Solubility of Gliclazide and Ion-Molecular Interactions with Aminopropanol in Aqueous Solutions
- Authors: Hamdan I.I.1, El-Sabawi D.1, Abu-Dahab R.1
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Affiliations:
- Faculty of Pharmacy
- Issue: Vol 92, No 1 (2018)
- Pages: 84-92
- Section: Physical Chemistry of Solutions
- URL: https://journals.rcsi.science/0036-0244/article/view/169864
- DOI: https://doi.org/10.1134/S0036024418010107
- ID: 169864
Cite item
Abstract
A new salt of gliclazide (GZD) was prepared and was shown to have a significantly higher aqueous solubility at physiological pH together with superior dissolution profiles in comparison to GZD employing an organic amino-alcohol base. Characterization by NMR, IR, DSC, conductometry and HPLC techniques concluded that an ion pair salt is formed between acidic GZD and basic aminopropanol (AMP). In addition to the presence of about 5% tightly bound water, hydrogen bonds appeared to form extensively between GZD, AMP and water molecules. Unlike many of solubility enhancing approaches, the salt did not hamper the permeability of GZD as shown by transport through Caco-2 cells model. In vivo studies on rats confirmed that the blood glucose lowering effect of GZD-AMP was significantly higher and more rapid compared to parent GZD indicating an enhanced overall performance of the prepared salt.
Keywords
About the authors
Imad I. Hamdan
Faculty of Pharmacy
Author for correspondence.
Email: I.hamdan@ju.edu.jo
Jordan, Amman, 11942
Dina El-Sabawi
Faculty of Pharmacy
Email: I.hamdan@ju.edu.jo
Jordan, Amman, 11942
Rana Abu-Dahab
Faculty of Pharmacy
Email: I.hamdan@ju.edu.jo
Jordan, Amman, 11942