PHARMACEUTICAL FORMULATION CONTAINING COMBINATION OF M3 ANTAGONIST-BETA-2 AGONIST AND INHALED CORTICOSTEROIDS
The present invention relates to a pharmaceutical formulation and a method for administering the pharmaceutical formulation by nebulizing the pharmaceutical formulation with an inhaler. The propellant-free pharmaceutical formulation comprises: batefenterol or a pharmaceutically acceptable salt thereof, fluticasone furoate, and a pH adjusting agent.
1 . A propellant free pharmaceutical formulation comprising batefenterol or a pharmaceutically acceptable salt thereof, fluticasone furoate, a surfactant, and a pH adjusting agent.
2 . The pharmaceutical formulation of claim 1 , wherein the batefenterol or a pharmaceutically acceptable salt thereof is batefenterol succinate.
3 . The pharmaceutical formulation of claim 2 , wherein the batefenterol succinate is present in an amount ranging from about 1 mg/ml to about 200 mg/ml.
4 . The pharmaceutical formulation of claim 1 , wherein the fluticasone furoate is present in an amount ranging from about 100 mg/100 ml to about 20 g/100 ml.
5 . The pharmaceutical formulation of claim 1 , wherein the surfactant is present in an amount ranging from about Omg/100 ml to about 100 mg/100 ml.
6 . The pharmaceutical formulation of claim 1 , wherein the surfactant is a polysorbate.
7 . The pharmaceutical formulation of claim 1 , wherein the surfactant is a polysorbate 80.
8 . The pharmaceutical formulation of claim 1 , wherein the pH ranges from about 2.0 to about 6.0.
9 . The pharmaceutical formulation of claim 1 , further comprising a preservative.
10 . The pharmaceutical formulation of claim 1 , wherein the preservative is selected from the group consisting of benzalkonium chloride, benzoic acid, and sodium benzoate.
11 . The pharmaceutical formulation of claim 10 , wherein the preservative is present in an amount ranging from about 2 mg/100 ml to about 300 mg/100 ml.
12 . The pharmaceutical formulation of claim 10 , wherein the preservative is benzalkonium chloride in an amount of about 10 mg/100 ml.
13 . The pharmaceutical formulation of claim 1 further comprising a complexing agent selected from the group consisting of edetic acid (EDTA), disodium edetate, and edetate disodium dihydrate, wherein the complexing agent is present in an amount ranging from about 1 mg/100 ml to about 500 mg/100 ml.
14 . A method for administering the pharmaceutical formulation of claim 1 comprising nebulizing a defined amount of the pharmaceutical formulation with an inhaler by using pressure to force the pharmaceutical preparation through a nozzle to form an inhalable aerosol.
15 . The method of claim 14 , wherein the inhalable aerosol has an average particle size of less than about 15 microns.
16 . The method of claim 14 , wherein the defined amount of the pharmaceutical formulation is less than about 70 microliters.
17 . A method of treating chronic obstructive pulmonary disease (COPD) or asthma in a patient comprising administering the formulation of claim 1 to the patient by inhalation.
18 . The pharmaceutical formulation of claim 1 comprising:
an aqueous solution comprising:
(i) batefenterol succinate in an amount of about 30 g/100 ml,
(ii) fluticasone furoate in an amount of about 19 g/100 ml,
(iii) polysorbate 80 in an amount of about 30 mg/100 ml,
(iv) edetate disodium dihydrate in an amount of about 15 mg/100 ml,
(v) 50% benzalkonium chloride aqueous solution in an amount of about 30 mg/100 ml, wherein the pH of the formulation ranges from about 3 to about 4.
19 . The pharmaceutical formulation of claim 1 comprising:
an aqueous solution comprising:
(i) batefenterol succinate in an amount of about 25 g/100 ml,
(ii) fluticasone furoate in an amount of about 17 g/100 ml,
(iii) polysorbate 80 in an amount of about 20 mg/100 ml,
(iv) edetate disodium dihydrate in an amount of about 10 mg/100 ml,
(v) 50% benzalkonium chloride aqueous solution in an amount of about 20 mg/100 ml, wherein the pH of the formulation ranges from about 3 to about 4.
20 . A pharmaceutical formulation comprising:
an aqueous solution comprising:
(i) batefenterol succinate in an amount of about 7.5 g/100 ml,
(ii) fluticasone furoate in an amount of about 2.5 g/100 ml,
(iii) sodium chloride in an amount of about 150 mg/100 ml,
(iv) 50% benzalkonium chloride aqueous solution in an amount of about 20 mg/100 ml, wherein the pH of the formulation ranges from about 3 to about 4.
21 . A pharmaceutical formulation comprising:
an aqueous solution comprising:
(i) batefenterol succinate in an amount of about 5 g/100 ml,
(ii) fluticasone furoate in an amount of about 1.5 g/100 ml,
(iii) sodium chloride in an amount of about 250 mg/100 ml,
(iv) 50% benzalkonium chloride aqueous solution in an amount of about 20 mg/100 ml, wherein the pH of the formulation ranges from about 3 to about 4.
22 . The method of claim 17 , wherein the batefenterol succinate is administered at a daily dose ranging from about 50 micrograms to about 1000 microgram and the fluticasone furoate is administered at a daily dose ranging from about 1 microgram to about 1000 micrograms.