Purpose <p>The purpose of the current research work was to develop controlled-release tablets of lornoxicam using polymers Carbopol^® 934 and Ethocel^® grade 7.</p> Methods <p>They were prepared by the direct compression method. The formulation mixture was analyzed by using Fourier transform infrared (FTIR) and differential scanning calorimeter (DSC). They were evaluated for weight uniformity, friability, thickness, breaking force, diameter, and dissolution. Drug release patterns incorporated numerous kinetic models. The optimized tablets (F5) and reference tablets were given to healthy male rabbits, F5 to group I and reference to group II. The drug and ingredients were compatible using DSC and FTIR.</p> Results <p>Physical characteristics met the USP ranges. In the dissolution study, the drug profile was extended over 24 h. The F5 pharmacokinetic parameters were Cmax, Tmax, AUCo-24, AUCo-∞, T1/2, and Cl, which were 1316 ± 0.16 (µg/mL), 6.8 ± 0.26 (h), 5016 ± 0.32 (µg/mL), 7345 ± 0.16 (µg.h/mL), 11.64 ± 0.28 (h), and 0.021 ± 0.36 (mL/min), respectively. The reference tablets’ Cmax, Tmax, AUCo-24, AUCo-∞, T1/2, and Cl were 1299 ± 0.41 (µg/mL), 1.9 ± 0.28 (h), 4985 ± 0.25 (µg/mL), 6981 ± 0.06 (µg.h/mL), 3.98 ± 0.32 (h), and 0.023 ± 0.13 (mL/min), respectively.</p> Conclusion <p>It is concluded from this research work that controlled-release tablets might reduce dosing frequency and improve patient compliance and therapeutic outcomes.</p>