Effects of cogrinding with β-cyclodextrin on the solid state fentanyl

✍ Scribed by Noriko Ogawa; Kenjirou Higashi; Hiromasa Nagase; Tomohiro Endo; Kunikazu Moribe; Thorsteinn Loftsson; Keiji Yamamoto; Haruhisa Ueda

• Publisher: John Wiley and Sons
• Year: 2010
• Tongue: English
• Weight: 565 KB
• Volume: 99
• Category: Article
• ISSN: 0022-3549
• DOI: 10.1002/jps.22193

✦ Synopsis

Fentanyl base and b-cyclodextrin (b-CD) were coground at 1:1 and 1:2 molar ratios (fentanyl: b-CD) and the physicochemical characteristics of the mixtures were studied using differential scanning calorimetry (DSC), Fourier transform infrared spectroscopy (FTIR), solid state 13 C nuclear magnetic resonance (NMR) spectroscopy and powder X-ray diffraction (PXRD) measurement. Additionally, portions of the coground samples were exposed to high relative humidity to investigate fentanyl and b-CD interactions. The results of DSC and PXRD analyses indicate that the ground mixtures are in an amorphous state, and the FTIR measurements show hydrogen bonding interactions between fentanyl and b-CD. Solid state 13 C NMR indicates that a fentanyl/b-CD inclusion compound is formed in the humidified mixture. Furthermore, PXRD data from the humidified mixtures are similar to the PXRD patterns from the inclusion complex.