Process for providing particles with reduced electrostatic charges

Patent metadata

Field	Value
Publication number	US-2019216731-A1
Application number	US-201916360479-A
Country	US
Kind code	A1
Filing date	Mar 21, 2019
Priority date	Apr 21, 2010
Publication date	Jul 18, 2019
Grant date	—

Abstract

Carrier particles for dry powder formulations for inhalation having reduced electrostatic charges are prepared.

First claim

1 . A process for preparing a dry powder formulation for inhalation,
said dry powder formulation comprising: formoterol fumarate dihydrate, beclomethasone dipropionate, and carrier particles, said carrier particles comprising: (i) a fraction of co-micronized particles made of a mixture of an excipient and an additive, the mixture having a mass median diameter (MMD) lower than 20 microns; and (ii) a fraction of coarse excipient particles having a MMD equal to or higher than 80 microns, said process comprising: (a) co-micronizing particles of said excipient and particles of said additive, to obtain co-micronized particles; (b) mixing said co-micronized particles with said coarse excipient particles, to obtain said carrier particles; and (c) mixing said carrier particles with said formoterol fumarate dihydrate and beclomethasone dipropionate; wherein said co-micronized particles are first conditioned by exposure to a relative humidity of 50 to 75% at a temperature of 20 to 25° C. for a time of 6 to 60 hours, prior to said mixing (b).

2 . A process according to claim 1 , wherein said co-micronized particles are conditioned by exposure to a relative humidity of 55 to 70% for a time of 24 to 48 hours.

3 . A process according to claim 1 , wherein said additive comprises magnesium stearate.

4 . A process according to claim 2 , wherein said additive comprises magnesium stearate.

5 . A process according to claim 1 , wherein said excipient comprises alpha-lactose monohydrate.

6 . A process according to claim 2 , wherein said excipient comprises alpha-lactose monohydrate.

7 . A process according to claim 3 , wherein said excipient comprises alpha-lactose monohydrate.

8 . A process according to claim 4 , wherein said excipient comprises alpha-lactose monohydrate.

9 . A process according to claim 1 , wherein said coarse excipient particles have a mass diameter of 212 to 355 microns.

10 - 12 . (canceled)

13 . A process according to claim 1 , wherein said dry powder formulation further comprises at least one anticholinergic bronchodilator selected from the group consisting of, ipratropium bromide, tiotropium bromide oxitropium bromide, and glycopyrronium bromide.

14 - 27 . (canceled)

Assignees

• Chiesi Farm Spa

Inventors

• Cocconi Daniela
• Musa Rossella

Classifications

• A61K31/137

  Arylalkylamines, e.g. amphetamine, epinephrine, salbutamol, ephedrine {or methadone} · CPC title

• A61K31/58

  containing heterocyclic rings, e.g. danazol, stanozolol, pancuronium or digitogenin (digitoxin {A61K31/7048}) · CPC title

• A61K9/0075 Primary

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

• A61K31/56

  Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids · CPC title

• A61K31/439

  the ring forming part of a bridged ring system, e.g. quinuclidine (8-azabicyclo [3.2.1] octanes A61K31/46) · CPC title