Abstract
The aim of present work was to design, fabricate and characterize gastro retentive matrix tablets of Caffeine with the application of sintering technique to achieve sustained release dosage form. Caffeine, a highly water-soluble drug, which is used as a CNS stimulant, mild diuretic, and respiratory stimulant, belonging to the methyl xanthine class has been selected as a model drug. Hence in the present study, an attempt has been made to develop sustained release matrix tablets of caffeine to reduce the gastric irritation. The polymers like HPMC K4M, Eudragit L 100, Guar gum and Sodium bicarbonate, Citric acid were utilized as gas generating agents in the formulation of matrix tablets containing Caffeine by direct compression techniques and evaluated for its in-vitro drug release. The powder blend was evaluated for bulk density tapped density, compressibility index and angle of repose shows characteristic results. Formulation was optimized on the basis of acceptable tablet parameters such as hardness, friability, drug content, weight variation, Buoyancy lag time, in-vitro drug release and stability studies. The results of the present work stated that sintering caused decrease in drug release as compared to unsintered tablets. It was found that F6, L2, I2 and H4 gave better results compared to other formulations. The stability studies were carried out according to ICH guideline which indicates that the selected formulations were stable. The release data was then fitted to various mathematical models such as Hixon Crowell, Korsmeyer peppas, First order, Zero order to evaluate the kinetics and the mechanism of the drug release. Thus it could be useful to retain Caffeine in stomach, minimize the mucosal irritation by drug releasing slowly at controlled rate, reduces drug waste and better patient compliance.
