# US 9,433,576 B2 · Cationic dry powders > Agents: this data is available as JSON from the patentgrep API and MCP server — see https://patentgrep.com/llms.txt - Number: US 9,433,576 B2 - Document ID: US9433576B2 - Status: Granted - Kind: B2 - Application number: 13/876,315 - Filed: 2011-09-29 - Published: 2013-09-19 - Granted: 2016-09-06 - Earliest claimed: 2010-09-29 - Assignees: Pulmatrix, Inc. - Applicants: Michael M. Lipp; Jean C. Sung - Inventors: Michael M. Lipp; Jean C. Sung - Web page: https://patentgrep.com/patent/US9433576B2 ## CPC - A61K 9/0075: {for inhalation via a dry powder inhaler [DPI], e.g. comprising micronized drug mixed with lactose carrier particles} - A61K 9/1611: {Inorganic compounds} - A61K 31/198: Alpha-amino acids, e.g. alanine or edetic acid [EDTA] (betaine A61K31/205; proline A61K31/401; tryptophan A61K31/405; histidine A61K31/4172; peptides not degraded to individual amino acids A61K38/00) - A61K 31/5383: ortho- or peri-condensed with heterocyclic ring systems - A61K 33/06: Aluminium, calcium or magnesium; Compounds thereof {, e.g. clay} - A61K 33/14: Alkali metal chlorides; Alkaline earth metal chlorides - A61K 47/02: Inorganic compounds - A61P 11/00: Drugs for disorders of the respiratory system - A61P 11/10: Expectorants - A61K: PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES (devices or methods specially adapted for bringing pharmaceutical products into particular physical or administering forms A61J3/00; chemical aspects of, or use of materials for deodorisation of air, for disinfection or sterilisation, or for bandages, dressings, absorbent pads or surgical articles A61L; soap compositions C11D) - A61P: SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS ## 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. ## Claims ### Claim 1 A respirable dry powder comprising respirable dry particles that comprise a) magnesium lactate; wherein the magnesium lactate provides magnesium ion in an amount between about 0.1% and 2.9% by weight of the dry particle, b) a pharmaceutical agent, and c) a pharmaceutically acceptable excipient, wherein the respirable dry powder does not contain a phospholipid, and wherein the respirable dry particles have a volume median geometric diameter (VMGD) of 5 microns or less when measured at a 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 wherein the respirable dry particles have a tap density of greater than 0.4 g/cc. ### Claim 2 (depends on 1) The respirable dry powder of claim 1, wherein the respirable dry particles have a tap density of about 0.45 g/cc or greater. ### Claim 3 (depends on 1) The respirable dry powder of claim 1, wherein the respirable dry powder has a Fine Particle Fraction (FPF) of less than 5.6 microns of at least 45%. ### Claim 4 (depends on 1) The respirable dry powder of claim 1, wherein the respirable dry powder has a mass median aerodynamic diameter (MMAD) of about 5 microns or less. ### Claim 5 (depends on 1) The respirable dry powder of claim 1, wherein the excipient is present in an amount of about ≦20% by weight and comprises leucine. ### Claim 6 (depends on 1) The respirable dry powder of claim 1, wherein the excipient is present in an amount of about ≦20% by weight and comprises maltodextrin or mannitol. ### Claim 7 (depends on 1) The respirable dry powder of claim 1, wherein the pharmaceutically active agent is an antibiotic, a long-acting beta2 agonist (LABA), long-acting muscarinic antagonist (LAMA), a corticosteroid, or any combination thereof. ### Claim 8 (depends on 1) The respirable dry powder of claim 1, wherein the pharmaceutically active agent is a macromolecule. ### Claim 9 (depends on 1) The respirable dry powder of claim 1, wherein the pharmaceutically active agent is an antibody. ### Claim 10 (depends on 1) The respirable dry powder of claim 1, wherein the therapeutic agent is an antibiotic. ### Claim 11 (depends on 10) The respirable dry powder of claim 10, wherein the antibiotic is levofloxacin. ### Claim 12 (depends on 1) The respirable dry powder of claim 1, wherein the therapeutic agent is a muscarinic antagonist and beta-2 agonist (MABA). ### Claim 13 (depends on 1) The respirable dry powder of claim 1, wherein the respirable dry particles are further characterized by a capsule emitted powder mass (CEPM) of at least 80% when emitted from a passive dry powder inhaler that has a resistance of about 0.036 sqrt(kPa)/liters per minute (LPM) under the following conditions: an inhalation flowrate of 30 LPM, an inhalation volume of 1 liter using a size 3 capsule that contains a total mass of 20 mg, said total mass consisting of the respirable dry particles. ### Claim 14 (depends on 1) The respirable dry powder of claim 1, wherein the respirable dry particles are further characterized by a geometric size (Dv50) of below 6 micrometers when emitted from a passive dry powder inhaler that has a resistance of about 0.036 sqrt(kPa)/liters per minute (LPM) under the following conditions: an inhalation flowrate of 30 LPM, an inhalation volume of 1 liter using a size 3 capsule that contains a total mass of 20 mg, said total mass consisting of the respirable dry particles. ### Claim 15 (depends on 1) A method for treating a respiratory disease comprising administering to the respiratory tract of a patient in need thereof an effective amount of a respirable dry powder of claim 1, wherein the respiratory disease is asthma, airway hyperresponsiveness, seasonal allergic allergy, bronchiectasis, chronic bronchitis, emphysema, chronic obstructive pulmonary disease, or cystic fibrosis. ### Claim 16 (depends on 1) A method for treating an acute exacerbation of a respiratory disease comprising administering to the respiratory tract of a patient in need thereof an effective amount of a respirable dry powder of claim 1, wherein the respiratory disease is asthma, airway hyperresponsiveness, seasonal allergic allergy, bronchiectasis, chronic bronchitis, emphysema, chronic obstructive pulmonary disease, or cystic fibrosis. ### Claim 17 (depends on 1) A method for treating an infectious disease of the respiratory tract comprising administering to the respiratory tract of a patient in need thereof an effective amount of a respirable dry powder of claim 1. ### Claim 18 A respirable dry powder comprising respirable dry particles that comprise a) a calcium salt; wherein the calcium salt provides divalent metal cation in an amount between about 0.1% and 2.9% by weight of the dry particle, and b) a pharmaceutical agent, wherein the respirable dry powder does not contain phospholipid, and wherein the respirable dry particles have a volume median geometric diameter (VMGD) of 5 microns or less when measured at a 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 wherein the respirable dry particles have a tap density of greater than 4 g/cc. ### Claim 19 (depends on 18) The respirable dry powder of claim 18, wherein the calcium salt is calcium lactate.