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Physical-chemical characterization of binary systems of metformin hydrochloride with triacetyl-beta-cyclodextrin.
J Pharm Biomed Anal. 2007 Nov 05; 45(3):480-6.JP

Abstract

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.

Authors+Show Affiliations

Department of Pharmaceutical Sciences, Faculty of Pharmacy, University of Florence, via U.Schiff 6, 50019 Sesto Fiorentino, Florence, Italy.No affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info available

Pub Type(s)

Journal Article
Research Support, Non-U.S. Gov't

Language

eng

PubMed ID

17822867

Citation

Corti, Giovanna, et al. "Physical-chemical Characterization of Binary Systems of Metformin Hydrochloride With Triacetyl-beta-cyclodextrin." Journal of Pharmaceutical and Biomedical Analysis, vol. 45, no. 3, 2007, pp. 480-6.
Corti G, Capasso G, Maestrelli F, et al. Physical-chemical characterization of binary systems of metformin hydrochloride with triacetyl-beta-cyclodextrin. J Pharm Biomed Anal. 2007;45(3):480-6.
Corti, G., Capasso, G., Maestrelli, F., Cirri, M., & Mura, P. (2007). Physical-chemical characterization of binary systems of metformin hydrochloride with triacetyl-beta-cyclodextrin. Journal of Pharmaceutical and Biomedical Analysis, 45(3), 480-6.
Corti G, et al. Physical-chemical Characterization of Binary Systems of Metformin Hydrochloride With Triacetyl-beta-cyclodextrin. J Pharm Biomed Anal. 2007 Nov 5;45(3):480-6. PubMed PMID: 17822867.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Physical-chemical characterization of binary systems of metformin hydrochloride with triacetyl-beta-cyclodextrin. AU - Corti,Giovanna, AU - Capasso,Gaetano, AU - Maestrelli,Francesca, AU - Cirri,Marzia, AU - Mura,Paola, Y1 - 2007/07/20/ PY - 2007/06/16/received PY - 2007/07/13/accepted PY - 2007/9/8/pubmed PY - 2008/3/4/medline PY - 2007/9/8/entrez SP - 480 EP - 6 JF - Journal of pharmaceutical and biomedical analysis JO - J Pharm Biomed Anal VL - 45 IS - 3 N2 - 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. SN - 0731-7085 UR - https://www.unboundmedicine.com/medline/citation/17822867/Physical_chemical_characterization_of_binary_systems_of_metformin_hydrochloride_with_triacetyl_beta_cyclodextrin_ L2 - https://linkinghub.elsevier.com/retrieve/pii/S0731-7085(07)00411-6 DB - PRIME DP - Unbound Medicine ER -