Pharmacokinetic evaluation in mice of amorphous itraconazole-based dry powder formulations for inhalation with high bioavailability and extended lung retention
Abstract Three Itraconazole (ITZ) dry powders for inhalation (DPI) were prepared by spray-drying a mannitol solution in which the ITZ was in suspension (F1) or was in solution without (F2) or with phospholipid (PL) (F3). These powders were endotracheally insufflated in vivo at a single dose of 0.5mg...
Ausführliche Beschreibung
Autor*in: |
Duret, Christophe [verfasserIn] |
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E-Artikel |
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Sprache: |
Englisch |
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2014transfer abstract |
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Umfang: |
9 |
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Übergeordnetes Werk: |
Enthalten in: Combat periarticular tibia injury outcome study (CAPTIOUS): risk factors for reoperation and amputation after open periarticular tibia fractures - Fleming, Mark E. ELSEVIER, 2015, EJPB : official journal of the International Association for Pharmaceutical Technology, New York, NY [u.a.] |
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Übergeordnetes Werk: |
volume:86 ; year:2014 ; number:1 ; pages:46-54 ; extent:9 |
Links: |
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DOI / URN: |
10.1016/j.ejpb.2013.03.005 |
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Katalog-ID: |
ELV028228898 |
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245 | 1 | 0 | |a Pharmacokinetic evaluation in mice of amorphous itraconazole-based dry powder formulations for inhalation with high bioavailability and extended lung retention |
264 | 1 | |c 2014transfer abstract | |
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520 | |a Abstract Three Itraconazole (ITZ) dry powders for inhalation (DPI) were prepared by spray-drying a mannitol solution in which the ITZ was in suspension (F1) or was in solution without (F2) or with phospholipid (PL) (F3). These powders were endotracheally insufflated in vivo at a single dose of 0.5mg/kg for pharmacokinetic profile (lung and plasma concentration) determination in ICR CD-1 mice. ITZ was crystalline in F1 and assumed to be amorphous in the F2 and F3 formulations. F2 and F3 formulations allowed the in vitro formation of an ITZ supersaturated solution with a maximum solubility of 450±124ng/ml (F2) and 498±44ng/ml (F3), in contrast to formulation F1 (<10ng/ml). As a result of these higher solubilities, absorption into the systemic compartment after endotracheal administration was faster for formulations F2 and F3 (shorter t max) and in larger quantities compared to the F1 formulation (plasmatic AUC0–24h of 182ngh/ml, 491.5ngh/ml and 376.8ngh/ml, and t max of 60min, 30min and 5min for F1, F2 and F3, respectively). PL increased the systemic bioavailability of ITZ (determined by the AUCplasma to AUClung ratio) as a consequence of their wetting and absorption enhancement effect. ITZ lung concentrations after pulmonary administration remained higher than the targeted dose, based on the minimal inhibitory concentrations for Aspergillus fumigatus (2μg/glung), 24h post-administration for both F1 and F2 formulations. However, this was not the case for formulation F3, which exhibited a faster elimination rate from the lung, with an elimination half-life of 4.1h vs. 6.5h and 14.7h for F1 and F2, respectively. | ||
520 | |a Abstract Three Itraconazole (ITZ) dry powders for inhalation (DPI) were prepared by spray-drying a mannitol solution in which the ITZ was in suspension (F1) or was in solution without (F2) or with phospholipid (PL) (F3). These powders were endotracheally insufflated in vivo at a single dose of 0.5mg/kg for pharmacokinetic profile (lung and plasma concentration) determination in ICR CD-1 mice. ITZ was crystalline in F1 and assumed to be amorphous in the F2 and F3 formulations. F2 and F3 formulations allowed the in vitro formation of an ITZ supersaturated solution with a maximum solubility of 450±124ng/ml (F2) and 498±44ng/ml (F3), in contrast to formulation F1 (<10ng/ml). As a result of these higher solubilities, absorption into the systemic compartment after endotracheal administration was faster for formulations F2 and F3 (shorter t max) and in larger quantities compared to the F1 formulation (plasmatic AUC0–24h of 182ngh/ml, 491.5ngh/ml and 376.8ngh/ml, and t max of 60min, 30min and 5min for F1, F2 and F3, respectively). PL increased the systemic bioavailability of ITZ (determined by the AUCplasma to AUClung ratio) as a consequence of their wetting and absorption enhancement effect. ITZ lung concentrations after pulmonary administration remained higher than the targeted dose, based on the minimal inhibitory concentrations for Aspergillus fumigatus (2μg/glung), 24h post-administration for both F1 and F2 formulations. However, this was not the case for formulation F3, which exhibited a faster elimination rate from the lung, with an elimination half-life of 4.1h vs. 6.5h and 14.7h for F1 and F2, respectively. | ||
650 | 7 | |a OH-ITZ-d8 |2 Elsevier | |
650 | 7 | |a OH-ITZ |2 Elsevier | |
650 | 7 | |a PSD |2 Elsevier | |
650 | 7 | |a MMAD |2 Elsevier | |
650 | 7 | |a ITZ-d9 |2 Elsevier | |
650 | 7 | |a ITZ |2 Elsevier | |
650 | 7 | |a NGI |2 Elsevier | |
650 | 7 | |a PA |2 Elsevier | |
650 | 7 | |a SD |2 Elsevier | |
650 | 7 | |a Kel |2 Elsevier | |
650 | 7 | |a AUC0–24h |2 Elsevier | |
650 | 7 | |a SEM |2 Elsevier | |
650 | 7 | |a PK |2 Elsevier | |
650 | 7 | |a DPI |2 Elsevier | |
650 | 7 | |a MDT |2 Elsevier | |
650 | 7 | |a PL |2 Elsevier | |
650 | 7 | |a FSI |2 Elsevier | |
650 | 7 | |a T max |2 Elsevier | |
650 | 7 | |a C max |2 Elsevier | |
650 | 7 | |a HPLC |2 Elsevier | |
650 | 7 | |a DPPC |2 Elsevier | |
650 | 7 | |a PXRD |2 Elsevier | |
700 | 1 | |a Merlos, Romain |4 oth | |
700 | 1 | |a Wauthoz, Nathalie |4 oth | |
700 | 1 | |a Sebti, Thami |4 oth | |
700 | 1 | |a Vanderbist, Francis |4 oth | |
700 | 1 | |a Amighi, Karim |4 oth | |
773 | 0 | 8 | |i Enthalten in |n Elsevier |a Fleming, Mark E. ELSEVIER |t Combat periarticular tibia injury outcome study (CAPTIOUS): risk factors for reoperation and amputation after open periarticular tibia fractures |d 2015 |d EJPB : official journal of the International Association for Pharmaceutical Technology |g New York, NY [u.a.] |w (DE-627)ELV013352458 |
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2014transfer abstract |
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publishDate |
2014 |
allfields |
10.1016/j.ejpb.2013.03.005 doi GBVA2014014000015.pica (DE-627)ELV028228898 (ELSEVIER)S0939-6411(13)00092-1 DE-627 ger DE-627 rakwb eng 610 610 DE-600 610 VZ 540 530 VZ ASIEN DE-1a fid 6,25 ssgn 35.90 bkl 33.61 bkl 51.00 bkl Duret, Christophe verfasserin aut Pharmacokinetic evaluation in mice of amorphous itraconazole-based dry powder formulations for inhalation with high bioavailability and extended lung retention 2014transfer abstract 9 nicht spezifiziert zzz rdacontent nicht spezifiziert z rdamedia nicht spezifiziert zu rdacarrier Abstract Three Itraconazole (ITZ) dry powders for inhalation (DPI) were prepared by spray-drying a mannitol solution in which the ITZ was in suspension (F1) or was in solution without (F2) or with phospholipid (PL) (F3). These powders were endotracheally insufflated in vivo at a single dose of 0.5mg/kg for pharmacokinetic profile (lung and plasma concentration) determination in ICR CD-1 mice. ITZ was crystalline in F1 and assumed to be amorphous in the F2 and F3 formulations. F2 and F3 formulations allowed the in vitro formation of an ITZ supersaturated solution with a maximum solubility of 450±124ng/ml (F2) and 498±44ng/ml (F3), in contrast to formulation F1 (<10ng/ml). As a result of these higher solubilities, absorption into the systemic compartment after endotracheal administration was faster for formulations F2 and F3 (shorter t max) and in larger quantities compared to the F1 formulation (plasmatic AUC0–24h of 182ngh/ml, 491.5ngh/ml and 376.8ngh/ml, and t max of 60min, 30min and 5min for F1, F2 and F3, respectively). PL increased the systemic bioavailability of ITZ (determined by the AUCplasma to AUClung ratio) as a consequence of their wetting and absorption enhancement effect. ITZ lung concentrations after pulmonary administration remained higher than the targeted dose, based on the minimal inhibitory concentrations for Aspergillus fumigatus (2μg/glung), 24h post-administration for both F1 and F2 formulations. However, this was not the case for formulation F3, which exhibited a faster elimination rate from the lung, with an elimination half-life of 4.1h vs. 6.5h and 14.7h for F1 and F2, respectively. Abstract Three Itraconazole (ITZ) dry powders for inhalation (DPI) were prepared by spray-drying a mannitol solution in which the ITZ was in suspension (F1) or was in solution without (F2) or with phospholipid (PL) (F3). These powders were endotracheally insufflated in vivo at a single dose of 0.5mg/kg for pharmacokinetic profile (lung and plasma concentration) determination in ICR CD-1 mice. ITZ was crystalline in F1 and assumed to be amorphous in the F2 and F3 formulations. F2 and F3 formulations allowed the in vitro formation of an ITZ supersaturated solution with a maximum solubility of 450±124ng/ml (F2) and 498±44ng/ml (F3), in contrast to formulation F1 (<10ng/ml). As a result of these higher solubilities, absorption into the systemic compartment after endotracheal administration was faster for formulations F2 and F3 (shorter t max) and in larger quantities compared to the F1 formulation (plasmatic AUC0–24h of 182ngh/ml, 491.5ngh/ml and 376.8ngh/ml, and t max of 60min, 30min and 5min for F1, F2 and F3, respectively). PL increased the systemic bioavailability of ITZ (determined by the AUCplasma to AUClung ratio) as a consequence of their wetting and absorption enhancement effect. ITZ lung concentrations after pulmonary administration remained higher than the targeted dose, based on the minimal inhibitory concentrations for Aspergillus fumigatus (2μg/glung), 24h post-administration for both F1 and F2 formulations. However, this was not the case for formulation F3, which exhibited a faster elimination rate from the lung, with an elimination half-life of 4.1h vs. 6.5h and 14.7h for F1 and F2, respectively. OH-ITZ-d8 Elsevier OH-ITZ Elsevier PSD Elsevier MMAD Elsevier ITZ-d9 Elsevier ITZ Elsevier NGI Elsevier PA Elsevier SD Elsevier Kel Elsevier AUC0–24h Elsevier SEM Elsevier PK Elsevier DPI Elsevier MDT Elsevier PL Elsevier FSI Elsevier T max Elsevier C max Elsevier HPLC Elsevier DPPC Elsevier PXRD Elsevier Merlos, Romain oth Wauthoz, Nathalie oth Sebti, Thami oth Vanderbist, Francis oth Amighi, Karim oth Enthalten in Elsevier Fleming, Mark E. ELSEVIER Combat periarticular tibia injury outcome study (CAPTIOUS): risk factors for reoperation and amputation after open periarticular tibia fractures 2015 EJPB : official journal of the International Association for Pharmaceutical Technology New York, NY [u.a.] (DE-627)ELV013352458 volume:86 year:2014 number:1 pages:46-54 extent:9 https://doi.org/10.1016/j.ejpb.2013.03.005 Volltext GBV_USEFLAG_U GBV_ELV SYSFLAG_U FID-ASIEN SSG-OLC-PHA GBV_ILN_40 35.90 Festkörperchemie VZ 33.61 Festkörperphysik VZ 51.00 Werkstoffkunde: Allgemeines VZ AR 86 2014 1 46-54 9 045F 610 |
spelling |
10.1016/j.ejpb.2013.03.005 doi GBVA2014014000015.pica (DE-627)ELV028228898 (ELSEVIER)S0939-6411(13)00092-1 DE-627 ger DE-627 rakwb eng 610 610 DE-600 610 VZ 540 530 VZ ASIEN DE-1a fid 6,25 ssgn 35.90 bkl 33.61 bkl 51.00 bkl Duret, Christophe verfasserin aut Pharmacokinetic evaluation in mice of amorphous itraconazole-based dry powder formulations for inhalation with high bioavailability and extended lung retention 2014transfer abstract 9 nicht spezifiziert zzz rdacontent nicht spezifiziert z rdamedia nicht spezifiziert zu rdacarrier Abstract Three Itraconazole (ITZ) dry powders for inhalation (DPI) were prepared by spray-drying a mannitol solution in which the ITZ was in suspension (F1) or was in solution without (F2) or with phospholipid (PL) (F3). These powders were endotracheally insufflated in vivo at a single dose of 0.5mg/kg for pharmacokinetic profile (lung and plasma concentration) determination in ICR CD-1 mice. ITZ was crystalline in F1 and assumed to be amorphous in the F2 and F3 formulations. F2 and F3 formulations allowed the in vitro formation of an ITZ supersaturated solution with a maximum solubility of 450±124ng/ml (F2) and 498±44ng/ml (F3), in contrast to formulation F1 (<10ng/ml). As a result of these higher solubilities, absorption into the systemic compartment after endotracheal administration was faster for formulations F2 and F3 (shorter t max) and in larger quantities compared to the F1 formulation (plasmatic AUC0–24h of 182ngh/ml, 491.5ngh/ml and 376.8ngh/ml, and t max of 60min, 30min and 5min for F1, F2 and F3, respectively). PL increased the systemic bioavailability of ITZ (determined by the AUCplasma to AUClung ratio) as a consequence of their wetting and absorption enhancement effect. ITZ lung concentrations after pulmonary administration remained higher than the targeted dose, based on the minimal inhibitory concentrations for Aspergillus fumigatus (2μg/glung), 24h post-administration for both F1 and F2 formulations. However, this was not the case for formulation F3, which exhibited a faster elimination rate from the lung, with an elimination half-life of 4.1h vs. 6.5h and 14.7h for F1 and F2, respectively. Abstract Three Itraconazole (ITZ) dry powders for inhalation (DPI) were prepared by spray-drying a mannitol solution in which the ITZ was in suspension (F1) or was in solution without (F2) or with phospholipid (PL) (F3). These powders were endotracheally insufflated in vivo at a single dose of 0.5mg/kg for pharmacokinetic profile (lung and plasma concentration) determination in ICR CD-1 mice. ITZ was crystalline in F1 and assumed to be amorphous in the F2 and F3 formulations. F2 and F3 formulations allowed the in vitro formation of an ITZ supersaturated solution with a maximum solubility of 450±124ng/ml (F2) and 498±44ng/ml (F3), in contrast to formulation F1 (<10ng/ml). As a result of these higher solubilities, absorption into the systemic compartment after endotracheal administration was faster for formulations F2 and F3 (shorter t max) and in larger quantities compared to the F1 formulation (plasmatic AUC0–24h of 182ngh/ml, 491.5ngh/ml and 376.8ngh/ml, and t max of 60min, 30min and 5min for F1, F2 and F3, respectively). PL increased the systemic bioavailability of ITZ (determined by the AUCplasma to AUClung ratio) as a consequence of their wetting and absorption enhancement effect. ITZ lung concentrations after pulmonary administration remained higher than the targeted dose, based on the minimal inhibitory concentrations for Aspergillus fumigatus (2μg/glung), 24h post-administration for both F1 and F2 formulations. However, this was not the case for formulation F3, which exhibited a faster elimination rate from the lung, with an elimination half-life of 4.1h vs. 6.5h and 14.7h for F1 and F2, respectively. OH-ITZ-d8 Elsevier OH-ITZ Elsevier PSD Elsevier MMAD Elsevier ITZ-d9 Elsevier ITZ Elsevier NGI Elsevier PA Elsevier SD Elsevier Kel Elsevier AUC0–24h Elsevier SEM Elsevier PK Elsevier DPI Elsevier MDT Elsevier PL Elsevier FSI Elsevier T max Elsevier C max Elsevier HPLC Elsevier DPPC Elsevier PXRD Elsevier Merlos, Romain oth Wauthoz, Nathalie oth Sebti, Thami oth Vanderbist, Francis oth Amighi, Karim oth Enthalten in Elsevier Fleming, Mark E. ELSEVIER Combat periarticular tibia injury outcome study (CAPTIOUS): risk factors for reoperation and amputation after open periarticular tibia fractures 2015 EJPB : official journal of the International Association for Pharmaceutical Technology New York, NY [u.a.] (DE-627)ELV013352458 volume:86 year:2014 number:1 pages:46-54 extent:9 https://doi.org/10.1016/j.ejpb.2013.03.005 Volltext GBV_USEFLAG_U GBV_ELV SYSFLAG_U FID-ASIEN SSG-OLC-PHA GBV_ILN_40 35.90 Festkörperchemie VZ 33.61 Festkörperphysik VZ 51.00 Werkstoffkunde: Allgemeines VZ AR 86 2014 1 46-54 9 045F 610 |
allfields_unstemmed |
10.1016/j.ejpb.2013.03.005 doi GBVA2014014000015.pica (DE-627)ELV028228898 (ELSEVIER)S0939-6411(13)00092-1 DE-627 ger DE-627 rakwb eng 610 610 DE-600 610 VZ 540 530 VZ ASIEN DE-1a fid 6,25 ssgn 35.90 bkl 33.61 bkl 51.00 bkl Duret, Christophe verfasserin aut Pharmacokinetic evaluation in mice of amorphous itraconazole-based dry powder formulations for inhalation with high bioavailability and extended lung retention 2014transfer abstract 9 nicht spezifiziert zzz rdacontent nicht spezifiziert z rdamedia nicht spezifiziert zu rdacarrier Abstract Three Itraconazole (ITZ) dry powders for inhalation (DPI) were prepared by spray-drying a mannitol solution in which the ITZ was in suspension (F1) or was in solution without (F2) or with phospholipid (PL) (F3). These powders were endotracheally insufflated in vivo at a single dose of 0.5mg/kg for pharmacokinetic profile (lung and plasma concentration) determination in ICR CD-1 mice. ITZ was crystalline in F1 and assumed to be amorphous in the F2 and F3 formulations. F2 and F3 formulations allowed the in vitro formation of an ITZ supersaturated solution with a maximum solubility of 450±124ng/ml (F2) and 498±44ng/ml (F3), in contrast to formulation F1 (<10ng/ml). As a result of these higher solubilities, absorption into the systemic compartment after endotracheal administration was faster for formulations F2 and F3 (shorter t max) and in larger quantities compared to the F1 formulation (plasmatic AUC0–24h of 182ngh/ml, 491.5ngh/ml and 376.8ngh/ml, and t max of 60min, 30min and 5min for F1, F2 and F3, respectively). PL increased the systemic bioavailability of ITZ (determined by the AUCplasma to AUClung ratio) as a consequence of their wetting and absorption enhancement effect. ITZ lung concentrations after pulmonary administration remained higher than the targeted dose, based on the minimal inhibitory concentrations for Aspergillus fumigatus (2μg/glung), 24h post-administration for both F1 and F2 formulations. However, this was not the case for formulation F3, which exhibited a faster elimination rate from the lung, with an elimination half-life of 4.1h vs. 6.5h and 14.7h for F1 and F2, respectively. Abstract Three Itraconazole (ITZ) dry powders for inhalation (DPI) were prepared by spray-drying a mannitol solution in which the ITZ was in suspension (F1) or was in solution without (F2) or with phospholipid (PL) (F3). These powders were endotracheally insufflated in vivo at a single dose of 0.5mg/kg for pharmacokinetic profile (lung and plasma concentration) determination in ICR CD-1 mice. ITZ was crystalline in F1 and assumed to be amorphous in the F2 and F3 formulations. F2 and F3 formulations allowed the in vitro formation of an ITZ supersaturated solution with a maximum solubility of 450±124ng/ml (F2) and 498±44ng/ml (F3), in contrast to formulation F1 (<10ng/ml). As a result of these higher solubilities, absorption into the systemic compartment after endotracheal administration was faster for formulations F2 and F3 (shorter t max) and in larger quantities compared to the F1 formulation (plasmatic AUC0–24h of 182ngh/ml, 491.5ngh/ml and 376.8ngh/ml, and t max of 60min, 30min and 5min for F1, F2 and F3, respectively). PL increased the systemic bioavailability of ITZ (determined by the AUCplasma to AUClung ratio) as a consequence of their wetting and absorption enhancement effect. ITZ lung concentrations after pulmonary administration remained higher than the targeted dose, based on the minimal inhibitory concentrations for Aspergillus fumigatus (2μg/glung), 24h post-administration for both F1 and F2 formulations. However, this was not the case for formulation F3, which exhibited a faster elimination rate from the lung, with an elimination half-life of 4.1h vs. 6.5h and 14.7h for F1 and F2, respectively. OH-ITZ-d8 Elsevier OH-ITZ Elsevier PSD Elsevier MMAD Elsevier ITZ-d9 Elsevier ITZ Elsevier NGI Elsevier PA Elsevier SD Elsevier Kel Elsevier AUC0–24h Elsevier SEM Elsevier PK Elsevier DPI Elsevier MDT Elsevier PL Elsevier FSI Elsevier T max Elsevier C max Elsevier HPLC Elsevier DPPC Elsevier PXRD Elsevier Merlos, Romain oth Wauthoz, Nathalie oth Sebti, Thami oth Vanderbist, Francis oth Amighi, Karim oth Enthalten in Elsevier Fleming, Mark E. ELSEVIER Combat periarticular tibia injury outcome study (CAPTIOUS): risk factors for reoperation and amputation after open periarticular tibia fractures 2015 EJPB : official journal of the International Association for Pharmaceutical Technology New York, NY [u.a.] (DE-627)ELV013352458 volume:86 year:2014 number:1 pages:46-54 extent:9 https://doi.org/10.1016/j.ejpb.2013.03.005 Volltext GBV_USEFLAG_U GBV_ELV SYSFLAG_U FID-ASIEN SSG-OLC-PHA GBV_ILN_40 35.90 Festkörperchemie VZ 33.61 Festkörperphysik VZ 51.00 Werkstoffkunde: Allgemeines VZ AR 86 2014 1 46-54 9 045F 610 |
allfieldsGer |
10.1016/j.ejpb.2013.03.005 doi GBVA2014014000015.pica (DE-627)ELV028228898 (ELSEVIER)S0939-6411(13)00092-1 DE-627 ger DE-627 rakwb eng 610 610 DE-600 610 VZ 540 530 VZ ASIEN DE-1a fid 6,25 ssgn 35.90 bkl 33.61 bkl 51.00 bkl Duret, Christophe verfasserin aut Pharmacokinetic evaluation in mice of amorphous itraconazole-based dry powder formulations for inhalation with high bioavailability and extended lung retention 2014transfer abstract 9 nicht spezifiziert zzz rdacontent nicht spezifiziert z rdamedia nicht spezifiziert zu rdacarrier Abstract Three Itraconazole (ITZ) dry powders for inhalation (DPI) were prepared by spray-drying a mannitol solution in which the ITZ was in suspension (F1) or was in solution without (F2) or with phospholipid (PL) (F3). These powders were endotracheally insufflated in vivo at a single dose of 0.5mg/kg for pharmacokinetic profile (lung and plasma concentration) determination in ICR CD-1 mice. ITZ was crystalline in F1 and assumed to be amorphous in the F2 and F3 formulations. F2 and F3 formulations allowed the in vitro formation of an ITZ supersaturated solution with a maximum solubility of 450±124ng/ml (F2) and 498±44ng/ml (F3), in contrast to formulation F1 (<10ng/ml). As a result of these higher solubilities, absorption into the systemic compartment after endotracheal administration was faster for formulations F2 and F3 (shorter t max) and in larger quantities compared to the F1 formulation (plasmatic AUC0–24h of 182ngh/ml, 491.5ngh/ml and 376.8ngh/ml, and t max of 60min, 30min and 5min for F1, F2 and F3, respectively). PL increased the systemic bioavailability of ITZ (determined by the AUCplasma to AUClung ratio) as a consequence of their wetting and absorption enhancement effect. ITZ lung concentrations after pulmonary administration remained higher than the targeted dose, based on the minimal inhibitory concentrations for Aspergillus fumigatus (2μg/glung), 24h post-administration for both F1 and F2 formulations. However, this was not the case for formulation F3, which exhibited a faster elimination rate from the lung, with an elimination half-life of 4.1h vs. 6.5h and 14.7h for F1 and F2, respectively. Abstract Three Itraconazole (ITZ) dry powders for inhalation (DPI) were prepared by spray-drying a mannitol solution in which the ITZ was in suspension (F1) or was in solution without (F2) or with phospholipid (PL) (F3). These powders were endotracheally insufflated in vivo at a single dose of 0.5mg/kg for pharmacokinetic profile (lung and plasma concentration) determination in ICR CD-1 mice. ITZ was crystalline in F1 and assumed to be amorphous in the F2 and F3 formulations. F2 and F3 formulations allowed the in vitro formation of an ITZ supersaturated solution with a maximum solubility of 450±124ng/ml (F2) and 498±44ng/ml (F3), in contrast to formulation F1 (<10ng/ml). As a result of these higher solubilities, absorption into the systemic compartment after endotracheal administration was faster for formulations F2 and F3 (shorter t max) and in larger quantities compared to the F1 formulation (plasmatic AUC0–24h of 182ngh/ml, 491.5ngh/ml and 376.8ngh/ml, and t max of 60min, 30min and 5min for F1, F2 and F3, respectively). PL increased the systemic bioavailability of ITZ (determined by the AUCplasma to AUClung ratio) as a consequence of their wetting and absorption enhancement effect. ITZ lung concentrations after pulmonary administration remained higher than the targeted dose, based on the minimal inhibitory concentrations for Aspergillus fumigatus (2μg/glung), 24h post-administration for both F1 and F2 formulations. However, this was not the case for formulation F3, which exhibited a faster elimination rate from the lung, with an elimination half-life of 4.1h vs. 6.5h and 14.7h for F1 and F2, respectively. OH-ITZ-d8 Elsevier OH-ITZ Elsevier PSD Elsevier MMAD Elsevier ITZ-d9 Elsevier ITZ Elsevier NGI Elsevier PA Elsevier SD Elsevier Kel Elsevier AUC0–24h Elsevier SEM Elsevier PK Elsevier DPI Elsevier MDT Elsevier PL Elsevier FSI Elsevier T max Elsevier C max Elsevier HPLC Elsevier DPPC Elsevier PXRD Elsevier Merlos, Romain oth Wauthoz, Nathalie oth Sebti, Thami oth Vanderbist, Francis oth Amighi, Karim oth Enthalten in Elsevier Fleming, Mark E. ELSEVIER Combat periarticular tibia injury outcome study (CAPTIOUS): risk factors for reoperation and amputation after open periarticular tibia fractures 2015 EJPB : official journal of the International Association for Pharmaceutical Technology New York, NY [u.a.] (DE-627)ELV013352458 volume:86 year:2014 number:1 pages:46-54 extent:9 https://doi.org/10.1016/j.ejpb.2013.03.005 Volltext GBV_USEFLAG_U GBV_ELV SYSFLAG_U FID-ASIEN SSG-OLC-PHA GBV_ILN_40 35.90 Festkörperchemie VZ 33.61 Festkörperphysik VZ 51.00 Werkstoffkunde: Allgemeines VZ AR 86 2014 1 46-54 9 045F 610 |
allfieldsSound |
10.1016/j.ejpb.2013.03.005 doi GBVA2014014000015.pica (DE-627)ELV028228898 (ELSEVIER)S0939-6411(13)00092-1 DE-627 ger DE-627 rakwb eng 610 610 DE-600 610 VZ 540 530 VZ ASIEN DE-1a fid 6,25 ssgn 35.90 bkl 33.61 bkl 51.00 bkl Duret, Christophe verfasserin aut Pharmacokinetic evaluation in mice of amorphous itraconazole-based dry powder formulations for inhalation with high bioavailability and extended lung retention 2014transfer abstract 9 nicht spezifiziert zzz rdacontent nicht spezifiziert z rdamedia nicht spezifiziert zu rdacarrier Abstract Three Itraconazole (ITZ) dry powders for inhalation (DPI) were prepared by spray-drying a mannitol solution in which the ITZ was in suspension (F1) or was in solution without (F2) or with phospholipid (PL) (F3). These powders were endotracheally insufflated in vivo at a single dose of 0.5mg/kg for pharmacokinetic profile (lung and plasma concentration) determination in ICR CD-1 mice. ITZ was crystalline in F1 and assumed to be amorphous in the F2 and F3 formulations. F2 and F3 formulations allowed the in vitro formation of an ITZ supersaturated solution with a maximum solubility of 450±124ng/ml (F2) and 498±44ng/ml (F3), in contrast to formulation F1 (<10ng/ml). As a result of these higher solubilities, absorption into the systemic compartment after endotracheal administration was faster for formulations F2 and F3 (shorter t max) and in larger quantities compared to the F1 formulation (plasmatic AUC0–24h of 182ngh/ml, 491.5ngh/ml and 376.8ngh/ml, and t max of 60min, 30min and 5min for F1, F2 and F3, respectively). PL increased the systemic bioavailability of ITZ (determined by the AUCplasma to AUClung ratio) as a consequence of their wetting and absorption enhancement effect. ITZ lung concentrations after pulmonary administration remained higher than the targeted dose, based on the minimal inhibitory concentrations for Aspergillus fumigatus (2μg/glung), 24h post-administration for both F1 and F2 formulations. However, this was not the case for formulation F3, which exhibited a faster elimination rate from the lung, with an elimination half-life of 4.1h vs. 6.5h and 14.7h for F1 and F2, respectively. Abstract Three Itraconazole (ITZ) dry powders for inhalation (DPI) were prepared by spray-drying a mannitol solution in which the ITZ was in suspension (F1) or was in solution without (F2) or with phospholipid (PL) (F3). These powders were endotracheally insufflated in vivo at a single dose of 0.5mg/kg for pharmacokinetic profile (lung and plasma concentration) determination in ICR CD-1 mice. ITZ was crystalline in F1 and assumed to be amorphous in the F2 and F3 formulations. F2 and F3 formulations allowed the in vitro formation of an ITZ supersaturated solution with a maximum solubility of 450±124ng/ml (F2) and 498±44ng/ml (F3), in contrast to formulation F1 (<10ng/ml). As a result of these higher solubilities, absorption into the systemic compartment after endotracheal administration was faster for formulations F2 and F3 (shorter t max) and in larger quantities compared to the F1 formulation (plasmatic AUC0–24h of 182ngh/ml, 491.5ngh/ml and 376.8ngh/ml, and t max of 60min, 30min and 5min for F1, F2 and F3, respectively). PL increased the systemic bioavailability of ITZ (determined by the AUCplasma to AUClung ratio) as a consequence of their wetting and absorption enhancement effect. ITZ lung concentrations after pulmonary administration remained higher than the targeted dose, based on the minimal inhibitory concentrations for Aspergillus fumigatus (2μg/glung), 24h post-administration for both F1 and F2 formulations. However, this was not the case for formulation F3, which exhibited a faster elimination rate from the lung, with an elimination half-life of 4.1h vs. 6.5h and 14.7h for F1 and F2, respectively. OH-ITZ-d8 Elsevier OH-ITZ Elsevier PSD Elsevier MMAD Elsevier ITZ-d9 Elsevier ITZ Elsevier NGI Elsevier PA Elsevier SD Elsevier Kel Elsevier AUC0–24h Elsevier SEM Elsevier PK Elsevier DPI Elsevier MDT Elsevier PL Elsevier FSI Elsevier T max Elsevier C max Elsevier HPLC Elsevier DPPC Elsevier PXRD Elsevier Merlos, Romain oth Wauthoz, Nathalie oth Sebti, Thami oth Vanderbist, Francis oth Amighi, Karim oth Enthalten in Elsevier Fleming, Mark E. ELSEVIER Combat periarticular tibia injury outcome study (CAPTIOUS): risk factors for reoperation and amputation after open periarticular tibia fractures 2015 EJPB : official journal of the International Association for Pharmaceutical Technology New York, NY [u.a.] (DE-627)ELV013352458 volume:86 year:2014 number:1 pages:46-54 extent:9 https://doi.org/10.1016/j.ejpb.2013.03.005 Volltext GBV_USEFLAG_U GBV_ELV SYSFLAG_U FID-ASIEN SSG-OLC-PHA GBV_ILN_40 35.90 Festkörperchemie VZ 33.61 Festkörperphysik VZ 51.00 Werkstoffkunde: Allgemeines VZ AR 86 2014 1 46-54 9 045F 610 |
language |
English |
source |
Enthalten in Combat periarticular tibia injury outcome study (CAPTIOUS): risk factors for reoperation and amputation after open periarticular tibia fractures New York, NY [u.a.] volume:86 year:2014 number:1 pages:46-54 extent:9 |
sourceStr |
Enthalten in Combat periarticular tibia injury outcome study (CAPTIOUS): risk factors for reoperation and amputation after open periarticular tibia fractures New York, NY [u.a.] volume:86 year:2014 number:1 pages:46-54 extent:9 |
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Combat periarticular tibia injury outcome study (CAPTIOUS): risk factors for reoperation and amputation after open periarticular tibia fractures |
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Duret, Christophe @@aut@@ Merlos, Romain @@oth@@ Wauthoz, Nathalie @@oth@@ Sebti, Thami @@oth@@ Vanderbist, Francis @@oth@@ Amighi, Karim @@oth@@ |
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These powders were endotracheally insufflated in vivo at a single dose of 0.5mg/kg for pharmacokinetic profile (lung and plasma concentration) determination in ICR CD-1 mice. ITZ was crystalline in F1 and assumed to be amorphous in the F2 and F3 formulations. F2 and F3 formulations allowed the in vitro formation of an ITZ supersaturated solution with a maximum solubility of 450±124ng/ml (F2) and 498±44ng/ml (F3), in contrast to formulation F1 (<10ng/ml). As a result of these higher solubilities, absorption into the systemic compartment after endotracheal administration was faster for formulations F2 and F3 (shorter t max) and in larger quantities compared to the F1 formulation (plasmatic AUC0–24h of 182ngh/ml, 491.5ngh/ml and 376.8ngh/ml, and t max of 60min, 30min and 5min for F1, F2 and F3, respectively). PL increased the systemic bioavailability of ITZ (determined by the AUCplasma to AUClung ratio) as a consequence of their wetting and absorption enhancement effect. ITZ lung concentrations after pulmonary administration remained higher than the targeted dose, based on the minimal inhibitory concentrations for Aspergillus fumigatus (2μg/glung), 24h post-administration for both F1 and F2 formulations. However, this was not the case for formulation F3, which exhibited a faster elimination rate from the lung, with an elimination half-life of 4.1h vs. 6.5h and 14.7h for F1 and F2, respectively.</subfield></datafield><datafield tag="520" ind1=" " ind2=" "><subfield code="a">Abstract Three Itraconazole (ITZ) dry powders for inhalation (DPI) were prepared by spray-drying a mannitol solution in which the ITZ was in suspension (F1) or was in solution without (F2) or with phospholipid (PL) (F3). These powders were endotracheally insufflated in vivo at a single dose of 0.5mg/kg for pharmacokinetic profile (lung and plasma concentration) determination in ICR CD-1 mice. ITZ was crystalline in F1 and assumed to be amorphous in the F2 and F3 formulations. 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pharmacokinetic evaluation in mice of amorphous itraconazole-based dry powder formulations for inhalation with high bioavailability and extended lung retention |
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Pharmacokinetic evaluation in mice of amorphous itraconazole-based dry powder formulations for inhalation with high bioavailability and extended lung retention |
abstract |
Abstract Three Itraconazole (ITZ) dry powders for inhalation (DPI) were prepared by spray-drying a mannitol solution in which the ITZ was in suspension (F1) or was in solution without (F2) or with phospholipid (PL) (F3). These powders were endotracheally insufflated in vivo at a single dose of 0.5mg/kg for pharmacokinetic profile (lung and plasma concentration) determination in ICR CD-1 mice. ITZ was crystalline in F1 and assumed to be amorphous in the F2 and F3 formulations. F2 and F3 formulations allowed the in vitro formation of an ITZ supersaturated solution with a maximum solubility of 450±124ng/ml (F2) and 498±44ng/ml (F3), in contrast to formulation F1 (<10ng/ml). As a result of these higher solubilities, absorption into the systemic compartment after endotracheal administration was faster for formulations F2 and F3 (shorter t max) and in larger quantities compared to the F1 formulation (plasmatic AUC0–24h of 182ngh/ml, 491.5ngh/ml and 376.8ngh/ml, and t max of 60min, 30min and 5min for F1, F2 and F3, respectively). PL increased the systemic bioavailability of ITZ (determined by the AUCplasma to AUClung ratio) as a consequence of their wetting and absorption enhancement effect. ITZ lung concentrations after pulmonary administration remained higher than the targeted dose, based on the minimal inhibitory concentrations for Aspergillus fumigatus (2μg/glung), 24h post-administration for both F1 and F2 formulations. However, this was not the case for formulation F3, which exhibited a faster elimination rate from the lung, with an elimination half-life of 4.1h vs. 6.5h and 14.7h for F1 and F2, respectively. |
abstractGer |
Abstract Three Itraconazole (ITZ) dry powders for inhalation (DPI) were prepared by spray-drying a mannitol solution in which the ITZ was in suspension (F1) or was in solution without (F2) or with phospholipid (PL) (F3). These powders were endotracheally insufflated in vivo at a single dose of 0.5mg/kg for pharmacokinetic profile (lung and plasma concentration) determination in ICR CD-1 mice. ITZ was crystalline in F1 and assumed to be amorphous in the F2 and F3 formulations. F2 and F3 formulations allowed the in vitro formation of an ITZ supersaturated solution with a maximum solubility of 450±124ng/ml (F2) and 498±44ng/ml (F3), in contrast to formulation F1 (<10ng/ml). As a result of these higher solubilities, absorption into the systemic compartment after endotracheal administration was faster for formulations F2 and F3 (shorter t max) and in larger quantities compared to the F1 formulation (plasmatic AUC0–24h of 182ngh/ml, 491.5ngh/ml and 376.8ngh/ml, and t max of 60min, 30min and 5min for F1, F2 and F3, respectively). PL increased the systemic bioavailability of ITZ (determined by the AUCplasma to AUClung ratio) as a consequence of their wetting and absorption enhancement effect. ITZ lung concentrations after pulmonary administration remained higher than the targeted dose, based on the minimal inhibitory concentrations for Aspergillus fumigatus (2μg/glung), 24h post-administration for both F1 and F2 formulations. However, this was not the case for formulation F3, which exhibited a faster elimination rate from the lung, with an elimination half-life of 4.1h vs. 6.5h and 14.7h for F1 and F2, respectively. |
abstract_unstemmed |
Abstract Three Itraconazole (ITZ) dry powders for inhalation (DPI) were prepared by spray-drying a mannitol solution in which the ITZ was in suspension (F1) or was in solution without (F2) or with phospholipid (PL) (F3). These powders were endotracheally insufflated in vivo at a single dose of 0.5mg/kg for pharmacokinetic profile (lung and plasma concentration) determination in ICR CD-1 mice. ITZ was crystalline in F1 and assumed to be amorphous in the F2 and F3 formulations. F2 and F3 formulations allowed the in vitro formation of an ITZ supersaturated solution with a maximum solubility of 450±124ng/ml (F2) and 498±44ng/ml (F3), in contrast to formulation F1 (<10ng/ml). As a result of these higher solubilities, absorption into the systemic compartment after endotracheal administration was faster for formulations F2 and F3 (shorter t max) and in larger quantities compared to the F1 formulation (plasmatic AUC0–24h of 182ngh/ml, 491.5ngh/ml and 376.8ngh/ml, and t max of 60min, 30min and 5min for F1, F2 and F3, respectively). PL increased the systemic bioavailability of ITZ (determined by the AUCplasma to AUClung ratio) as a consequence of their wetting and absorption enhancement effect. ITZ lung concentrations after pulmonary administration remained higher than the targeted dose, based on the minimal inhibitory concentrations for Aspergillus fumigatus (2μg/glung), 24h post-administration for both F1 and F2 formulations. However, this was not the case for formulation F3, which exhibited a faster elimination rate from the lung, with an elimination half-life of 4.1h vs. 6.5h and 14.7h for F1 and F2, respectively. |
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ITZ lung concentrations after pulmonary administration remained higher than the targeted dose, based on the minimal inhibitory concentrations for Aspergillus fumigatus (2μg/glung), 24h post-administration for both F1 and F2 formulations. However, this was not the case for formulation F3, which exhibited a faster elimination rate from the lung, with an elimination half-life of 4.1h vs. 6.5h and 14.7h for F1 and F2, respectively.</subfield></datafield><datafield tag="520" ind1=" " ind2=" "><subfield code="a">Abstract Three Itraconazole (ITZ) dry powders for inhalation (DPI) were prepared by spray-drying a mannitol solution in which the ITZ was in suspension (F1) or was in solution without (F2) or with phospholipid (PL) (F3). These powders were endotracheally insufflated in vivo at a single dose of 0.5mg/kg for pharmacokinetic profile (lung and plasma concentration) determination in ICR CD-1 mice. ITZ was crystalline in F1 and assumed to be amorphous in the F2 and F3 formulations. F2 and F3 formulations allowed the in vitro formation of an ITZ supersaturated solution with a maximum solubility of 450±124ng/ml (F2) and 498±44ng/ml (F3), in contrast to formulation F1 (<10ng/ml). As a result of these higher solubilities, absorption into the systemic compartment after endotracheal administration was faster for formulations F2 and F3 (shorter t max) and in larger quantities compared to the F1 formulation (plasmatic AUC0–24h of 182ngh/ml, 491.5ngh/ml and 376.8ngh/ml, and t max of 60min, 30min and 5min for F1, F2 and F3, respectively). PL increased the systemic bioavailability of ITZ (determined by the AUCplasma to AUClung ratio) as a consequence of their wetting and absorption enhancement effect. ITZ lung concentrations after pulmonary administration remained higher than the targeted dose, based on the minimal inhibitory concentrations for Aspergillus fumigatus (2μg/glung), 24h post-administration for both F1 and F2 formulations. 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