# US 10,945,972 B2 · Particulate materials

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- Number: US 10,945,972 B2
- Document ID: US10945972B2
- Status: Granted
- Kind: B2
- Application number: 16/222,607
- Filed: 2018-12-17
- Published: 2019-11-21
- Granted: 2021-03-16
- Earliest claimed: 2002-05-03
- Assignees: Nektar Therapeutics
- Applicants: Nektar Therapeutics
- Inventors: Peter York; Boris Yu Shekunov; Mahboob Ur Rehman; Jane Catherine Feeley
- Web page: https://patentgrep.com/patent/US10945972B2

## CPC

- A61K 31/137: Arylalkylamines, e.g. amphetamine, epinephrine, salbutamol, ephedrine {or methadone}
- A61K 9/0075: {for inhalation via a dry powder inhaler [DPI], e.g. comprising micronized drug mixed with lactose carrier particles}
- A61K 9/16: Agglomerates; Granulates; Microbeadlets {; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction (A61K9/20 takes precedence if the final form is a tablet; microspheres with drug-free outer coating, microcapsules A61K9/50; mixture of different granules, microcapsules, (coated) microparticles A61K9/5084; nanoparticles A61K9/51)}
- A61K 9/1688: {resulting in pure drug agglomerate optionally containing up to 5% of excipient}
- A61K 31/48: Ergoline derivatives, e.g. lysergic acid, ergotamine
- A61K 31/485: Morphinan derivatives, e.g. morphine, codeine
- A61K 31/4985: Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems
- A61M 15/0091: {mechanically breath-triggered}
- A61M 2202/064: Powder
- 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)
- A61M: DEVICES FOR INTRODUCING MEDIA INTO, OR ONTO, THE BODY (introducing media into or onto the bodies of animals A61D7/00; means for inserting tampons A61F13/26; devices for administering food or medicines orally A61J; containers for collecting, storing or administering blood or medical fluids A61J1/05); DEVICES FOR TRANSDUCING BODY MEDIA OR FOR TAKING MEDIA FROM THE BODY (surgery A61B; chemical aspects of surgical articles A61L); DEVICES FOR PRODUCING OR ENDING SLEEP OR STUPOR {(Electrotherapy, e.g. producing anaesthesia by the use of alternating or intermittent currents A61N1/36021)}

## Abstract

The present invention relates to active substances in particulate form, to methods for preparing them and to their uses. The present invention provides particulate powders, such as might be of use for delivery using a dry powder inhaler (DPI) or similar delivery device, having properties which may be beneficial to the DPI delivery process.

## Claims

### Claim 1

A method of administering an active substance by inhalation, said method comprising:
providing a composition comprising an active substance in particulate form suitable for administration via a dry powder inhaler, said particulates comprising:
a) a volume mean aerodynamic diameter of less than 7 microns;
b) a density less than 0.5 g/ml; and
c) a surface-to-volume ratio of at least twice that of spherical particles of the same volume diameter, and
administering said composition to the respiratory tract by oral inhalation via a dry powder inhaler.

### Claim 2 (depends on 1)

The method according to claim 1 wherein the composition is administered via a passive dry powder inhaler.

### Claim 3 (depends on 1)

The method of claim 1, wherein the dry powder inhaler is a passive dry powder inhaler, and the administering yields a fine particle fraction in the emitted dose which is at least 20% greater than that of the same active substance produced by micronisation, granulation, or solvent crystallization and having the same or smaller volume mean diameter.