Effects of cogrinding with β-cyclodextrin on the solid state fentanyl.
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.
Ogawa
Noriko
N
Department of Physical Chemistry, Hoshi University, 4-41 Ebara 2-chome, Shinagawa-ku, Tokyo 142-8501, Japan. n-ogawa@hoshi.ac.jp
Higashi
Kenjirou
K
Nagase
Hiromasa
H
Endo
Tomohiro
T
Moribe
Kunikazu
K
Loftsson
Thorsteinn
T
Yamamoto
Keiji
K
Ueda
Haruhisa
H
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*
D000701:Analgesics, Opioid; D004304:Dosage Forms; D047392:beta-Cyclodextrins; C031215:betadex; D005283:Fentanyl