order was observed also in dissolution studies. In fact the time to dissolve 100% drug varied increased from 1 min, for pure drug, to 3, 7, 40, 120 up to 420 min for physically mixed, sealed-heated, kneaded, co-ground and spray-dried products, respectively. Thus the drug–TA(CyD products obtained by spray drying and co-grinding were selected as the best candidates for the future development of a suitable prolonged-release oral dosage form of MF·HCl.
2007
45
480
486
G.Corti; G.Capasso; F. Maestrelli; M.Cirri; P. Mura
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Utilizza questo identificatore per citare o creare un link a questa risorsa: https://hdl.handle.net/2158/254436
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