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

Nazrul Haq,Faiyaz Shakeel,Fars K Alanazi,Ibrahim A Alsarra

doi:10.5562/cca2413

Abstract

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

Highlights

The IUPAC name of gliclazide (GLZ) is 1-(3,3a,4,5,6, 6a-hexahydro - 1H - cyclopenta[c]pyrrol - 2 - yl) - 3 - (4 - methylphenyl) sulfonylurea (Figure 1, molecular formula: C15H21N3O3S, molecular mass: 323.411 g mol–1, CAS registry number: 21187-98-4).[1,2]. It is a second generation hypoglycemic agent which is prescribed in the treatment of type 2 diabetes mellitus.[1,2,3,4]. It is very poorly soluble drug according to the biopharmaceutical classification system (BCS) of drugs (BCS class II) due to which its dissolution is poor.[2,4]
The mole fraction solubility of GLZ was found to be lowest in pure water
The ∆H o values for GLZ dissolution in pure Transcutol were significantly reduced as compared to pure water. These results indicated that relatively low energy is required for solubilization of GLZ in pure Transcutol as compared to pure water

Summary

Introduction

The IUPAC name of gliclazide (GLZ) is 1-(3,3a,4,5,6, 6a-hexahydro - 1H - cyclopenta[c]pyrrol - 2 - yl) - 3 - (4 - methylphenyl) sulfonylurea (Figure 1, molecular formula: C15H21N3O3S, molecular mass: 323.411 g mol–1, CAS registry number: 21187-98-4).[1,2] It is a second generation hypoglycemic agent which is prescribed in the treatment of type 2 diabetes mellitus.[1,2,3,4] It is very poorly soluble drug according to the biopharmaceutical classification system (BCS) of drugs (BCS class II) due to which its dissolution is poor.[2,4] Poor solubility and dissolution often resulted in poor in vivo absorption of such drugs.[4]. The aim of present investigation was to determine the mole fraction solubility of GLZ in monosolvents (pure water and pure Transcutol) as well as in various Transcutol-water co-solvent mixtures at temperature range from (298.15 to 333.15) K. The experimental mole fraction solubility data was correlated with the modified Apelblat model.

Results

Conclusion