Inhalable formulation of a solution containing vilanterol trifenatate and umeclidinium bromide
The present invention relates to a liquid, propellant-free pharmaceutical preparation and a method for administering a pharmaceutical preparation by nebulizing the pharmaceutical preparation in an inhaler. The propellant-free pharmaceutical preparation comprises: (a) an active substance selected from umeclidinium bromide and vilanterol trifenatate and combinations thereof; (b) a solvent; (c) a pharmacologically acceptable solubilizing agent; and (d) a pharmacologically acceptable preservative, and optionally includes a pharmacologically acceptable stabilizer, a pharmacologically acceptable co-solvent, or other pharmacologically acceptable additives.
1. A liquid, propellant-free pharmaceutical preparation consisting of: (a) umeclidinium bromide in an amount ranging from about 15 mg/100 mL to about 50 mg/100 mL and vilanterol trifenatate in an amount ranging from about 8 mg/100 mL to about 30 mg/100 mL; (b) a mixture of water and ethanol wherein the amount of ethanol ranges from about 5% to about 30% (v/v); (c) tween-80 in an amount ranging from about 20 mg/100 mL to about 40 mg/100 mL; and (d) edetate disodium dihydrate in an amount of about 11 mg/100 mL to less than about 20 mg/100 mL; optionally further comprising benzalkonium chloride.
2. A method for administering the pharmaceutical preparation according to claim 1 to a patient, comprising forming an inhalable aerosol by using pressure to force a defined amount of the pharmaceutical preparation through a nozzle to nebulize the pharmaceutical preparation.
3. The method according to claim 2 , wherein the defined amount of the pharmaceutical preparation ranges from about 5 to about 30 microliters.
4. The pharmaceutical preparation according to claim 2 , which has an aerosol MMAD of less than about 10 μm.
5. The pharmaceutical preparation according to claim 2 , which has an aerosol D50 of less than about 10 μm.
6. A method of treating asthma or COPD in a patient, comprising administering to the patient the pharmaceutical preparation according to claim 1 .
7. A method for administering the pharmaceutical preparation according to claim 1 to a patient, comprising nebulizing the pharmaceutical preparation in an inhaler, wherein the inhaler includes a block function and counter.
8. The method of claim 7 , wherein the patient has asthma or COPD.
9. The method of claim 7 , wherein the patient has asthma or COPD.
10. The pharmaceutical preparation according to claim 1 , wherein the pharmaceutical preparation is suitable for delivery by soft mist inhalation or nebulization inhalation.
11. A method for administering the pharmaceutical preparation according to claim 1 to a patient, comprising administering the pharmaceutical preparation using a soft mist inhaler.
12. A method for administering the pharmaceutical preparation according to claim 1 to a patient, comprising administering the pharmaceutical preparation using a nebulization inhaler.
13. The pharmaceutical preparation of claim 1 comprising umeclidinium bromide in an amount of about 21 mg/100 mL, vilanterol trifenatate in an amount of about 11 mg/100 mL, tween-80 in an amount of about 40 mg/100 mL, edetate disodium dihydrate in an amount of about 11 mg/100 mL, and ethanol in an amount of about 19% (v/v).
14. The pharmaceutical preparation of claim 13 , further comprising 50% benzalkonium chloride in an amount of about 20 mg/100 mL.
15. The pharmaceutical preparation of claim 1 comprising umeclidinium bromide in an amount of about 21 mg/100 mL, vilanterol trifenatate in an amount of about 11 mg/100 mL, tween-80 in an amount of about 40 mg/100 mL, edetate disodium dihydrate in an amount of about 11 mg/100 mL, and ethanol in an amount of about 15% (v/v).
16. The pharmaceutical preparation of claim 15 , further comprising 50% benzalkonium chloride in an amount of about 20 mg/100 mL.
17. The pharmaceutical preparation of claim 1 comprising umeclidinium bromide in an amount of about 21 mg/100 mL, vilanterol trifenatate in an amount of about 11 mg/100 mL, tween-80 in an amount of about 40 mg/100 mL, edetate disodium dihydrate in an amount of about 11 mg/100 mL, and ethanol in an amount of about 23% (v/v).
18. The pharmaceutical preparation of claim 17 , further comprising 50% benzalkonium chloride in an amount of about 20 mg/100 mL.
19. The pharmaceutical preparation of claim 1 comprising umeclidinium bromide in an amount of about 21 mg/100 mL, vilanterol trifenatate in an amount of about 11 mg/100 mL, tween-80 in an amount of about 30 mg/100 mL, edetate disodium dihydrate in an amount of about 11 mg/100 mL, and ethanol in an amount of about 15% (v/v).
20. The pharmaceutical preparation of claim 19 , further comprising 50% benzalkonium chloride in an amount of about 20 mg/100 mL.
21. The pharmaceutical preparation of claim 1 comprising umeclidinium bromide in an amount of about 21 mg/100 mL, vilanterol trifenatate in an amount of about 11 mg/100 mL, tween-80 in an amount of about 30 mg/100 mL, edetate disodium dihydrate in an amount of about 11 mg/100 mL, and ethanol in an amount of about 19% (v/v).
22. The pharmaceutical preparation of claim 12 , further comprising 50% benzalkonium chloride in an amount of about 20 mg/100 mL.
23. The pharmaceutical preparation of claim 1 comprising umeclidinium bromide in an amount of about 21 mg/100 mL, vilanterol trifenatate in an amount of about 11 mg/100 mL, tween-80 in an amount of about 30 mg/100 mL, edetate disodium dihydrate in an amount of about 11 mg/100 mL, and ethanol in an amount of about 23% (v/v).
24. The pharmaceutical preparation of claim 23 , further comprising 50% benzalkonium chloride in an amount of about 20 mg/100 mL.