Ultra low density pulmonary powders

• US 9,539,211 B2
• Filed: 05/08/2015
• Issued: 01/10/2017
• Est. Priority Date: 11/09/2012
• Status: Active Grant

• Current Assignee: Civitas Therapeutics, Inc. (Acorda Therapeutics Incorporated)
• Original Assignee: Civitas Therapeutics, Inc. (Acorda Therapeutics Incorporated)
• Inventors: Lipp, Michael M., Batycky, Richard P.
• Primary Examiner(s): Barham, Bethany
• Assistant Examiner(s): FRAZIER, BARBARA S
• Application Number:
  US14/707,071
• Publication Number:
  US 20150342885A1
• Time in Patent Office: 613 Days
• Field of Search: None
• US Class Current: 1/1
• CPC Class Codes: A61J 3/074 Filling capsules; Related operations
• CPC Class Codes: 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
• CPC Class Codes: A61K 9/0073 Sprays or powders for inhalation; Aerolised or nebulised preparations generated by other means than thermal energy; nasal sprays A61K9/0043; inhalation of vapours of volatile or heated drugs, e.g. essential oils or nicotine, A61K9/007; devices A61M
• CPC Class Codes: A61K 9/0075 for inhalation via a dry powder inhaler [DPI], e.g. comprising micronized drug mixed with lactose carrier particles
• CPC Class Codes: A61K 9/145 with organic compounds
• CPC Class Codes: A61K 9/1611 Inorganic compounds
• CPC Class Codes: A61K 9/1617 Organic compounds, e.g. phospholipids, fats
• CPC Class Codes: A61K 9/4816 Wall or shell material
• CPC Class Codes: A61K 9/4833 Encapsulating processes; Filling of capsules mechanical aspects A61J3/07
• CPC Class Codes: A61K 9/4858 Organic compounds
• CPC Class Codes: A61P 11/06 Antiasthmatics
• CPC Class Codes: A61P 25/16 Anti-Parkinson drugs
• CPC Class Codes: B65B 1/16 by pneumatic means, e.g. by suction
• CPC Class Codes: B65B 1/26 by pneumatic means, e.g. suction
• CPC Class Codes: B65B 1/36 by volumetric devices or methods checking volume of filled material B65B1/48
• CPC Class Codes: B65B 63/028 by pneumatic means

Abstract

The invention provides pharmaceutical compositions for pulmonary delivery comprising particles containing a pharmaceutical agent and having a geometric size of greater than about 5 μm and a tap density of less than about 0.075 g/cm³. The invention also provides methods for delivering the pharmaceutical compositions of the invention to the respiratory tract of a patient.

Claims

1. A pharmaceutical composition for pulmonary delivery comprising particles of levodopa having:

a geometric size of about 8 μ

m to about 12 μ

m;

a tap density of about 0.025 g/cm³ to about 0.050 g/cm³;

a water content between 1.90 and 2.90 weight percent.

2. The pharmaceutical composition of claim 1, wherein said particles comprise a phospholipid.

3. The pharmaceutical composition of claim 1, wherein said particles comprise a salt.

4. The pharmaceutical composition of claim 1, wherein said particles comprise a surfactant.

5. The pharmaceutical composition of claim 1, wherein said particles comprise a polymer.

6. The pharmaceutical composition of claim 1, wherein said particles comprise a sugar.

7. The pharmaceutical composition of claim 1, wherein said particles have an aerodynamic diameter of between about 2.5 μ

m and 5 μ

m.

8. The pharmaceutical composition of claim 1, wherein said particles have an external surface area of about 10 m²/g to about 50 m²/g.

9. The pharmaceutical composition of claim 1, wherein said particles further comprise a salt and a phospholipid.