IP Library Granted Patent US 11,103,480
Granted Patent B2
US 11,103,480 · App. 16/582,973 · Granted Aug 31, 2021

Pharmaceutical composition

Inventors: Stuart Corr (Cheshire, GB); Timothy James Noakes (Flintshire, GB)
Assignee: MEXICHEM FLUOR S.A. DE C.V.
A61K31/40A61K9/008A61K31/4704A61K31/56A61K31/573A61K45/06A61K47/10A61K47/12A61K47/24A61K47/32A61K47/58A61P11/00
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Quick Facts
Patent No.
US 11,103,480
App. No.
16/582,973
Granted
Aug 31, 2021
Kind
B2
Abstract

A pharmaceutical composition is described. The composition may include: (i) a drug component including at least one pharmaceutically acceptable salt of glycopyrrolate; and (ii) a propellant component including 1,1-difluoroethane (HFA-152a).

Claims (20)

1. A pharmaceutical composition comprising:

(i) a drug component comprising at least one pharmaceutically acceptable salt of glycopyrrolate, at least one corticosteroid selected from budesonide and beclomethasone dipropionate, and optionally at least one long acting beta-2-agonist (LABA) selected from formoterol and the pharmaceutically acceptable salts thereof; and

(ii) a propellant component comprising 1,1-difluoroethane (HFA-152a), wherein the composition contains less than 500 ppm of water and less than 1000 ppm of oxygen based on the total weight of the pharmaceutical composition.

2. The pharmaceutical composition of claim 1 , wherein the at least one pharmaceutically acceptable salt of glycopyrrolate is glycopyrronium bromide.

3. The pharmaceutical composition of claim 1 , wherein the drug component additionally comprises the at least one long acting beta-2-agonist (LABA).

4. The pharmaceutical composition of claim 1 , wherein the at least one pharmaceutically acceptable salt of glycopyrrolate, the at least one corticosteroid and the at least one long acting beta-2-agonist (LABA) where present are in a micronized form.

5. A pharmaceutical composition comprising:

(i) a drug component comprising at least one pharmaceutically acceptable salt of glycopyrrolate, at least one corticosteroid selected from budesonide and beclomethasone dipropionate, and optionally at least one long acting beta-2-agonist (LABA) selected from formoterol and the pharmaceutically acceptable salts thereof, and

(ii) a propellant component comprising 1,1-difluoroethane (HFA-152a), wherein the propellant component contains from 0.5 to 10 ppm of unsaturated impurities.

6. The pharmaceutical composition of claim 1 further comprising a surfactant component comprising at least one surfactant compound.

7. The pharmaceutical composition of claim 1 further comprising a polar excipient.

8. The pharmaceutical composition of claim 7 , wherein the polar excipient is ethanol.

9. The pharmaceutical composition of claim 1 which is free of one or more of (i) polar excipients, (ii) acid stabilisers and (iii) perforated microstructures.

10. The pharmaceutical composition of claim 1 which after storage in uncoated aluminium containers at 25° C. and 60% relative humidity for 3 months will produce less than 1.0% by weight of impurities from the degradation of the at least one pharmaceutically acceptable salt of glycopyrrolate based on the total weight of the at least one pharmaceutically acceptable salt of glycopyrrolate and the impurities.

11. The pharmaceutical composition of claim 1 which after storage in uncoated aluminium containers at 40° C. and 75% relative humidity for 3 months will produce less than 1.0% by weight of impurities from the degradation of the at least one pharmaceutically acceptable salt of glycopyrrolate based on the total weight of the at least one pharmaceutically acceptable salt of glycopyrrolate and the impurities.

12. The pharmaceutical composition of claim 1 , wherein at least 96.0% by weight of the at least one pharmaceutically acceptable salt of glycopyrrolate that is contained originally in the pharmaceutical composition immediately following preparation will be present in the composition after storage in uncoated aluminium containers at 25° C. and 60% relative humidity for 3 months and after storage in uncoated aluminium containers at 40° C. and 75% relative humidity for 3 months.

13. The pharmaceutical composition of claim 1 which when delivered from a metered dose inhaler yields a fine particle fraction of the at least one pharmaceutically acceptable salt of glycopyrrolate which is at least 40 weight % of the emitted dose of the at least one pharmaceutically acceptable salt of glycopyrrolate.

14. The pharmaceutical composition of claim 1 in the form of a suspension.

15. The pharmaceutical composition of claim 1 in the form of a solution.

16. A metered dose inhaler (MDI) fitted with a sealed and pressurized aerosol container that contains a pharmaceutical composition as claimed in claim 1 .

Assignments (1)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jun 4, 2020
From: CORR, STUART; NOAKES, TIMOTHY JAMES
To: MEXICHEM FLUOR S.A. DE C.V.
Reel/Frame 052837/0479 →
Priority Claims (2)
GB 1615917 · Sep 19, 2016 · national
GB 1620519 · Dec 2, 2016 · national
Continuity (2)
Continuation 16334158
Related Publication 20200016119A1 · Jan 16, 2020