Enhancement of dissolution rate of gliclazide using solid dispersions with polyethylene glycol 6000.
The aim of the present study was to enhance the dissolution rate of gliclazide using its solid dispersions (SDs) with polyethylene glycol (PEG) 6000. The phase solubility behavior of gliclazide in presence of various concentrations of PEG 6000 in 0.1 N HCl was obtained at 37 degrees C. The solubility of gliclazide increased with increasing amount of PEG 6000 in water. Gibbs free energy (deltaG(o)(tr)) values were all negative, indicating the spontaneous nature of gliclazide solubilization and they decreased with increase in the PEG 6000 concentration, demonstrating that the reaction conditions became more favorable as the concentration of PEG 6000 increased. The SDs of gliclazide with PEG 6000 were prepared at 1:1, 1:2 and 1:5 (gliclazide/PEG 6000) ratio by melting-solvent method and solvent evaporation method. Evaluation of the properties of the SDs was performed by using dissolution, Fourier-transform infrared (FTIR) spectroscopy, differential scanning calorimetry (DSC) and X-ray diffraction (XRD) studies. The SDs of gliclazide with PEG 6000 exhibited enhanced dissolution rate of gliclazide, and the rate increased with increasing concentration of PEG 6000 in SDs. Mean dissolution time (MDT)of gliclazide decreased significantly after preparation of SDs and physical mixture with PEG 6000. The FTIR spectroscopic studies showed the stability of gliclazide and absence of well-defined gliclazide-PEG 6000 interaction. The DSC and XRD studies indicated the microcrystalline or amorphous state of gliclazide in SDs of gliclazide with PEG 6000.
Biswal
S
S
Royal College of Pharmacy and Health Sciences, Andhapasara Road, Berhampur, 760002 Orissa, India. sudarsan_mpharm@yahoo.co.in
Sahoo
J
J
Murthy
P N
PN
Giradkar
R P
RP
Avari
J G
JG
D002152:Calorimetry, Differential Scanning; D002626:Chemistry, Pharmaceutical; D018360:Crystallography, X-Ray; D004339:Drug Compounding; D004355:Drug Stability; D005907:Gliclazide / Q000737:chemistry*; D007004:Hypoglycemic Agents / Q000737:chemistry*; D007700:Kinetics; D011092:Polyethylene Glycols / Q000737:chemistry*; D012995:Solubility; D017550:Spectroscopy, Fourier Transform Infrared; D013678:Technology, Pharmaceutical / Q000379:methods; D013816:Thermodynamics
D007004:Hypoglycemic Agents; D011092:Polyethylene Glycols; D005907:Gliclazide