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 13C nuclear magnetic reso...

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Bibliographic Details
Published in:Journal of pharmaceutical sciences 2010-12, Vol.99 (12), p.5019-5029
Main Authors: Ogawa, Noriko, Higashi, Kenjirou, Nagase, Hiromasa, Endo, Tomohiro, Moribe, Kunikazu, Loftsson, Thorsteinn, Yamamoto, Keiji, Ueda, Haruhisa
Format: Article
Language:English
Subjects:
Analgesics, Opioid - chemistry
beta-Cyclodextrins - chemistry
Biological and medical sciences
Calorimetry, Differential Scanning
Chemical Phenomena
crystallization
cyclodextrins
Dosage Forms
Fentanyl - chemistry
FTIR
General pharmacology
Humidity
Hydrogen Bonding
inclusion compounds
interaction
Magnetic Resonance Spectroscopy
Medical sciences
milling
Molecular Structure
Pharmaceutical technology. Pharmaceutical industry
Pharmacology. Drug treatments
physicochemical properties
solid state NMR
Spectroscopy, Fourier Transform Infrared - methods
Technology, Pharmaceutical - methods
thermal analysis
X-Ray Diffraction
X-ray powder diffractometry
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Summary: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 13C 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 p-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 13C 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.
ISSN:0022-3549
1520-6017
DOI:10.1002/jps.22193