Department of Pharmaceutics, Faculty of Pharmacy, Modern University for Technology and Information, Cairo, Egypt.
Department of Pharmaceutical Technology, Faculty of Pharmacy, Tanta University, Tanta, Egypt.
Pharm Dev Technol. 2020 Sep;25(7):882-891. doi: 10.1080/10837450.2020.1755982. Epub 2020 Apr 22.
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.
美洛昔康是一种广泛使用的非甾体抗炎药。然而，其不规则和较差的溶解度会延迟其作用的开始。增强这种药物的溶解度对于获得快速的疼痛缓解至关重要。氨基酸在药物共加工后显示出提高药物溶解速度的巨大潜力。因此，本工作的目的是研究美洛昔康与精氨酸、半胱氨酸和甘氨酸共加工对其晶体结构和溶解速率的影响。在丙酮辅助捏合之前，将美洛昔康与氨基酸以递增的摩尔比混合。使用傅里叶变换红外光谱、差示扫描量热法和 X 射线衍射对所得产物进行了检查，同时监测了溶解行为。联合仪器分析表明，在氨基酸浓度较高时可能形成盐，同时存在进一步的晶体变化的可能性。盐形成和晶体结构的改变与美洛昔康溶解速率的显著提高有关。该研究介绍了氨基酸作为潜在的辅料，通过湿共加工可增强美洛昔康的溶解度。
