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

被引:41
作者
Corti, Giovanna [1 ]
Capasso, Gaetano [1 ]
Maestrelli, Francesca [1 ]
Cirri, Marzia [1 ]
Mura, Paola [1 ]
机构
[1] Univ Florence, Fac Pharm, Dept Pharmaceut Sci, I-50019 Florence, Italy
关键词
triacetyl-beta-eyelodextrin; metformin hydrochloride; differential scanning calorimetry; X-ray powder diffractometry; Fourier transform infrared spectroscopy; scanning electron microscopy; dissolution rate;
D O I
10.1016/j.jpba.2007.07.018
中图分类号
O65 [分析化学];
学科分类号
070302 ; 081704 ;
摘要
Interaction products of metformin hydrochloride (MF.HCl), an oral anti-hyperglycaemic agent highly soluble in water, with triacetyl-beta-cyclodextrin (TA beta CyD), 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-TA beta CyD 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-TA beta CyD 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 approximate to 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. (c) 2007 Elsevier B.V. All rights reserved.
引用
收藏
页码:480 / 486
页数:7
相关论文
共 21 条
[21]   METFORMIN IN THE DIGESTIVE-TRACT [J].
VIDON, N ;
CHAUSSADE, S ;
NOEL, M ;
FRANCHISSEUR, C ;
HUCHET, B ;
BERNIER, JJ .
DIABETES RESEARCH AND CLINICAL PRACTICE, 1988, 4 (03) :223-229