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|Título:||Complexation of budesonide in cyclodextrins and particle aerodynamic characterization of the complex solid form for dry powder inhalation|
|Editora:||KLUWER ACADEMIC PUBL|
|Citação:||JOURNAL OF INCLUSION PHENOMENA AND MACROCYCLIC CHEMISTRY. - Vol. 44, n. 40269 (DEC 2002), p. 111-115|
|Resumo:||The purpose of this study is to evaluate the effect of budesonide-cyclodextrins (CDs) complex formation in the in-vitro aerodynamic properties of the dry powder produced for pulmonary delivery. Phase-solubility studies were performed using budesonide and beta-CD, DM-beta-CD and HP-beta-CD. The complex budesonide:DM-beta-CD revealed the highest stability constant (K-s = 3339.7 +/- 4.76%; n = 3) and the solid powder was prepared by spray-drying. Complexation was evidenced by Differential Scanning Calorimetry (DSC). A physical mixture of budesonide and DM-beta-CD was prepared for use as reference. The fine particle fraction and particle size distribution of both powders were assessed using Twin Stage liquid Impinger (TSLI) and Aerosizer(R)LD, respectively. The content uniformity of the capsules filled (sd); (n) was 191.8 (+/- 2.74) mug; (10) for the budesonide: DM-beta-CD solid complex and 204.9 (+/- 9.35) mug; (10) for the physical mixture. The emitted dose (rsd); (n) was 68.0% (+/- 26.1%); (5) of the nominal dose (solid complex) and 70.6% (+/- 12.6%); (5) (physical mixture). The fine particle fraction was 67.7% (+/- 18.9%); (5) of the emitted dose (solid complex) and 39.8% (+/- 16.9%); (5) (physical mixture). While no statistically significant difference was observed between the emitted dose means of both the solid complex and physical mixture, a statistically significant higher fine particle fraction mean was obtained for the solid complex. The results suggest that using a spray-dried CD complex powder for pulmonary drug delivery may increase the drug's respirable fraction and consequently its therapeutic efficacy.|
|Aparece nas colecções:||FF - Produção Científica 2000-2009|
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