Formulation development and in vitro evaluation of gastroretentive hollow microspheres of famotidine

Abstract

Background:The main aim of this study was to develop a gastroretentive, multiple-unit floating drug delivery system for a drug which is poorly absorbed from the lower gastrointestinal tract. Such a dosage form may provide an extended retention of drug in the upper gastrointestinal tract resulting in enhanced absorption and improved bioavailability.Materials and Methods:Microspheres were prepared by the emulsion solvent diffusion method. Four different ratios (1:1, 1:2, 1:3, and 1:4) from each polymer, i.e., Eudragit RL 100 (E1–E4) and cellulose acetate (C1–C4) were prepared.Results:Hollow microspheres were characterized by particle size using optical microscopy. The in vitro release data obtained for the formulations E1–E4 and C1–C4 showed good entrapment efficiency, good percentage buoyancy, and prolonged drug release. The in vitro drug release showed the highest regression coefficient values for Higuchi's model, indicating diffusion to be the predominant mechanism of drug release. The surface and cross-sectional morphology of the formulations E1-A and C1-A were determined using scanning electron microscopy.Conclusions:Thus, prepared floating hollow microspheres of famotidine may prove to be potential candidates for the multiple-unit drug delivery device adaptable for any intragastric condition.

A flexible-dose dispenser for immediate and extended release 3D printed tablets

“…It is likely that the 365 highly water-soluble drug has escaped the insoluble macromolec-366 ular matrix of Eudragit RL. Previous reports indicated that drug 367 release from Eudragit RL matrix is governed by diffusion mecha-368 nism[30][31][32][33]. Faster release pattern is demonstrated in smaller 369 size tablets (60 mg and 120 mg) compared to that of larger ones, 370 e.g.…”

Towards predicting the product quality in hot-melt extrusion: Pilot plant scale extrusion

“…The investigated formulation was a simple two-component system with an 80% mass loading of Eudragit RL PO and a 20% mass loading of famotidine. Importantly, famotidine is known to be prone to degradation right after melting ( Chordiya et al, 2011 ; Maniruzzaman et al, 2013 ; Mustafin, 2011 ; Parikh et al, 2014 ; Perpétuo et al, 2013 ; Viciosa et al, 2016 ). Hence, API degradation was expected during extrusion and was used as a quality attribute.…”

Towards predicting the product quality in hot-melt extrusion: Small scale extrusion

“…Research shows that the two components do not interact with each other ( Chordiya et al 2011 ). They are suitable candidates for the preparation of solid dispersions since the melting point of Famotidine (form B, 166°) and the expected extrusion temperature window of Eudragit RL (165–170 °C) ( Parikh et al 2014 ) are within a similar temperature range.…”