Development characterization and evaluation of floating drug delivery system of Tolbutamide

Abstract

Oral controlled release formulations impact drug delivery, especially for medicines with a small absorption window, yet avoid stomach retention. By lingering in the stomach longer, controlled release gastroretentive dose forms reduce pharmaceutical waste and improve absorption. Patient compliance, reduced plasma level volatility, lower dose intake, and less drug accumulation with local and systemic side effects are other benefits. The floating drug delivery system (FDDS) is the most practical swelling and expanding, polymeric bioadhesive, high-density, and modified-shape method. The study created and tested floating Tolbutamide microspheres to prolong medication release. Meglitinide class oral anti-diabetic RG has a half-life of 1 hour and 56% bioavailability, therefore it is quickly removed from blood circulation and requires repeated doses. Solvent diffusion-evaporation has developed floating microspheres of ethylcellulose (EC) alone and in combination with HPMC of grades 5, 100, and 4000 cps to overcome these disadvantages.
Organoleptic characteristics, melting point, drug and polymer solubility, partition coefficient, UV, and IR investigations were evaluated in preformulation. FTIR and physical inspection assessed drug-polymer compatibility. Physical property changes and medication absorption band movements were minor, eliminating out interaction. Tolbutamide -loaded microspheres (E1-E9) of EC: HPMC (5, 100, and 4000 cps) were synthesised employing polymer ratio, drug concentration, emulsifier concentration, and stirring speed. The formulations were examined for SEM, FTIR, in-vitro buoyancy, yield, entrapment efficiency, and drug release. Optimised formulation release data from all four batches was fitted to mathematical models to establish release mechanism.