Carrier particles for dry powder formulations for inhalation

Patent metadata

Field	Value
Publication number	US-10583085-B2
Application number	US-201815978599-A
Country	US
Kind code	B2
Filing date	May 14, 2018
Priority date	May 17, 2017
Publication date	Mar 10, 2020
Grant date	Mar 10, 2020

Abstract

Carrier particles in the form of granules described herein are suitable for use in dry powder formulations for inhalation, and preferably administering high-strength dose active ingredients.

First claim

The invention claimed is:

1. A granule of a physiologically acceptable excipient to be used as a carrier for a dry powder formulation for inhalation, said granule having a mass diameter of from 200 to 800 micrometers and having on its surface pores with a perimeter of from 70 to 300 micrometers and a diameter of from 30 to 100 micrometers, a specific surface area of 0.13 to 0.20 m 2 /g, and a loading capacity equal to or higher than 35%, wherein said physiologically acceptable excipient is selected from the group consisting of lactose, mannitol, trehalose, dextran, glucose, and mixtures thereof; wherein said granule has a friability of less than 3%.

2. The granule according to claim 1 , which is in the form of an agglomerate consisting of a plurality of crystals fused to one another.

3. The granule according to claim 1 , wherein said mass diameter is from 300 to 600 micrometers.

4. The granule according to claim 1 , wherein said mass diameter is from 400 to 500 micrometers.

5. The granule according to claim 1 , wherein said perimeter of said pores is from 100 to 220 micrometers and said diameter of said pores is from 30 to 80 micrometers.

6. The granule according to claim 1 , wherein said physiologically acceptable excipient is alpha-lactose monohydrate or mannitol.

7. The granule according to claim 1 , obtainable by a process comprising:
(i) selecting particles of a physiologically acceptable excipient having a starting median volume diameter of at least 100 micrometers;
(ii) preparing an oversaturated aqueous solution comprising a part of said physiologically acceptable excipient having a concentration in water of from 30 to 50% w/v;
(iii) wetting the remaining part of said physiologically acceptable excipient with 10 to 25% w/w of said aqueous solution obtained in (ii), to obtain a mixture;
(iv) stirring said mixture to obtain a slurry;
(v) forcing said slurry through a sieve, to obtain a wet mass; and
vi) drying said wet mass to obtain said granules.

8. A pharmaceutical composition in form of dry powder for inhalation, comprising granules according to claim 1 and one or more active ingredients.

9. The pharmaceutical composition according to claim 8 , wherein said active ingredient is present in an amount sufficient to deliver a dose, per actuation of the inhaler, equal to or higher than 1 mg.

10. A dry powder inhaler containing a powder pharmaceutical composition according to claim 8 .

11. A dry powder inhaler containing a powder pharmaceutical composition according to claim 9 .

12. A package, containing a pharmaceutical composition according to claim 8 and a dry powder inhaler.

13. A package, containing a pharmaceutical composition according to claim 9 and a dry powder inhaler.

14. A method of treating a disease or condition of the respiratory tract, comprising administering to a subject in need thereof an effective amount of a pharmaceutical composition according to claim 8 .

15. The method accordingly to claim 14 , wherein said disease or condition of the respiratory tract is asthma or chronic obstructive pulmonary disease.

Assignees

• Chiesi Farm Spa

Inventors

• Schiaretti Francesca
• Buttini Francesca
• Bettini Ruggero
• Salomi Enrico
• Benassi Andrea

Classifications

• A61K47/26

  Carbohydrates, e.g. sugar alcohols, amino sugars, nucleic acids, mono-, di- or oligo-saccharides; Derivatives thereof, e.g. polysorbates, sorbitan fatty acid esters or glycyrrhizin · CPC title

• A61K9/145 Primary

  with organic compounds · CPC title

• A61K31/573

  substituted in position 21, e.g. cortisone, dexamethasone, prednisone or aldosterone · CPC title

• A61K9/0075

  for inhalation via a dry powder inhaler [DPI], e.g. comprising micronized drug mixed with lactose carrier particles · CPC title

• A61K9/1623

  Sugars or sugar alcohols, e.g. lactose; Derivatives thereof; Homeopathic globules · CPC title