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Supercritical fluids crystallisation of budesonide and flunisolide

Velaga, Sitaram (author)
Uppsala universitet,Institutionen för farmaci
Berger, Rolf (author)
Uppsala universitet,Oorganisk kemi,Uppsala University, Department of Materials Chemistry, Ångström Laboratory
Carlfors, Johan (author)
Uppsala universitet,Institutionen för farmaci,Uppsala University, Department of Pharmacy, BMC
 (creator_code:org_t)
2002
2002
English.
In: Pharmaceutical research. - 0724-8741 .- 1573-904X. ; 19:10, s. 1564-1571
  • Journal article (peer-reviewed)
Abstract Subject headings
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  • Purpose: Budesonide and flunisolide anhydrate were crystallized using the solution enhanced dispersion by supercritical fluids (SEDS) technique. The aim was to investigate the possibility of preparing different pure polymorphs.Methods: 0.25% w/v solutions of each drug were prepared from acetone and methanol. Operating conditions were 40-80°C and 80-200 bars. The flow rate of drug solution was 0.3 mL/min and that of CO2 was 9-25 mL/min. Sample characterizations included differential scanning calorimetry, X-ray powder diffraction, variable temperature X-ray diffraction, scanning electron microscopy, and solubility studies.Results: The particle morphology of budesonide was dependent on the nature of the solvent. SEDS processing of flunisolide with acetone at 100 bars resulted in the formation of polymorphic mixtures at 80°C and a new polymorph III at 60 C and 40°C. With methanol at 100 bars another new polymorph IV was formed with different particle morphology at 80°C and a polymorphic mixture at 60°C.Conclusion: Using the SEDS, microparticles of crystalline budesonide were prepared and new polymorphs of flunisolide were produced. Particle characteristics were controlled by the temperature, pressure and relative flow rates of drug solution and CO2.

Subject headings

NATURVETENSKAP  -- Kemi -- Oorganisk kemi (hsv//swe)
NATURAL SCIENCES  -- Chemical Sciences -- Inorganic Chemistry (hsv//eng)

Keyword

Budesonide
chemistry
Crystallization
Fluocinolone Acetonide
analogs & derivatives
chemistry
Solvents/chemistry
Inorganic chemistry
Oorganisk kemi

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ref (subject category)
art (subject category)

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