114 ISSN: 2347-7881 PharmaTutor Magazine | Vol. 2, Issue 12 | magazine.pharmatutor.org Research Article Formulation and Evaluation of Gastroretentive Drug Delivery System of Cefuroxime Axetil Balay Ragini*, A.Pavani, R.Raja Reddy Department of Pharmaceutics, Malla Reddy Pharmacy College, Maisammaguda(via-hakimpet), Secunderabad, Telengana, India *ragini.balay@gmail.com ABSTRACT Cefuroxime Axetil is a second generation antibacterial belongs to Cephalosporin Group. The drug undergoes rapid metabolism in intestinal mucosa due to change in pH Environment and hence has decreased oral bioavailability. The aim of present investigation is to increase the gastric residence time by preparing gastroretentive tablets here by improving bioavailability of Cefuroxime Axetil. A simple UV spectrophotometric method has been employed for the estimation of Cefuroxime Axetil at 281 nm. A floating drug delivery system (FDDS) was developed using gas-forming agents, like sodium bicarbonate, sodium alginate and hydrocolloids like hydroxyl propyl methyl cellulose (HPMC) and guggul. The prepared tablets were evaluated in terms of their precompression parameters, physical characteristics, In vitro release, buoyancy lag-time and swelling index. The formulations were optimized for the different grades of HPMC, and its concentrations and combinations. The results of the In vitro release studies showed that the optimized formulation F3 could sustain drug release of 92% and remain buoyant for 10h. The optimized formulation was subjected to various kinetic release investigations and it was found that the mechanism of drug release was predominately Higuhci with non fickian diffusion. Finally the tablets formulations found to be economical and may overcome the draw backs associated with the drug during its absorption. Keywords: Gastroretentive Drug Delivery System, Cefuroxime Axetil, lag time INTRODUCTION The Floating drug delivery system (FDDS) is one of the Gastroretentive technique becomes most promising drug delivery to improve the bioavailability of drug which is unstable in the intestinal environment and also FDDS provides prolonged drug release by increasing the residence time of the drug in GIT due to its buoyancy capacity in stomach fluid. [1, 2] To achieve the buoyancy of dosage form in stomach fluid, the dosage form should have less density than the density of stomach fluid which is approximately 1.004 g/cc. The drugs which are unstable in intestine and the drug with short biological half-life are more suitable for the floating drug delivery system [3,4]. Cefuroxime Axetil (CA) is 1-acetoxyethyl ester of ab- lactamase-stable cephalosporin, cefuroxime with a broadspectrum of activity against Gram- positive and Gram-negative microorganisms. After oral administration CA is absorbed and rapidly hydrolyzed by esterases to produce cefuroxime. The 1-acetoxyethylester group at 4th position of CA ensures lipophilicity and promotes the absorption of cefuroxime but at the same time compromises on solubility and hence, the prodrug shows poor and variable oral bioavailability. [5] CA exists in crystalline as well as amorphous forms; of these, latter exhibits higher bioavailability owing to How to cite this article: R Balay, A Pavani, RR Reddy; Formulation and Evaluation of Gastroretentive Drug Delivery System of Cefuroxime Axetil; PharmaTutor; 2014; 2(12); 114-122