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Solid-state investigation of fluocinolone acetonide
M Bartolomei1, M C Ramusino, P Ghetti
1Laboratorio di Chimica del Farmaco, Istituto Superiore di Sanita, Rome, Italy.
Journal of Pharmaceutical and Biomedical Analysis
|August 1, 1997
Summary
Three fluocinolone acetonide polymorphs (A, B, C) were identified using spectroscopy and X-ray diffraction. Forms A and C convert to form B upon heating, revealing distinct thermal behaviors and crystallographic relationships.
Area of Science:
- Solid-state chemistry
- Pharmaceutical sciences
- Materials characterization
Background:
- Fluocinolone acetonide is a corticosteroid with potential for polymorphism.
- Understanding crystalline forms is crucial for drug formulation and stability.
- Polymorphism can significantly impact a drug's bioavailability and efficacy.
Purpose of the Study:
- To characterize and differentiate three crystalline modifications of fluocinolone acetonide (A, B, and C).
- To investigate the thermal behavior and interconversion of these polymorphs.
- To elucidate the crystallographic relationships between the different forms.
Main Methods:
- Fourier Transform Infrared (FTIR) spectroscopy, including Micro-FTIR.
- Differential Scanning Calorimetry (DSC) and Thermogravimetry (TG-FTIR).
- X-ray diffractometry and thermomicroscopy.
Main Results:
- Fluocinolone acetonide exhibits three distinct crystalline forms (A, B, C), easily identifiable by FTIR in the 3600-3400 cm-1 range.
- Forms A and C convert to form B upon heating, with their thermal events elucidated by combined thermal analysis techniques.
- Polymorph A shows an enantiotropic relationship with B, while form C is monotropically related to B, confirmed by X-ray diffraction patterns.
Conclusions:
- The study successfully characterized three polymorphs of fluocinolone acetonide using a combination of spectroscopic and thermal analysis methods.
- Detailed preparation methods for each crystalline form are provided.
- The findings contribute to a better understanding of fluocinolone acetonide's solid-state properties and polymorphism.