Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
2487962 | Journal of Pharmaceutical Sciences | 2006 | 11 Pages |
Abstract
The aim was to investigate if solid drug/cyclodextrin complexes could be produced in a singleâstep process with a solution enhanced dispersion by supercritical fluids (SEDS) method. Budesonide and γâcyclodextrin (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°C. SEDSâprocessed powders were characterised with HPLC, DSC and XRPD for budesonide content, complexation and crystallinity. The budesonide dissolution rate was determined in 1% γâCD aqueous solution. Solid, white budesonide/γâCD 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 65â±â12% with 0.14â±â0.02 mg budesonide/mg powder, corresponding to 1:2 drug:CD molar ratio. The dissolution rate of this complexed budesonide (93â±â2% after 15 min) was markedly higher compared to unprocessed micronised budesonide (41â±â10%) and SEDSâprocessed budesonide without CD (61â±â3%). As a conclusion, SEDS is a novel method to produce solid drug/CD complexes in a singleâstep process.
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Authors
Tarja Toropainen, Sitaram Velaga, Teemu Heikkilä, Laura Matilainen, Pekka Jarho, Johan Carlfors, VesaâPekka Lehto, Tomi Järvinen, Kristiina Järvinen,