Original scientific paper

https://doi.org/10.5562/cca2413

Solubility of Gliclazide in Transcutol + Water Co-solvent Mixtures at (298.15 to 333.15) K

Nazrul Haq ; Research Center, College of Science, King Saud University, Riyadh 11451, Saudi Arabia;Department of Pharmaceutics, College of Pharmacy, King Saud University, P.O. Box 2457, Riyadh 11451, Saudi Arabia
Fars K. Alanazi ; Department of Pharmaceutics, College of Pharmacy, King Saud University, P.O. Box 2457, Riyadh 11451, Saudi Arabia;Kayyali Chair for Pharmaceutical Industry, Department of Pharmaceutics, College of Pharmacy, King Saud University, P.O. Box 2457, Riyadh 1145
Ibrahim A. Alsarra ; Research Center, College of Science, King Saud University, Riyadh 11451, Saudi Arabia;Department of Pharmaceutics, College of Pharmacy, King Saud University, P.O. Box 2457, Riyadh 11451, Saudi Arabia
Faiyaz Shakeel ; Research Center, College of Science, King Saud University, Riyadh 11451, Saudi Arabia;Department of Pharmaceutics, College of Pharmacy, King Saud University, P.O. Box 2457, Riyadh 11451, Saudi Arabia

Abstract

The aim of present investigation was to determine the mole fraction solubility of a poorly water soluble antidiabetic drug gliclazide (GLZ) in mono-solvents and various Transcutol + water co-solvent mixtures at (298.15 to 333.15) K. The experimental solubility of GLZ was measured by shake flask method and resulting data was correlated with the modified Apelblat model at each temperature studied. Good correlation was observed between the experimental data of GLZ and calculated one with absolute relative deviation in the range of (0.050 to 5.680) %. The correlation coefficients were observed in the range of 0.9966 to 0.9995 which indicated good fitting of experimental solubility data. The lowest mole fraction solubility of GLZ was observed in pure water (1.9 × 10–6 at 298.15 K) whereas the highest one was observed in pure Transcutol (11.9 × 10–3 at 298.15 K). The enthalpies and entropies for GLZ dissolution were observed as positive values in the range of (15.742 to 40.551) kJ mol–1 and (52.801 to 121.721) J mol–1 K–1, respectively in all sample matrices. These results of thermodynamic parameters indicated that the dissolution of GLZ is endothermic and an entropy-driven process. Based on current solubility data, GLZ was considered as practically insoluble (poorly soluble) in pure water and soluble in Transcutol. These preliminary studies indicated that Transcutol could be used as a co-solvent for solubility enhancement of GLZ which could help in preformulation studies and formulation development of GLZ.

Keywords

gliclazide; modified Apelblat model; solubility; thermodynamics; Transcutol

Hrčak ID:

130520

URI

https://hrcak.srce.hr/130520

Publication date:

18.11.2014.

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