Production and Characterization of ITZ‐based Solid Dispersions as DPIs DPIs were produced by spra... more Production and Characterization of ITZ‐based Solid Dispersions as DPIs DPIs were produced by spray‐drying an hydro‐alcoholic solution of mannitol with or without phospholipids with ITZ in solution or suspension using a B‐191‐a Mini Spray‐Dryer (Büchi Laboratory‐Techniques, Flawil, Switzerland). Conclusion These studies (Duret et al., Eur J Pharm Biopharm 2012; Duret et al., Eur J Pharm Biopharm 2013) demonstrated that DPIs based on solid dispersion with amorphous ITZ and without phospholipids could present adequate aerodynamic particle size, increased ITZ aqueous solubility and therefore an extended ITZ lung retention. Moreover, an insufflated ITZ dose of 5mg/kg/48h in a highly aggressive murine model of invasive pulmonary Aspergillosis exerts a similar prophylactic efficacy as the gold standard oral voriconazole at a dose of 12.5 mg/kg/12h. Solid dispersions containing amorphous ITZ with or without phospholipids increase ITZ dissolution profile and ITZ aqueous solubility
The aim of the study was to develop an efficient combination antibiotic formulation containing to... more The aim of the study was to develop an efficient combination antibiotic formulation containing tobramycin and clarithromycin as a dry powder for inhalation. A carrier-free formulation of the two drugs was produced by spray-drying and characterised for its aerodynamic behaviour by impaction tests with an NGI and release profiles. The particle size distribution, morphological evaluation and crystallinity state were determined by laser diffraction, scanning electron microscopy and powder X-ray diffraction, respectively. Drug deposition profiles were similar for the two antibiotics, which has a synergistic effect, allowing them to reach the target simultaneously at the expected dose. The release profiles show that tobramycin and clarithromycin should probably dissolve without any difficulties in vivo in the lung as 95% of tobramycin and 57% of clarithromycin mass dissolved in 10min for the spray-dried formulation. The FPF increased from 35% and 31% for the physical blend for tobramycin and clarithromycin, respectively, to 65% and 63% for the spray-dried formulation. The spray-dried formulation shows particularly high deposition results, even at sub-optimal inspiratory flow rates, and therefore, represents an attractive alternative in the local treatment of lung infection such as in cystic fibrosis.
European Journal of Pharmaceutics and Biopharmaceutics, 2006
The present study relates to compositions of solid lipidic microparticles (SLmP), composed of bio... more The present study relates to compositions of solid lipidic microparticles (SLmP), composed of biocompatible phospholipids and cholesterol, and their use as carriers or as fillers delivering drugs directly to the lungs via a dry powder inhaler (DPI). SLmP were obtained by spray-drying and were formulated as lipidic matrices entrapping budesonide or as physical blends (drug carrier). They were developed in
Production and Characterization of ITZ‐based Solid Dispersions as DPIs DPIs were produced by spra... more Production and Characterization of ITZ‐based Solid Dispersions as DPIs DPIs were produced by spray‐drying an hydro‐alcoholic solution of mannitol with or without phospholipids with ITZ in solution or suspension using a B‐191‐a Mini Spray‐Dryer (Büchi Laboratory‐Techniques, Flawil, Switzerland). Conclusion These studies (Duret et al., Eur J Pharm Biopharm 2012; Duret et al., Eur J Pharm Biopharm 2013) demonstrated that DPIs based on solid dispersion with amorphous ITZ and without phospholipids could present adequate aerodynamic particle size, increased ITZ aqueous solubility and therefore an extended ITZ lung retention. Moreover, an insufflated ITZ dose of 5mg/kg/48h in a highly aggressive murine model of invasive pulmonary Aspergillosis exerts a similar prophylactic efficacy as the gold standard oral voriconazole at a dose of 12.5 mg/kg/12h. Solid dispersions containing amorphous ITZ with or without phospholipids increase ITZ dissolution profile and ITZ aqueous solubility
The aim of the study was to develop an efficient combination antibiotic formulation containing to... more The aim of the study was to develop an efficient combination antibiotic formulation containing tobramycin and clarithromycin as a dry powder for inhalation. A carrier-free formulation of the two drugs was produced by spray-drying and characterised for its aerodynamic behaviour by impaction tests with an NGI and release profiles. The particle size distribution, morphological evaluation and crystallinity state were determined by laser diffraction, scanning electron microscopy and powder X-ray diffraction, respectively. Drug deposition profiles were similar for the two antibiotics, which has a synergistic effect, allowing them to reach the target simultaneously at the expected dose. The release profiles show that tobramycin and clarithromycin should probably dissolve without any difficulties in vivo in the lung as 95% of tobramycin and 57% of clarithromycin mass dissolved in 10min for the spray-dried formulation. The FPF increased from 35% and 31% for the physical blend for tobramycin and clarithromycin, respectively, to 65% and 63% for the spray-dried formulation. The spray-dried formulation shows particularly high deposition results, even at sub-optimal inspiratory flow rates, and therefore, represents an attractive alternative in the local treatment of lung infection such as in cystic fibrosis.
European Journal of Pharmaceutics and Biopharmaceutics, 2006
The present study relates to compositions of solid lipidic microparticles (SLmP), composed of bio... more The present study relates to compositions of solid lipidic microparticles (SLmP), composed of biocompatible phospholipids and cholesterol, and their use as carriers or as fillers delivering drugs directly to the lungs via a dry powder inhaler (DPI). SLmP were obtained by spray-drying and were formulated as lipidic matrices entrapping budesonide or as physical blends (drug carrier). They were developed in
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