Formulation and Evaluation of Tolterodine Tartrate SustainedRelease Pellets by Using Spheronization and Extrusion Technique

Abstract

This study aimed to formulate and evaluate sustained-release pellets of Tolterodine Tartrate using extrusion and spheroidization techniques, focusing on the tablet form for improved drug delivery. Tolterodine Tartrate, commonly used for overactive bladder treatment, requires controlled release to enhance therapeutic efficacy and patient compliance. Drug-excipient compatibility was assessed through physical observation and Fourier Transform Infrared (FTIR) spectroscopy, with no significant interactions observed. The flow properties, including bulk density, tapped density, and angle of repose, were optimized to ensure uniform pellet formation. The physicochemical evaluation of the pellets, including drug content, friability, and weight variation, met the required quality standards for tablet use. In-vitro drug release studies, conducted using the USP type I basket method, revealed that the optimized formulation (F5) exhibited a cumulative drug release of 88% after 7 hours, closely mimicking the performance of the innovator tablet formulation. Kinetic modeling of the release profiles indicated a diffusion-controlled release mechanism, fitting Zero-order and Higuchi models. Stability studies under accelerated conditions (40°C/75% RH) over 6 months showed no significant changes in the physical appearance, drug release profile, or assay values, indicating the stability of the optimized formulation. The results highlight the effectiveness of the sustained-release tablet formulation, offering a promising alternative to traditional immediate-release tablets, ensuring prolonged therapeutic effects and improved patient adherence to treatment.