Abstract

STUDIES ON FORMULATION OF GLIMEPIRIDE SUSTAINED RELEASE TABLETS USING HPMC K4M and HPC 75-100

Dr. Ch. Saibabu*, Dr. K. Thejomoorthy and Padige Uttej

Abstract

Glimepiride is an oral blood glucose lowering drug of sulfonylurea. Used as an adjunct to diet and exercise to lower the blood glucose in patient with Type 2 diabetes mellitus. Hypoglycemia cannot be controlled by diet and exercise alone. Glimepiride may be used concomitantly with Metformin. Glimepiride, a widely prescribed anti diabetic drug belongs to class II under BCS classification and exhibit low and variable oral bioavailability due to its poor aqueous solubility. It needs control in the dissolution rate in its formulation development to provide long therapeutic effect. In the present study HPMC K4M, HPC 75-100 and in combination with Dicalcium phosphate, PVP K30 and Aerosil were tried to control the dissolution rate of glimepiride in its tablet formulation development. The objective of the study is to prepare sustained release formulation. There are nine formulations[1] employing selected combinations of the HPMC K4M, HPC 75-100 and in combination with Dicalcium phosphate, PVP K30 and Aerosil were formulated. The tablets were prepared by direct compression method and were evaluated. The physical parameters[2] of the Glimepiride tablets evaluated and hardness of the tablets was in the range 5.1-6.1 kg /cm2. Weight loss in the friability test was less than 0.14% in all the cases. Glimepiride content of the tablets prepared was within 96.26±3%. Much variations were observed in the swelling and dissolution characteristics of the Glimepiride tablets prepared. Dissolution rate of Glimepiride tablets prepared was studied from all the tablets prepared followed first order kinetics with coefficient of determination (R2) values above 0.996. The first order dissolution rate constant (K1) values were estimated from the slope of the first order linear plots. Much variations were observed in the dissolution rate (K1) of the tablets prepared due to formulation variables. The K1 values indicated that the individual and combined effects of the dissolution rate of Glimepiride tablets are highly significant (P < 0.01). Glimepiride tablet formulations F9 gave sustained release of Glimepiride others. These tablets (F9) shown 12 hours dissolution profile and found stabile in accelerated condition also.

Keywords: Glimepiride tablets, Sustained release, HPMC K4M, HPC 75-100, Dicalcium phosphate, PVP K30 and Aerosil.