"Development and Characterization of Floating Tablets of Repaglinide forthe Management of Type 2 Diabetes Mellitus"

ABSTRACTBackground: Repaglinide is a short-acting antidiabetic agent used in the management of Type 2Diabetes Mellitus. Due to its short biological half-life and frequent dosing requirement, thedevelopment of a gastroretentive floating drug delivery system can improve therapeutic efficacyby prolonging gastric residence time and sustaining drug release.Objective: The present study aimed to develop and characterize floating matrix tablets ofRepaglinide for prolonged gastric retention and controlled drug release.Methods: Floating tablets containing 10 mg of Repaglinide were prepared by direct compressionusing Hydroxypropyl Methylcellulose (HPMC K750 PH PRM and HPMC K1500 PH PRM) asrelease-retarding polymers and sodium bicarbonate as a gas-generating agent. Fourteen formulations (F1–F14) were developed and evaluated for pre-compression parameters, post-compression characteristics, buoyancy behavior, in vitro drug release, drug–excipient compatibility, and stability. FTIR and DSC studies were performed to assess compatibility andthermal characteristics of the drug.Results: FTIR and DSC analyses confirmed the absence of significant drug–excipientinteractions and demonstrated the thermal stability of Repaglinide. The prepared powder blendsexhibited satisfactory flow properties with angle of repose values ranging from 23° to 31°. Allformulations complied with pharmacopoeial requirements for weight variation, hardness,friability, and drug content. Floating lag times were below 60 seconds, and all tablets remainedbuoyant for more than 24 hours. In vitro dissolution studies revealed sustained drug release over24 hours. Among all formulations, F14 showed the best performance with a floating lag time of36 seconds, drug content of 99.18%, and cumulative drug release of 99.18% at 24 hours.Accelerated stability studies conducted at 40 ± 2°C and 75 ± 5% RH for six months indicated nosignificant changes in drug content, buoyancy, or dissolution profile.Conclusion: The optimized floating tablet formulation (F14) successfully achieved prolongedgastric retention and sustained release of Repaglinide for 24 hours. The developedgastroretentive floating drug delivery system represents a promising approach for improvingpatient compliance and therapeutic effectiveness in the management of Type 2 DiabetesMellitus.