Abstract
Nifedipine is a dihydropyridine calcium channel antagonist effective in the clinical management of cardiovascular disease. Due to nifedipine's poor water solubility and erratic bioavailability, complexation with selected cyclodextrins was studied in order to overcome these limitations. The aim was to develop a quantitative structure property relationship (QSPR) to identify cyclodextrin molecular properties important in complex formation and provide a predictive tool which would be valuable during preformulation studies. The QSPR developed indicates that the major driving forces for nifedipine complexation, in addition to cyclodextrin concentration, are hydrophobicity and Van der Waals interactions (3D solubility parameters, hydrophilic surface area and differential connectivity index).
Keywords: Artificial neural networks (ANN), cyclodextrin (CD), complexation, nifedipine, phase solubility studies, quantitative structure property relationship (QSPR)
Current Drug Discovery Technologies
Title: Modeling the Effect of Selected Cyclodextrins on Nifedipine Solubility
Volume: 8 Issue: 2
Author(s): Snezana Agatonovic-Kustrin, David W. Morton, Matthew S. Worthington and Beverley D. Glass
Affiliation:
Keywords: Artificial neural networks (ANN), cyclodextrin (CD), complexation, nifedipine, phase solubility studies, quantitative structure property relationship (QSPR)
Abstract: Nifedipine is a dihydropyridine calcium channel antagonist effective in the clinical management of cardiovascular disease. Due to nifedipine's poor water solubility and erratic bioavailability, complexation with selected cyclodextrins was studied in order to overcome these limitations. The aim was to develop a quantitative structure property relationship (QSPR) to identify cyclodextrin molecular properties important in complex formation and provide a predictive tool which would be valuable during preformulation studies. The QSPR developed indicates that the major driving forces for nifedipine complexation, in addition to cyclodextrin concentration, are hydrophobicity and Van der Waals interactions (3D solubility parameters, hydrophilic surface area and differential connectivity index).
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Cite this article as:
Agatonovic-Kustrin Snezana, W. Morton David, S. Worthington Matthew and D. Glass Beverley, Modeling the Effect of Selected Cyclodextrins on Nifedipine Solubility, Current Drug Discovery Technologies 2011; 8 (2) . https://dx.doi.org/10.2174/157016311795563884
DOI https://dx.doi.org/10.2174/157016311795563884 |
Print ISSN 1570-1638 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-6220 |
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