Tablet Formulation of a Synthesized Celecoxib Potassium Salt and Development of a Validated Method for Its Analysis

Abstract

Background: Celecoxib is a non-steroidal anti-inflammatory drug (NSAID) and cyclooxygenase-2 (COX-2) inhibitor. It is used for the treatment of rheumatoid arthritis, osteoarthritis, juvenile arthritis, and acute pain. Celecoxib has low systemic bioavailability due to its low water solubility. This study aimed to improve water solubility and dissolution profile by synthesizing a suitable celecoxib potassium salt (celecoxib–K salt). Methods: Four celecoxib salts were synthesized, and the solubility of these four salts was determined. Celecoxib– K monohydrate salt was chosen for tablet formulation. A simple and feasible reversed-phase high-performance liquid chromatography (HPLC) method was developed for the analysis of the formulated tablet and then validated according to international guidelines. The dissolution profile, shelf life, and accelerated stability studies on the formulated tablet were conducted. Results: Celecoxib–K monohydrate salt exhibited increased water solubility by more than 140-folds (0.464 mg/ml) compared with celecoxib. The in vitro dissolution profile of the formulated celecoxib–K salt tablet was totally dissolved after 10 min. The developed analytical HPLC method was a reliable and valid method with good linearity, accuracy, and precision. Moreover, it was sensitive, and the limit of detection and quantification (LOD and LOQ) were 0.001 and 0.1 mg/L, respectively. The formulated celecoxib–K monohydrate salt tablet was stable under room temperature and accelerated condition for 60 days. Conclusion: The potassium salt of celecoxib was highly increased, and the formulated tablet of celecoxib–K salt exhibited a good dissolution profile in the water. In addition, the developed HPLC method was valid and reliable for the analysis and quantification of the formulated tablet. The formulated tablet was stable both at room temperature and under stress conditions.