Solid state interconversion between anhydrous norfloxacin and its hydrates.
This work is focused on characterizing and evaluating the solid state interconversion of norfloxacin (NF) hydrates. Four stoichiometric NF hydrates, dihydrate, hemipentahydrate, trihydrate, pentahydrate and a disordered NF state, were generated by various methods and characterized by X-ray powder diffractometry (XRPD), thermal analysis and Karl Fisher titrimetry. XRPD patterns of all NF hydrates exhibited crystalline structures. NF hydrate conversion was studied with respect to mild elevated temperature and various degrees of moisture levels. NF hydrates transformed to anhydrous NF Form A after gentle heating at 60 degrees C for 48 h except dihydrate and trihydrate where mixture in XRPD patterns between anhydrous NF Form A and former structures existed. Desiccation of NF hydrates at 0% RH for 7 days resulted in only partial removal of water molecules from the hydrated structures. The hydrated transitional phase and the disordered NF state were obtained from the incomplete dehydration of NF hydrates after thermal treatment and pentahydrate NF after desiccation, respectively. Anhydrous NF Form A and NF hydrates transformed to pentahydrate NF when exposed to high moisture environment except dihydrate. In conclusion, surrounding moisture levels, temperatures and the duration of exposure strongly influenced the interconversion pathways and stoichiometry of anhydrous NF and its hydrates.
Chongcharoen
Wanchai
W
Faculty of Pharmaceutical Sciences, Chulalongkorn University, Bangkok, Thailand.
Byrn
Stephen R
SR
Sutanthavibul
Narueporn
N
D000900:Anti-Bacterial Agents / Q000008:administration & dosage / Q000737:chemistry*; D055598:Chemical Phenomena; D002627:Chemistry, Physical; D002851:Chromatography, High Pressure Liquid; D004055:Differential Thermal Analysis; D004339:Drug Compounding; D004355:Drug Stability; D006813:Humidity; D007202:Indicators and Reagents; D008855:Microscopy, Electron, Scanning; D009643:Norfloxacin / Q000008:administration & dosage / Q000737:chemistry*; D012995:Solubility; D017550:Spectroscopy, Fourier Transform Infrared; D013607:Tablets; D014867:Water / Q000737:chemistry; D014961:X-Ray Diffraction
D000900:Anti-Bacterial Agents; D007202:Indicators and Reagents; D013607:Tablets; D014867:Water; D009643:Norfloxacin