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ENHANCEMENT OF ANTI-DIABETIC EFFECTS OF GLICLAZIDE USING IMMEDIATE RELEASE TABLETS IN STREPTOZOTOCIN-INDUCED DIABETIC AND NORMAL RATS

JALEH VARSHOSAZ^*, NASER TAVAKOLI, SAIDEH ENTESHARY

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Gliclazide is widely used in the treatment of non-insulin dependent diabetes mellitus. Its major drawback is the hydrophobic nature, low dissolution rate and interindividual variation in bioavailability. The objective of the present study was to enhance dissolution rate and antidiabetic effect of gliclazide using immediate release tablets. Tablets containing wetting agents like: propylene glycol (PG), ethanol (Et) and Solutol H15 (S) in ratios of 1:1, 2:1, 4:1 to drug and mixed with ProSolv (A) as filler in concentrations of 10, 15, 20% were prepared. Sodium starch glycolate as disintegrating agent was added 5% w/w. The dissolution of gliclazide in tablets was investigated in HCl 0.1 N. The blood glucose lowering effect of tablets was studied in normal and streptozotocin-diabetic rats. The developed tablets caused significantly higher drug release rate than conventional tablets due to increased wetting properties and increased surface of drug available for dissolution. Increasing the ratio of ProSolv from 10 to 20% caused to increase drug dissolution rate. The area under the normalized blood glucose level vs. time curve up to 25 hr after administration of the optimized formulation (PG)4A20 showed significant decrease in blood glucose level in both normal and diabetic rats compared to conventional tablets. The developed tablets enhance water solubility of gliclazide and its efficacy.