Studies on development and characterization of gastroretentive drug delivery system for antibiotics: Cefdinir

Aims/objective

Oral SR gastroretentive dosage forms offer many advantages for drugs having absorption from upper GIT and improve the bioavailability of medications that are characterized by narrow absorption window. Cefdinir is a third generation cephalosporin with broad spectrum of activity with low bioavailability (20–30%) and short biological half life (1–2 h). It has better absorption from upper part of gastrointestinal tract. The purpose of present study was to formulate and develop a new GRDDS using bilayered tablet technology for cefdinir as a model drug.

Methods

Cefdinir bilayer tablets (CBT) were prepared by using double compression cup and core method. First layer, floating matrix layer contained different rate retarding polymers and effervescent mixture. Second layer is loading layer contained cefdinir and fast releasing components (soluble starch, sodium bicarbonate and citric acid). All CBT were evaluated for their pre and post compression parameters.

Results

Precompression and post compression parameter of all CBT were within the pharmacopeial limits. In vitro buoyancy behavior and matrix integrity study revealed that FLT of optimized formulation was 1.57 ± 0.52 min and the tablet remained floatable throughout the study. In vitro drug release of optimized CBT follows initially first order release upto 30 min (till their release of loading layer), then zero order release upto 12 h and kinetic profile followed the Peppas (R² = 0.9838) and zero order (R² = 0.9986). FTIR studies revealed no drug–excipients interactions. Stability studies conducted for optimized formulation did not show any change in physical appearance, drug content, floatability, matrix integrity.

Conclusion

Kinetics of CBT showed biphasic release in the first phase, immediate dose was released in less than 60 min and second phase was released from matrix layer as a controlled zero order fashion. Cefdinir is a suitable drug for development of gastroretentive bilayer tablet.