Acetone-assisted co-processing of meloxicam with amino acids for enhanced dissolution rate

Abstract

Meloxicam is a widely used non-steroidal anti-inflammatory agent. However, its erratic and poor dissolution delays its onset of action. Dissolution enhancement of such medicine is essential to obtain rapid pain relief. Amino acids showed high potential to enhance the dissolution rate of drugs after co-processing. Accordingly, the objective of this work was to investigate the effect of co-processing of meloxicam with arginine, cysteine, and glycine on its crystalline structure and dissolution rate. Meloxicam was mixed with increasing molar ratios of amino acids before acetone-assisted kneading. The resulting products were examined using Fourier transform infrared spectroscopy, differential scanning calorimetry, and X-ray diffraction in addition to monitoring the dissolution behavior. Combined instrumental analysis indicated salt formation with a possibility of further crystalline changes at high concentration of amino acids. Salt formation and crystalline structure modification were associated with a significant increase in the dissolution rate of meloxicam. The study introduced amino acids as potential excipients for enhanced dissolution of meloxicam after wet co-processing.

Graphical Abstract

Keywords:

• Salt formation
• co-crystallization
• amorphous
• X-ray diffraction
• analgesics

Disclosure statement

No potential conflict of interest was reported by the author(s).