The solid state of rebamipide: preparation, characterization, and dissolution.
Rebamipide is marketed as a peptic ulcer agent under the trade name Mucosta(R). The objective of this work was to investigate the existence of polymorphs and pseudopolymorphs of rebamipide. Two crystal forms of rebamipide were isolated by recrystallization and characterized by differential thermal analysis (DTA), thermogravimetric analysis (TG), powder X-ray diffractometry, infrared spectrometry, and nuclear magnetic resonance. The DTA curve of Form 1 showed one endothermic peak at 305.2 °C, and that of Form 2 showed one endothermic peak at 307.3 °C. The TG curve of Form 1 showed a single weight loss at 305.2 °C, which corresponded to melting. The TG curve of Form 2 also showed a single weight loss at 307.3 °C, which corresponded to melting. The melting point of Form 2 was higher than that of Form 1. In the dissolution studies in pH 6.8 buffer at 37 ± 0.5 °C, the two crystal forms showed no significant differences in dissolution. After 3 months of storage at 0, 52, and 95% RH, the two crystal forms were not transformed. After milling with a Specamill for 2 h, the two crystal forms were not transformed.
['Jeon|Seong Hyeon|SH|', 'Sohn|Young Taek|YT|']
D000409:Alanine D000897:Anti-Ulcer Agents D003460:Crystallization D004339:Drug Compounding D004355:Drug Stability D004356:Drug Storage D006863:Hydrogen-Ion Concentration D009682:Magnetic Resonance Spectroscopy D015363:Quinolones D012995:Solubility D017550:Spectroscopy, Fourier Transform Infrared D013696:Temperature D014961:X-Ray Diffraction
Rebamipide Dissolution Crystal form DTA Transformation PXRD