title: Effects of cogrinding with β-cyclodextrin on the solid state fentanyl.
abstract: Fentanyl base and β-cyclodextrin (β-CD) were coground at 1:1 and 1:2 molar ratios (fentanyl: β-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 β-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 β-CD. Solid state (13)C NMR indicates that a fentanyl/β-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.
authors.affiliation: Department of Physical Chemistry, Hoshi University, 4-41 Ebara 2-chome, Shinagawa-ku, Tokyo 142-8501, Japan. n-ogawa@hoshi.ac.jp
authors.forename: Noriko
authors.initials: N
authors.lastname: Ogawa
authors.forename: Kenjirou
authors.initials: K
authors.lastname: Higashi
authors.forename: Hiromasa
authors.initials: H
authors.lastname: Nagase
authors.forename: Tomohiro
authors.initials: T
authors.lastname: Endo
authors.forename: Kunikazu
authors.initials: K
authors.lastname: Moribe
authors.forename: Thorsteinn
authors.initials: T
authors.lastname: Loftsson
authors.forename: Keiji
authors.initials: K
authors.lastname: Yamamoto
authors.forename: Haruhisa
authors.initials: H
authors.lastname: Ueda
mesh_terms: D000701:Analgesics, Opioid / Q000737:chemistry*; D002152:Calorimetry, Differential Scanning; D055598:Chemical Phenomena; D004304:Dosage Forms; D005283:Fentanyl / Q000737:chemistry*; D006813:Humidity; D006860:Hydrogen Bonding; D009682:Magnetic Resonance Spectroscopy; D015394:Molecular Structure; D017550:Spectroscopy, Fourier Transform Infrared / Q000379:methods; D013678:Technology, Pharmaceutical / Q000379:methods*; D014961:X-Ray Diffraction; D047392:beta-Cyclodextrins / Q000737:chemistry*
chemical_list: D000701:Analgesics, Opioid; D004304:Dosage Forms; D047392:beta-Cyclodextrins; C031215:betadex; D005283:Fentanyl