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Publication Number
US-9433576-B2
Publication Date
2016-09-06
Expiration Date
Abstract
The invention relates to respirable dry particles that contain one or more divalent metal cations, such as calcium, in an amount of less than 3% by weight, and to dry powders that contain the respirable particles. The dry particles can further contain an active agent, or can be used as carrier particles to deliver an active agent.
Core Innovation
The invention provides a respirable dry powder comprising respirable dry particles that comprise a divalent metal cation source, a pharmaceutical agent, and a pharmaceutically acceptable excipient. The respirable dry powder does not contain a phospholipid, and the divalent metal cations are provided by magnesium lactate or a calcium salt in an amount between about 0.1% and 2.9% by weight of the dry particle.
The respirable dry particles are defined by aerosol performance and physical properties measured by a RODOS/HELOS system. The particles have a volume median geometric diameter (VMGD) of 5 microns or less when measured at a dispersion pressure of 1 bar, a dispersibility ratio (1 bar/4 bar) of less than about 1.5 as measured by laser diffraction, and a tap density greater than 0.4 g/cc in the magnesium lactate embodiment and greater than 4 g/cc in the calcium salt embodiment.
The disclosed content positions the powder compositions for administration to a patient's respiratory tract for respiratory diseases and infections, including asthma, COPD, cystic fibrosis, infectious pneumonia, and influenza. The document also discusses evaluation in pneumonia, influenza, tobacco smoke COPD, sheep MCC, and mucociliary clearance models, together with aerosol metrics including MMAD, fine particle fraction, emitted dose, and Hausner ratio.
Claims Coverage
The consolidated content contains two independent claim sets, both directed to respirable dry powders with divalent-metal-salt sources, exclusion of phospholipid, and particle performance metrics measured using a RODOS/HELOS laser diffraction workflow plus tap density constraints. The independent claims differ in the divalent metal cation source and in the tap density threshold.
Magnesium lactate-based respirable dry powder with defined dispersibility and tap density
A respirable dry powder comprising respirable dry particles that comprise magnesium lactate providing magnesium ions in an amount between about 0.1% and 2.9% by weight of the dry particle, a pharmaceutical agent, and a pharmaceutically acceptable excipient, wherein the respirable dry powder does not contain a phospholipid; the respirable dry particles have a VMGD of 5 microns or less at dispersion pressure of 1 bar and a dispersibility ratio (1 bar/4 bar) of less than about 1.5 as measured by laser diffraction (RODOS/HELOS system), and a tap density greater than 0.4 g/cc.
Calcium salt-based respirable dry powder with higher tap density threshold
A respirable dry powder comprising respirable dry particles comprising a calcium salt providing divalent metal cations in an amount between about 0.1% and 2.9% by weight of the dry particle, a pharmaceutical agent, wherein the respirable dry powder does not contain phospholipid; the respirable dry particles have a VMGD of 5 microns or less at dispersion pressure of 1 bar and a dispersibility ratio (1 bar/4 bar) of less than about 1.5 as measured by laser diffraction (RODOS/HELOS system), and the respirable dry particles have a tap density greater than 4 g/cc.
Across the independent claims, coverage is directed to phospholipid-free respirable dry powders in which divalent metal cations are supplied by magnesium lactate or a calcium salt, and particle performance is constrained by VMGD (≤5 microns), dispersibility ratio (1 bar/4 bar < about 1.5) measured on RODOS/HELOS, together with specified tap density thresholds.
Stated Advantages
Improved dispersibility without added mechanical energy beyond inhalation.
Reduced non-drug carrier burden by enabling active-agent dense formulations.
Improved flow and reduced aggregation expectations, supporting passive DPI suitability.
Documented Applications
Treatment of acute exacerbation of a respiratory disease by administering an effective amount of a respirable dry powder to a patient's respiratory tract, where the respiratory disease includes asthma and COPD, among other listed respiratory conditions.
Use of the respirable dry powder for respiratory diseases and infectious respiratory diseases including infectious pneumonia and influenza, as described in the document.
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