Abstract:

The aim of this study was to prepare pellets of gliclazide by extrusion spheronization process by use of two methods in situ cross linking method and interfacial complexation method and to study the effect of different cross linking agents on the formed pellets. Extrusion/spheronization being an established technique for producing spherical pellets so this technique was used to prepare pellets. The gliclazide pellets prepared by extrusion-spheronization techniques and then the formed pellets were coated with pectin solution by interfacial complexation method. The effect of cross-linkers calcium chloride and aluminium chloride concentration, by in situ cross linking on properties of gliclazide pellets like swelling and drug release were studied. The formed pellets were subjected to swelling, analysis of morphology, in dissolution and vivo studies. Most of the pellets were of acceptable shape. From the results calcium chloride when coated with pectin, retarded drug release. As the concentration of calcium chloride increased, it led to slow release of the drug. This may be due to the water solubility of calcium salt, which induced cross linking with pectin. Thus pellets with calcium chloride cross linked with pectin were beneficial, because it retarded the release of the drug. Though the release from interfacial coated pellets was retarded, it was less as compared to the in situ formed pellets. The in vivo studies on alloxan-induced diabetic rats indicated the significant hypoglycemic effect that was observed 24 h after oral administration of optimized pellets. Thus, the developed and optimized pellets were suitable for prolonged systemic absorption of gliclazide to maintain lower blood glucose level and improved patient compliance. The results suggested that the in situ cross linking pellets were able to retard the release of gliclazide greater than the interfacial complexation method. Therefore, this approach has been effectively achieved.

Key words: Extrusion-spheronization, Gliclazide, Pellets, Pectin, Anti-diabetic activity