Physical-chemical characterization of binary systems of metformin hydrochloride with triacetyl-beta-cyclodextrin
| Autor: | Francesca Maestrelli, Gaetano Capasso, Marzia Cirri, Paola Mura, Giovanna Corti |
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| Rok vydání: | 2007 |
| Předmět: |
Clinical Biochemistry
Analytical chemistry Pharmaceutical Science Dosage form Analytical Chemistry Inclusion compound chemistry.chemical_compound Differential scanning calorimetry X-Ray Diffraction Drug Discovery Hypoglycemic Agents Solubility Fourier transform infrared spectroscopy Dissolution Spectroscopy chemistry.chemical_classification Drug Carriers Cyclodextrin Calorimetry Differential Scanning Chemistry beta-Cyclodextrins Metformin Spray drying Delayed-Action Preparations Microscopy Electron Scanning Nuclear chemistry |
| Zdroj: | Journal of pharmaceutical and biomedical analysis. 45(3) |
| ISSN: | 0731-7085 |
| Popis: | Interaction products of metformin hydrochloride (MF.HCl), an oral anti-hyperglycaemic agent highly soluble in water, with triacetyl-beta-cyclodextrin (TAbetaCyD), a hydrophobic CyD derivative practically insoluble in water, were prepared to evaluate their suitability for the development of a sustained-release dosage form of the drug. Equimolar MF.HCl-TAbetaCyD 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-TAbetaCyD 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>co-grinding>kneading>sealed-heating approximately 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. |
| Databáze: | OpenAIRE |
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