PROPELLANT-FREE FORMULATION FOR INHALATION
The present invention provides a propellant-free pharmaceutical formulation and a method for administering the pharmaceutical formulation by nebulizing the pharmaceutical formulation in an inhaler. The propellant-free pharmaceutical formulation comprises: (a) glycopyrronium or a salt thereof; (b) formoterol or a salt thereof; (c) a pharmacologically acceptable stabilizer; (d) a pharmacologically acceptable preservative; and (d) a solvent. Additionally, the present invention provides the use of a combination product comprising glycopyrronium or a salt thereof and formoterol or a salt thereof for the prevention or treatment of chronic obstructive pulmonary disease (COPD) and other respiratory diseases.
1 . A propellant-free pharmaceutical preparation comprising: (a) glycopyrronium or a salt thereof; (b) formoterol or a salt thereof; (c) a pharmacologically acceptable stabilizer; (d) a pharmacologically acceptable preservative, and (e) a solvent, wherein the pH of the pharmaceutical preparation is between about 2.5 and about 7.5
2 . The pharmaceutical preparation according to claim 1 , comprising glycopyrronium bromide and formoterol fumarate.
3 . The pharmaceutical preparation according to claim 2 , wherein the glycopyrronium bromide is present in an amount ranging from about 30 mg/100 g to about 300 mg/100 g.
4 . The pharmaceutical preparation according to claim 2 , wherein the formoterol fumarate is present in an amount ranging from about 10 mg/100 g to about 100 mg/100 g.
5 . The pharmaceutical preparation according to claim 1 , wherein the pharmacologically acceptable preservative is selected from the group consisting of benzalkonium chloride, benzoic acid, sodium benzoate, and combinations thereof.
6 . The pharmaceutical preparation according to claim 5 , wherein the pharmacologically acceptable preservative is present in an amount ranging from about 10 mg/100 g to about 50 mg/100 g.
7 . The pharmaceutical preparation according to claim 1 , wherein the stabilizer is selected from the group consisting of edetic acid, edetate disodium dehydrate, edetate disodium, and combinations thereof.
8 . The pharmaceutical preparation according to claim 1 , wherein the stabilizer is present in amount ranging from about 5 mg/100 g to about 22 mg/100 g.
9 . The pharmaceutical preparation according to claim 1 , wherein the solvent comprises water or normal saline.
10 . The pharmaceutical preparation according to claim 9 , further comprising a co-solvent containing a hydroxyl group.
11 . The pharmaceutical preparation according to claim 10 , wherein the co-solvent is selected from the group consisting of isopropyl alcohol, propylene glycol, polyethylene glycol, polypropylene glycol, glycerol, polyoxyethylene alcohols, and combinations thereof.
12 . The pharmaceutical preparation according to claim 1 , further comprising a pharmacologically acceptable additive.
13 . The pharmaceutical preparation according to claim 12 , wherein pharmacologically acceptable additive is an antioxidant.
14 . A method for administering the pharmaceutical preparation according to claim 1 , comprising nebulizing a defined amount of the pharmaceutical preparation through a nozzle by the application of pressure to form an inhalable aerosol.
15 . The method according to claim 14 , wherein the inhalable aerosol has a mass median aerodynamic diameter (MMAD) of less than about 6 microns.
16 . The method according to claim 14 , wherein the inhalable aerosol has a particle size distribution with a D50 less than 5 μm.
17 . The method of claim 14 , wherein the pharmaceutical preparation is nebulized using an inhaler according to FIG. 1 .
18 . The method according to claim 14 , wherein the defined amount of the pharmaceutical preparation ranges from about 5 to about 30 microliters.
19 . The method according to claim 17 , wherein the inhaler comprises a block function and a counter.
20 . A method of treating asthma or COPD in a patient, comprising administering to the patient a pharmaceutical preparation according to claim 1 .
21 . A method of treating asthma or COPD in a patient, the method comprising administering to the patient a pharmaceutical preparation using the method of claim 14 .
22 . A method of treating asthma or COPD in a patient, the method comprising administering to the patient a pharmaceutical preparation using the method of claim 17 .
23 . A method of treating asthma or COPD in a patient, the method comprising administering to the patient a pharmaceutical preparation using the method of claim 19 .