Process for providing particles with reduced electrostatic charges

Patent metadata

Field	Value
Publication number	US-2023364015-A1
Application number	US-202318222641-A
Country	US
Kind code	A1
Filing date	Jul 17, 2023
Priority date	Apr 21, 2010
Publication date	Nov 16, 2023
Grant date	—

Abstract

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

First claim

1 . A process for preparing carrier particles for a dry powder formulation for inhalation, 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; and
(b) mixing said co-micronized particles with said coarse excipient particles;
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.

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 . (canceled)

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

6 - 8 . (canceled)

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

10 . A process for preparing a dry powder formulation for inhalation, comprising mixing carrier particles prepared according to claim 1 with one or more active ingredients.

11 . A process according to claim 10 , wherein said active ingredient comprises at least one β2-adrenoceptor agonist selected from the group consisting of salbutamol, terbutaline, fenoterol, salmeterol, formoterol, indacaterol, vilanterol, and milveterol.

12 . A process according to claim 10 , wherein said active ingredient comprises at least one corticosteroid selected from the group consisting of budesonide, fluticasone propionate, fluticasone furoate, mometasone furoate, beclomethasone dipropionate, and ciclesonide.

13 . A process according to claim 10 , wherein said active ingredient comprises at least one anticholinergic bronchodilators selected from the group consisting of, ipratropium bromide, tiotropium bromide oxitropium bromide, and glycopyrronium bromide.

14 . Carrier particles for a dry powder formulation for inhalation, which are prepared by a process according to claim 1 .

15 . A dry powder formulation for inhalation, which is prepared by a process according to claim 10 .

16 . A mixture of co-micronized particles comprising an excipient and an additive for use in a dry powder formulation for inhalation, said mixture having a mass charge density of -9 x10 -10 to -5 x 10 -8 nC/g, said mixture being obtainable by a process which comprises conditioning by exposure to a relative humidity of 50 to 75% at a temperature of 20 to 25° C. for a time of 24 to 60 hours.

17 . A mixture according to claim 16 , wherein said additive comprises magnesium stearate.

18 . A dry powder formulation for inhalation, comprising a mixture of co-micronized particles according to claim 16 and one or more active ingredients.

19 . A dry powder formulation for inhalation, comprising carrier particles according to claim 14 and one or more active ingredients.

20 . A dry powder inhaler, filled with a dry powder formulation according to claim 15 .

21 . A dry powder inhaler, filled with a dry powder formulation according to claim 19 .

22 . A method for the prophylaxis and/or treatment of a pulmonary disease comprising administering an effective amount of a dry powder formulation according to claim 15 to a subject in need thereof.

23 . (canceled)

24 . A method for the prophylaxis and/or treatment of a pulmonary disease comprising administering an effective amount of a dry powder formulation according to claim 18 to a subject in need thereof.

25 . (canceled)

26 . A method for the prophylaxis and/or treatment of a pulmonary disease comprising administering an effective amount of a dry powder formulation according to claim 19 to a subject in need thereof.

27 . (canceled)

Assignees

• Chiesi Farm Spa

Inventors

• Cocconi Daniela
• Musa Rossella

Classifications

• A61K9/0075 Primary

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

• A61K31/137

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

• A61K31/138

  Aryloxyalkylamines, e.g. propranolol, tamoxifen, phenoxybenzamine (atenolol A61K31/165; pindolol A61K31/404; timolol A61K31/5377) · CPC title

• A61K31/167

  having the nitrogen of a carboxamide group directly attached to the aromatic ring, e.g. lidocaine, paracetamol · CPC title

• A61K31/40

  having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil · CPC title