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Preparation of budesonide/gamma-cyclodextrin complexes in supercritical fluids with a novel SEDS method
Uppsala University, Disciplinary Domain of Medicine and Pharmacy, Faculty of Pharmacy, Department of Pharmacy.
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2006 (English)In: Journal of Pharmaceutical Sciences, ISSN 0022-3549, E-ISSN 1520-6017, Vol. 95, no 10, p. 2235-2245Article in journal (Refereed) Published
Abstract [en]

The aim was to investigate if solid drug/cyclodextrin complexes could be produced in a single-step process with a solution enhanced dispersion by supercritical fluids (SEDS) method. Budesonide and gamma-cyclodextrin (CD) solutions (50% or 99.5% ethanol) were pumped from the same (conventional method) or separate (modified method) containers together with supercritical carbon dioxide through a coaxial nozzle into a particle formation chamber. The pressure was maintained at 100, 150 or 200 bar with a temperature of 40, 60 or 80 degrees C. SEDS-processed powders were characterised with HPLC, DSC and XRPD for budesonide content, complexation and crystallinity. The budesonide dissolution rate was determined in 1% gamma-CD aqueous solution. Solid, white budesonide/gamma-CD complex particles were formed using the conventional and modified SEDS processes. The complexation efficiency was dependent on the processing conditions. For example, with the conventional method (100 bar, 60 C) the yield of the powder was 65 +/- 12% with 0.14 +/- 0.02 mg budesonide/mg powder, corresponding to 1:2 drug:CD molar ratio. The dissolution rate of this complexed budesonide (93 +/- 2% after 15 min) was markedly higher compared to unprocessed micronised budesonide (41 +/- 10%) and SEDS-processed budesonide without CD (61 +/- 3%). As a conclusion, SEDS is a novel method to produce solid drug/CD complexes in a single-step process.

Place, publisher, year, edition, pages
2006. Vol. 95, no 10, p. 2235-2245
Keywords [en]
budesonide, gamma-cyclodextrin, complex, SEDS, supercritical fluids
National Category
Pharmaceutical Sciences
Identifiers
URN: urn:nbn:se:uu:diva-81969DOI: 10.1002/jps.20702ISI: 000240811100014PubMedID: 16883551OAI: oai:DiVA.org:uu-81969DiVA, id: diva2:109884
Available from: 2006-09-06 Created: 2006-09-06 Last updated: 2018-01-13Bibliographically approved

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Carlfors, Johan

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