USE OF A COMPOSITION COMPRISING FORMOTEROL AND BUDESONIDE FOR THE PREVENTION OR TREATMENT OF AN ACUTE CONDITION OF ASTHMA

• US 20010049396A1
• Filed: 08/18/1999
• Published: 12/06/2001
• Est. Priority Date: 06/11/1998
• Status: Abandoned Application

• Current Assignee: Astrazeneca AB (Astrazeneca PLC)
• Original Assignee: Astrazeneca AB (Astrazeneca PLC)
• Inventors: EKSTROM, TOMMY
• Application Number:
  US09/367,950
• Publication Number:
  US 20010049396A1
• Time in Patent Office: Days
• US Class Current: 514/727
• CPC Class Codes: A61K 2300/00 Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00
• CPC Class Codes: A61K 31/165 having aromatic rings, e.g. colchicine, atenolol, progabide
• CPC Class Codes: A61K 31/58 containing heterocyclic rings, e.g. danazol, stanozolol, pancuronium or digitogenin digitoxin A61K31/7048
• CPC Class Codes: A61K 45/06 Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
• CPC Class Codes: A61K 9/0075 for inhalation via a dry powder inhaler [DPI], e.g. comprising micronized drug mixed with lactose carrier particles
• CPC Class Codes: A61K 9/145 with organic compounds
• CPC Class Codes: A61P 11/00 Drugs for disorders of the respiratory system
• CPC Class Codes: A61P 11/06 Antiasthmatics
• CPC Class Codes: A61P 11/08 Bronchodilators

Abstract

The present invention relates to use of a composition for symptomatic relief, when needed, comprising, in admixture

(a) a first active ingredient which is formoterol, a pharmaceutically acceptable salt or solvate thereof or a solvate of such a salt; and

(b) a second active ingredient which is budesonide;

for the manufacture of a medicament for use in the prevention or treatment of an acute condition of asthma and/or intermittent asthma and/or episodes in chronic asthma. The invention further relates to a method for prevention or treatment of an acute condition of asthma and/or intermittent asthma and/or episodes in chronic asthma by administering. by inhalation, a composition comprising the first and second active ingredients as defined previously.

Claims

1. Use of a composition for symptomatic relief, when needed, comprising, in admixture

(a) a first active ingredient which is formoterol, a pharmaceutically acceptable salt or solvate thereof or a solvate of such a salt;

and

(b) a second active ingredient which is budesonide;

for the manufacture of a medicament for use in the prevention or treatment of an acute condition of asthma and/or intermittent asthma and/or episodes in chronic asthma.

2. Use according to

claim 1

, wherein the molar ratio of (a) to (b) calculated as formoterol to budesonide is from 1:

1 to 1;

100, preferably from 1;

1 to 1;

70.

3. Use according to

claim 1

or

2

, wherein the first active ingredient is formoterol fumarate dihydrate.

4. Use according to any previous claim, wherein the first active ingredient is the R,R enantiomer of formoterol.

5. Use according to any previous claim, wherein a unit dose of formoterol lies in the range of from 1 μ

g to 48 μ

g, preferably between 3 μ

g to 12 μ

g, calculated as formoterol fumarate dihydrate.

6. Use according to any previous claim, wherein the daily dose of formoterol, including maintenance therapy, lies in the range of from 1 μ

g to 100 μ

g, preferably from 2 μ

g to 60 μ

g, calculated as formoterol fumarate dihydrate.

7. Use according to any previous claim, wherein the second active ingredient is the 22 R epimer of budesonide.

8. Use according to any previous claim, wherein a unit dose of budesonide lies in the range of from 20 μ

g to 1600 μ

g, preferably between 50 μ

g to 400 μ

g.

9. Use according to any previous claim, wherein the daily dose of budesonide, including maintenance therapy, lies in the range of from 20 μ

g to 4800 μ

g, preferably from 30 μ

g to 3200 μ

g.

10. Use according to any previous claim, wherein the particle size of the active ingredients (a) and (b) is less than 10 μ

m.

11. Use according to any previous claim, wherein the composition additionally comprises one or more pharmaceutically acceptable additives, diluents or carriers.

12. Use according to

claim 11

, wherein the pharmaceutically acceptable additive, diluent or carrier is lactose monohydrate.

16. The method according to any of

claims 13

to

15

, previous claim, wherein the first active ingredient is the R,R enantiomer of formoterol.

13. A method of prevention or treatment of an acute condition of asthma and/or intermittent asthma and/or episodes in chronic asthma, when needed, which comprises administering, by inhalation, to a patient an effective amount of a composition comprising, in admixture:

(a) a first active ingredient which is formoterol, a pharmaceutically acceptable salt or solvate thereof or a solvate of such a salt; and

(b) a second active ingredient which is budesonide.

14. The method according to

claim 13

, wherein the molar ratio of (a) to (b) calculated as formoterol to budesonide is from 1:

1 to 1;

100, preferably from 1;

1 to 1;

70.

15. The method according to

claim 13

or

14

, wherein the first active ingredient is formoterol fumarate dihydrate.

17. The method according to any of

claims 13

to

16

, wherein a unit dose of formoterol lies in the range of from 1 μ

g to 48 μ

g, preferably between 3 μ

g to 12 μ

g, calculated as formoterol fumarate dihydrate.

18. The method according to any of

claims 13

to

17

, wherein the daily dose of formoterol, including maintenance therapy, lies in the range of from 1 μ

g to 100 μ

g, preferably from 2 μ

g to 60 μ

g, calculated as formoterol fumarate dihydrate.

19. The method according to any of

claims 13

to

18

, wherein the second active ingredient is the 22 R epimer of budesonide.

20. The method according to any of

claims 13

to

19

, wherein a unit dose of budesonide lies in the range of from 20 μ

g to 1600 μ

g, preferably between 50 μ

g to 400 μ

g.

21. The method according to any of

claims 13

to

20

, wherein the daily dose of budesonide, including maintenance therapy, lies in the range of from 20 μ

g to 4800 μ

g, preferably from 30 μ

g to 3200 μ

g.

22. The method according to any of

claims 13

to

21

, wherein the particle size of the active ingredients (a) and (b) is less than 10 μ

m.

23. The method according to any of

claims 13

to

22

, wherein the composition additionally comprises one or more pharmaceutically acceptable additives, diluents or carriers.

24. The method according to

claim 23

, wherein the pharmaceutically acceptable additive, diluent or carrier is lactose monohydrate.