Drug-excipient compatibility assessment of solid formulations containing meloxicam

摘要

Abstract Meloxicam (MLX) is a non-steroidal anti-inflammatory cyclooxygenase (COX) inhibitor that is used to relieve inflammation and pain. MLX has a preferential affinity for COX-2, which is associated with a lower incidence of gastrointestinal side effects. The drug belongs to Class II of the Biopharmaceutical Classification System (BCS) in which dissolution is the limiting step of its bioavailability. In view of this classification, carrying out further studies regarding the compatibility of MLX with excipients and the mechanisms and kinetics of its degradation reactions is fundamental because any changes would directly influence the quality of the product. The aim of the present work is to evaluate solid pharmaceutical formulations containing MLX found on the market to define the more suitable excipients to improve the stability of the pharmaceutical formulations. Thermal analysis techniques were used to characterize and evaluate the compatibility between the drug and the excipients present in the market formulations. In the evaluation of its solid-state kinetics, MLX raw material under inert conditions had a shelf life of approximately 6years. In the study of compatibility between the drug and excipients, MLX was found to be incompatible with magnesium stearate after DSC analysis under binary mixtures, which was confirmed by stress studies and chromatographic analyzes. Graphical abstract Display Omitted