Development and In Vitro Characterization of Sustained-Release Tranexamic Acid Matrix Tablets Using Chitosan and HPMC K15M

Research Article

Abstract

Tranexamic acid (TXA), an antifibrinolytic agent, has a short biological half-life, which needs frequent administration and can lead to non-adherence. This investigation focused on the design and in vitro assessment of sustained-release (SR) matrix tablets for TXA to provide a 12-hour dosing interval. Two different polymeric carriers, the natural polysaccharide Chitosan and the synthetic cellulose derivative Hydroxypropyl Methylcellulose (HPMC K15M), were evaluated for their release-retarding capabilities. Ten formulations (CF1-CF5 with Chitosan; HF1-HF5 with HPMC K15M) were prepared by the direct compression method, varying the polymer concentration. Fourier Transform Infrared (FT-IR) spectroscopy confirmed the absence of chemical interactions between TXA and the excipients. All prepared formulations exhibited satisfactory pre-compression flow characteristics and post-compression parameters (weight variation, hardness, thickness, friability, and drug content) that complied with official pharmacopeial specifications. In vitro dissolution studies conducted in 0.1 N HCl for 12 hours revealed that drug release was inversely proportional to the polymer concentration. The optimized formulations, CF5 (20 mg Chitosan) and HF5 (20 mg HPMC K15M), indicated the most effective release modulation, with cumulative drug release of 94.9% ± 0.30 and 94.5% ± 1.24, respectively. Kinetic modeling of the release data indicated that both CF5 and HF5 formulations closely followed a zero-order release pattern, suggesting a constant rate of drug liberation. The results indicate that both Chitosan and HPMC K15M can be effectively employed to formulate SR matrix tablets of Tranexamic acid, with the Chitosan-based system (CF5) providing a marginally superior and highly consistent release profile suitable for twice-daily dosing.