Optimization of bilayer floating tablet containing metoprolol tartrate as a model drug for gastric retention

Abstract

The purpose of the present study was to develop an optimized gastric floating drug delivery system (GFDDS) containing metoprolol tartrate (MT) as a model drug by the optimization technique. A 2(3) factorial design was employed in formulating the GFDDS with total polymer content-to-drug ratio (X1), polymer-to-polymer ratio (X2), and different viscosity grades of hydroxypropyl methyl cellulose (HPMC) (X3) as independent variables. Four dependent variables were considered: percentage of MT release at 8 hours, T50%, diffusion coefficient, and floating time. The main effect and interaction terms were quantitatively evaluated using a mathematical model. The results indicate that X1 and X2 significantly affected the floating time and release properties, but the effect of different viscosity grades of HPMC (K4M and K10M) was nonsignificant. Regression analysis and numerical optimization were performed to identify the best formulation. Fickian release transport was confirmed as the release mechanism from the optimized formulation. The predicted values agreed well with the experimental values, and the results demonstrate the feasibility of the model in the development of GFDDS.

Crushed Puffed Rice-HPMC-Chitosan based Single-Unit Hydro-dynamically Balanced System for the Sustained Stomach Specific Delivery of Metoprolol Succinate

“…A gastroretentive is particularly useful for drugs that are primarily absorbed in the duodenum and upper jejunum segments (Narendra et al, 2006). MS is highly soluble throughout the physiological pH.…”

“…It comes under the category of Biopharmaceutical Class System (BCS) I drug which states that it is extremely soluble and highly permeable. It is, therefore, a suitable candidate with the high solubility for an Hydrodynamically Balanced System (HBS) sustained delivery systems (Ravishankar et al, 2006;Wikstrand et al, 2003).…”

Application of an anionic polymer in the formulation of floating tablets containing an alkaline model drug

“…[3][4][5][6] Several studies have been conducted on the formulations of effervescent tablets and non-effervescent tablets with prolonged GRTs. [7][8][9][10][11][12][13][14][15] Floating effervescent tablets contain sodium bicarbonate and citric acid that enable floatage of the tablet on the surface of the gastric fluid by releasing carbon dioxide upon contact with water in the GIT. Consequently, the density of the tablet decreases, resulting in floatation.…”

“…Studies on bilayer floating polymeric tablets of hydroxyl propyl methyl cellulose (HPMC) containing metoprolol tartrate as a model drug with a prolonged gastric retention time were conducted by Narendra et al 10 The results suggest that total polymer content to drug ratio and polymer to polymer ratio have a significant impact on the floating time (FT) and release properties, but that the HPMC viscosity grade had no effect. Jeganathan et al studied the non-effervescent floating tablets of tramadol hydrochloride composed of polyethylene oxide (PEO) and a combination of cationic and anionic polymethacrylate polymers Eudragit ® EPO (EE) and Eudragit ® L100-55 (EL).…”

“…Although there are numerous papers and patents concerning non-effervescent floating tablets, few of them address polyacrylates. [10][11][12][13][14][15] In the present study, the authors propose an application of polyacrylic acid in combination with granulated sorbitol for preparation of tablets presumed for prolonged release of a model alkali drug. The parallel usage of 2 effects, floatation and ionic bonding of alkali molecules, is supported in the tablets by the addition of a soluble filler -sorbitol.…”