Pharmaceutical aerosol product for administration by oral or nasal inhalation

Abstract

The inventive subject matter relates to a pharmaceutical aerosol product suitable for administration by oral or nasal inhalation and its use in the treatment of respiratory diseases, in particular in the treatment of children.

Claims

1. A pharmaceutical composition comprising the following components: a. an effective amount of ciclesonide, b. a propellant selected from the group consisting of 1,1,1,2-tetrafluoroethane, 1,1,1,2,3,3,3-heptafluoropropane and a mixture thereof, and c. ethanol in an amount independently effective to solubilize the ciclesonide wherein the concentration of ciclesonide in the composition is from 0.1 to 0.9 mg per ml, and the ciclesonide is solubilized by the ethanol, wherein the ciclesonide is the sole drug in the pharmaceutical composition, and wherein the pharmaceutical composition is a nasal aerosol.

2. The pharmaceutical composition according to claim 1, in which the concentration of ciclesonide in the composition is from 0.4 to 0.5 mg per ml.

3. The pharmaceutical composition according to claim 2, wherein the concentration of ciclesonide in the composition is 0.5 mg per ml.

4. The pharmaceutical composition according to claim 1, in which the concentration of ethanol in the composition is from 30 to 300 mg per ml.

5. The pharmaceutical composition according to claim 4, in which the concentration of ethanol in the composition is from 90 to 100 mg per ml.

6. The pharmaceutical composition according to claim 1, in which the propellant is 1,1,1,2-tetrafluoroethane.

7. The pharmaceutical composition according to claim 1, in which the propellant is 1,1,1,2,3,3,3-heptafluoropropane.

8. The pharmaceutical composition according to claim 1, in which the propellant is a mixture of 1,1,1,2-tetrafluoroethane and 1,1,1,2,3,3,3-heptafluoropropane.

9. The pharmaceutical composition according to claim 1, consisting essentially of a. ciclesonide in a concentration in the composition of 0.9 mg per ml, b. the propellant 1,1,1,2-tetrafluoroethane in a concentration in the composition of 1000 to 1200 mg per ml and c. ethanol in a concentration in the composition of 90 to 100 mg per ml.

10. The pharmaceutical composition according to claim 1, consisting essentially of a. ciclesonide in a concentration in the composition of 0.9 mg per ml, b. ethanol, and c. 1,1,1,2-tetrafluoroethane wherein the ratio of ethanol:1,1,1,2-tetrafluoroethane is from 3:97 by weight to 12:88 by weight, and wherein the pharmaceutical composition is a nasal aerosol.

11. A pharmaceutical product comprising an aerosol canister equipped with a metering valve and containing a pharmaceutical composition according to claim 1.

12. A method for treating or preventing a respiratory disease in a patient, which method comprises administering to the patient a dose of a composition according to claim 1.

13. A method for treating or preventing nasal symptoms associated with allergic rhinitis in a child, which method comprises administering to the nose of the child a dose of a composition according to claim 1.

14. The pharmaceutical composition of claim 1, wherein the concentration of ethanol in the composition is from 40 to 300 mg per ml.

15. The pharmaceutical composition of claim 1, wherein the composition is formulated for delivery to a patient as one spray, delivered once daily.

16. The pharmaceutical composition of claim 1, wherein the composition is formulated to accurate dose delivery to a pediatric patient.

Description

EXAMPLES

(1) Ciclesonide can be provided as a pharmaceutical product comprising an aerosol vial equipped with a dispensing valve. Further, ciclesonide can be provided as a pharmaceutical product comprising an actuator and an aerosol vial equipped with a dispensing metering valve. The following compositions further illustrate the present invention in terms of exemplary formulations and ingredients. However, it will be understood that the invention is not limited to these specific embodiments.

(2) TABLE-US-00001 Composition 1 Ingredient mg per ml % w/w Ciclesonide 0.50 0.04 Ethanol 94.84 8.00 1,1,1,2-Tetrafluoroethane 1090.66 91.96 (Propellant 134a) Total 1186.00 100

(3) TABLE-US-00002 Composition 2 Ingredient mg per ml % w/w Ciclesonide 0.25 0.02 Ethanol 94.88 8.00 1,1,1,2-Tetrafluoroethane 1090.87 91.98 (Propellant 134a) Total 1186.00 100

(4) TABLE-US-00003 Composition 3 Ingredient mg per ml % w/w Ciclesonide 0.75 0.06 Ethanol 94.80 8.00 1,1,1,2-Tetrafluoroethane 1090.45 91.94 (Propellant 134a) Total 1186.00 100

(5) TABLE-US-00004 Composition 4 Ingredient mg per ml % w/w Ciclesonide 0.50 0.04 Ethanol 47.42 3.93 1,1,1,2-Tetrafluoroethane 1159.08 96.03 (Propellant 134a) Total 1207.00 100

(6) TABLE-US-00005 Composition 5 Ingredient mg per ml % w/w Ciclesonide 0.50 0.04 Ethanol 71.13 5.93 1,1,1,2-Tetrafluoroethane 1127.37 94.03 (Propellant 134a) Total 1199.00 100

(7) TABLE-US-00006 Composition 6 Ingredient mg per ml % w/w Ciclesonide 0.50 0.04 Ethanol 118.55 10.03 1,1,1,2-Tetrafluoroethane 1062.95 89.93 (Propellant 134a) Total 1182.00 100

(8) TABLE-US-00007 Composition 7 Ingredient mg per ml % w/w Ciclesonide 0.50 0.04 Ethanol 55.32 4.00 1,1,1,2,3,3,3 1327.18 95.96 heptafluoropropane (Propellant 227) Total 1383.00 100

(9) TABLE-US-00008 Composition 8 Ingredient mg per ml % w/w Ciclesonide 0.50 0.04 Ethanol 106.08 8.00 1,1,1,2,3,3,3 1219.42 91.96 heptafluoropropane (Propellant 227) Total 1326.00 100

(10) TABLE-US-00009 Composition 9 Ingredient mg per ml % w/w Ciclesonide 0.50 0.04 Ethanol 130.90 10.00 1,1,1,2,3,3,3 1177.60 89.96 heptafluoropropane (Propellant 227) Total 1309.00 100

(11) TABLE-US-00010 Composition 10 Ingredient mg per ml % w/w Ciclesonide 0.50 0.04 Ethanol 101.92 8.00 1,1,1,2-Tetrafluoroethane 585.79 45.98 (Propellant 134a) 1,1,1,2,3,3,3 585.79 45.98 heptafluoropropane (Propellant 227) Total 1274.00 100