Formulation Development and Optimization of Reservoir Type Extended Release Oral Solid Dosage Form Of Highly Soluble Anti-Diabetic Drug

Abstract

Extended release (ER) drug delivery has been extensively used as a substitute to conventional dosage forms in the treatment of type 2 diabetes mellitus, a common chronic metabolic disease. It has become a promising strategy for orally administered drugs having a shorter half-life and a high dosing frequency, and also helps in the maintenance of steady state levels. The objective of this research is to formulate reservoir type ER tablet of first line antihyperglycemic agent using wet granulation technique. The core tablets were coated using rate controlling polymers to obtain reservoir type system. Cellulose acetate, Aquacoat ECD 30, Ethyl Cellulose (10 cps & 45 cps) were evaluated as a functional coating material, along with different pore formers and plasticizers to obtain desired release rate in comparison to marketed product. Hardness, % LOD, dissolution profile and other in-vitro parameters were evaluated for the same. Similar drug release profile was seen when Ethyl Cellulose 45 cps, HPMC E5 and Dibutyl Sebacate were combined in the formulation. 23 full factorial design was used, in which independent variables were coded as X1 (Product bed temp), X2 (Spray rate), X3 (Atomization air pressure) were investigated at two levels (-1 and +1). The effect of individual variables and their interactions on in-vitro drug release (%) were studied. From the statistical analysis, product bed temperature and spray rate were found to be the most effective functional coating process parameters. Other potential parameters were investigated by OFAT design that might affect the CQAs of drug product. It was then concluded that the optimized batch was equivalent to the marketed product.