(W1030-08-49) Solubility and Dissolution Improvement of Gliclazide through Complex formation with Meglumine

Purpose: Gliclazide is an oral antidiabetic drug belonging to the sulfonylurea class. It is practically insoluble in water and is classified as a Biopharmaceutics Classification System (BCS) class II drug. Gliclazide is an acidic drug with a pKa value of 5.8. The objective of this research is to improve the solubility and dissolution characteristics of gliclazide through complexation with meglumine. Meglumine is an amine sugar pharmaceutical excipient known to enhance the solubility of acidic drugs.

Methods: Two grams of gliclazide were dissolved in a hydroalcoholic solution of 44:156 ratio. In separate beaker, an equimolar amount of meglumine was dissolved in 10 ml of water. The two solutions were mixed for 30 minutes until a clear solution was obtained. This solution was then dried using a rotary evaporator, and the resulting solid complex was collected and triturated using mortar and pestle. The prepared product was characterized using Differential Scanning  Calorimeter (DSC), Fourier-Transform Infrared Spectroscopy (FTIR), and particle size analysis. Solubility and dissolution characteristics were also conducted. The prepared product was characterized using DSC, FTIR, and particle size. Solubility and dissolution characteristics were also performed.

Results: DSC and FTIR analysis confirmed the formation of the complex. The prepared product was found to be amorphous. The average particle size was 12.3 micrometers with a narrow size distribution. Solubility was significantly enhanced to 4.672 mg/ml, representing a 75-fold increase. Dissolution studies indicated that the drug achieved complete dissolution within 15 minutes.

Conclusion: Complex formation between gliclazide and meglumine is an effective strategy to enhance the solubility and dissolution rate of the gliclazide. This approach can significantly improve the drug`s biopharmaceutical properties.

Differential Scanning Calorimetry Thermograms of (A) Raw Gliclazide and (B) Gliclazide Meglumine Complex

Physicochemical Characteristics of the Raw Gliclazide and the Prepared Gliclazide Meglumine Complex

Dissolution of Raw Gliclazide and Gliclazide Meglumine Complex in 6.8 Phosphate Buffer at 37 oC