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          Institute: MPI für Herz- und Lungenforschung (W. G. Kerckhoff Institut)     Collection: Yearbook_2015     Display Documents



ID: 711927.0, MPI für Herz- und Lungenforschung (W. G. Kerckhoff Institut) / Yearbook_2015
Nebulization of active pharmaceutical ingredients with the eFlow((R)) rapid: impact of formulation variables on aerodynamic characteristics
Authors:Beck-Broichsitter, M.; Prufer, N.; Oesterheld, N.; Seeger, W.; Schmehl, T.
Date of Publication (YYYY-MM-DD):2014-08
Title of Journal:J Pharm Sci
Volume:103
Issue / Number:8
Start Page:2585
End Page:2589
Audience:Not Specified
Abstract / Description:Nebulization of active pharmaceutical ingredient (API) solutions is a well-established means to achieve pulmonary drug deposition. The current study identified the impact of formulation variables on the aerosolization performance of the eFlow((R)) rapid with special respect to optimized lung application. API formulations (including excipient-supplemented samples) were investigated for physicochemical properties, then nebulized using vibrating-mesh technology. The generated aerosol clouds were analyzed by laser diffraction. Aerosol deposition characteristics in the human respiratory tract were estimated using an algebraic model. Remarkable effects on aerosolization performance [i.e., mass median aerodynamic diameter (MMAD)] of API solutions were obtained when the sample conductivity (by API concentration and type, sodium chloride addition) and dynamic viscosity (by application of sucrose and poly(ethylene glycol) 200) were elevated. A similar influence was observed for a decline in surface tension (by ethanol addition). Thus, a defined adjustment of formulation parameters allowed for a decrease of the MMAD from approximately 8.0 mum to values as small as approximately 3.5 mum. Consequently, the pattern and efficiency of aerosol deposition in the human respiratory tract were improved. In conclusion, identification of physicochemical variables and their way of influencing vibrating-mesh nebulization has been provided to deliver a platform for tailoring aerosol characteristics and thus, advancing pulmonary therapy.
Free Keywords:Aerosols/*chemistry; Excipients/*chemistry; Humans; Lung/metabolism; *Nebulizers and Vaporizers; Particle Size; Polyethylene Glycols/chemistry; Sucrose/chemistry; Surface Tension; active pharmaceutical ingredient; aerosol manipulation; aerosols; excipients; lung deposition; mass median aerodynamic diameter; preformulation; pulmonary drug delivery; vibrating-mesh nebulizer
External Publication Status:published
Document Type:Article
Communicated by:MPI für Herz- und Lungenforschung
Affiliations:MPI für physiologische und klinische Forschung
External Affiliations:%^ 1435822045
Identifiers:ISSN:1520-6017 (Electronic) 0022-3549 (Linking) %R 10.1002/jps.24079
URL:http://www.ncbi.nlm.nih.gov/pubmed/24986144
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