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Preparation and characterization of glassy celecoxib
A R Paradkar1, B Chauhan, S Yamamura
1Department of Pharmaceutics, Poona College of Pharmacy, Bharati Vidyapeeth Deemed University, Erandwane, Pune, Maharashtra State, India. arparadkar@rediffmail.com
Drug Development and Industrial Pharmacy
|August 9, 2003
Summary
Creating glassy celecoxib via melt quenching significantly enhances drug dissolution and compressibility. However, the amorphous celecoxib (glass) requires stabilization to prevent recrystallization after pulverization.
Area of Science:
- Pharmaceutical Science
- Materials Science
- Physical Chemistry
Background:
- Celecoxib is a poorly water-soluble non-steroidal anti-inflammatory drug (NSAID).
- Poor solubility often limits the bioavailability and therapeutic efficacy of drug candidates.
- Amorphous solid dispersions are a strategy to improve the dissolution of poorly soluble drugs.
Purpose of the Study:
- To transform crystalline celecoxib into a glassy (amorphous) state using melt quenching.
- To characterize the physicochemical properties of glassy celecoxib.
- To evaluate the impact of the glassy state on celecoxib's dissolution rate and compressibility.
Main Methods:
- Melt quenching technique for amorphization.
- Differential Scanning Calorimetry (DSC) for thermal analysis (glass transition temperature).
- X-ray Powder Diffraction (XRPD) for crystallinity assessment.
- Infrared (IR) Spectroscopy for structural analysis (hydrogen bonding).
- Intrinsic Dissolution Rate (IDR) studies.
- Heckel plot analysis for compressibility.
- Stability studies post-pulverization.
Main Results:
- Glass transition temperature (Tg) of celecoxib glass was determined to be 51.8°C.
- IR spectroscopy indicated significant changes in hydrogen bonding in the glassy state.
- Glassy celecoxib exhibited approximately 15-fold faster dissolution compared to its crystalline form.
- Heckel analysis revealed improved compressibility of celecoxib in the glassy state.
- Unpulverized glassy celecoxib remained stable for 3 months, but pulverization induced ~70% recrystallization within 100 hours.
Conclusions:
- Melt quenching is an effective method to produce amorphous celecoxib with enhanced dissolution and compressibility.
- The amorphous state of celecoxib offers significant advantages for drug delivery.
- Stabilization strategies are crucial to maintain the amorphous form of celecoxib after processing, especially pulverization, to prevent loss of improved properties.