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Griseofulvin micronization and dissolution rate improvement by supercritical assisted atomization
E Reverchon1, G Della Porta, A Spada
1Dipartimento di Ingegneria Chimica e Alimentare, Università di Salerno, Via Ponte Don Melillo, 84084 Fisciano (SA), Italy. ereverchon@unisat.it
The Journal of Pharmacy and Pharmacology
|November 5, 2004
Summary
Supercritical assisted atomization (SAA) effectively micronized griseofulvin (GF) into spherical particles with controlled size and improved dissolution. This innovative process offers enhanced drug delivery potential.
Area of Science:
- Pharmaceutical Technology
- Materials Science
- Chemical Engineering
Background:
- Micronization of active pharmaceutical ingredients (APIs) is crucial for enhancing bioavailability and dissolution rates.
- Conventional methods like jet milling can lead to particle aggregation and thermal degradation.
- Supercritical assisted atomization (SAA) presents an innovative approach for particle engineering.
Purpose of the Study:
- To evaluate the performance of supercritical assisted atomization (SAA) for micronizing griseofulvin (GF) as a model compound.
- To investigate the influence of precipitation temperature and drug concentration on particle characteristics.
- To compare the dissolution profiles of SAA-processed GF with conventionally processed GF.
Main Methods:
- Supercritical assisted atomization (SAA) utilizing supercritical carbon dioxide.
- Characterization of micronized griseofulvin using HPLC-UV/vis, GC-FID, DSC, BET, and X-ray diffraction.
- Formulation of griseofulvin capsules and dissolution rate testing.
Main Results:
- SAA produced spherical griseofulvin microparticles (0.5–2.5 µm) with narrow particle size distribution.
- No drug degradation was observed, with acetone residues below 800 ppm.
- Micronized griseofulvin exhibited good stability, surface areas of 4–6 m²/g, and retained crystalline structure.
- SAA-processed griseofulvin showed faster and more reproducible dissolution rates compared to jet-milled griseofulvin.
Conclusions:
- Supercritical assisted atomization is a viable and effective method for griseofulvin micronization.
- SAA offers superior control over particle size, morphology, and dissolution properties.
- The enhanced dissolution profile of SAA-processed griseofulvin suggests improved therapeutic efficacy.