Carrier particles for dry powder formulations for inhalation

Patent metadata

Field	Value
Publication number	US-10709666-B2
Application number	US-202016776020-A
Country	US
Kind code	B2
Filing date	Jan 29, 2020
Priority date	May 17, 2017
Publication date	Jul 14, 2020
Grant date	Jul 14, 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 process for preparing a granule of a physiologically acceptable excipient to be used as a carrier for dry powder formulations for inhalation, said granule having a mass diameter of from 200 to 800 micrometers and having on its surface pores with a perimeter from 70 to 300 micrometers and a diameter from 30 to 100 micrometers, a specific surface area of 0.13 to 0.20 m 2 /g, and a loading capacity equal 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%, said process comprising the following steps:
(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 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 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.

2. The process according to claim 1 , wherein said (vi) drying is performed in a microwave or in an oven under vacuum.

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

• A61K31/573

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

• A61K9/1623

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

• A61K9/145 Primary

  with organic compounds · CPC title

• A61K9/0075

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