INHALABLE FORMULATION OF A SOLUTION CONTAINING INDACATEROL MALEATE AND GLYCOPYRRONIUM BROMIDE
The present invention discloses 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 comprising: (a) active substances selected from glycopyrronium bromide and indacaterol maleate; (b) a solvent; and (c) a pharmacologically acceptable preservative, optionally including a pharmacologically acceptable stabilizer, a pharmacologically acceptable solubilizing agent, a pharmacologically acceptable co-solvent, or other pharmacologically acceptable additives.
1 . A liquid, propellant-free pharmaceutical preparation comprising: (a) an active substance selected from the group consisting of glycopyrronium, indacaterol, pharmaceutically acceptable salts of glycopyrronium, pharmaceutically acceptable salts of indacaterol, and combinations thereof; (b) a solvent; (c) a pharmacologically acceptable solubilizing agent; and (d) a pharmacologically acceptable preservative.
2 . The pharmaceutical preparation according to claim 1 , wherein the active substance is selected from the group consisting of glycopyrronium bromide, indacaterol maleate, and combinations thereof.
3 . The pharmaceutical preparation according to claim 2 further comprising one or more of a pharmacologically acceptable stabilizer, a pharmacologically acceptable co-solvent, and other pharmacologically acceptable additives.
4 . The pharmaceutical preparation according to claim 2 , comprising glycopyrronium bromide in an amount ranging from about 6.5 mg/100 ml to about 26 mg/100 ml.
5 . The pharmaceutical preparation according to claim 2 , comprising indacaterol maleate in an amount ranging from about 15 mg/100 ml to about 59 mg/100 ml.
6 . The pharmaceutical preparation according to claim 2 , wherein the solvent is a mixture of water and ethanol wherein the amount of ethanol ranges from about 5% to about 30% (v/v).
7 . The pharmaceutical preparation according to claim 2 , wherein the solubilizing agent is selected from the group consisting of tween-80, poloxamer, polyoxyethylated castor oil, polyethylene glycol, solutol HS 15, polyvinylpyrrolidone, and combinations thereof.
8 . The pharmaceutical preparation according to claim 7 , wherein the solubilizing agent is present in an amount ranging from about 20 mg/100 ml to about 180 mg/100 ml.
9 . The pharmaceutical preparation according to claim 2 , wherein the pharmacologically acceptable preservative is selected from the group consisting of benzalkonium chloride, benzoic acid, sodium benzoate, and combinations thereof.
10 . The pharmaceutical preparation according to claim 9 , wherein the preservative is present in an amount ranging from about 20 mg/100 ml to about 30 mg/100 ml.
11 . The pharmaceutical preparation according to claim 2 , wherein the stabilizer is selected from the group consisting of edetic acid, edetate disodium dehydrate, edetate disodium, citric acid, and combinations thereof.
12 . The pharmaceutical preparation according to claim 11 , wherein the stabilizer is present in an amount ranging from about 5.5 mg/100 ml to about 22 mg/100 ml.
13 . The pharmaceutical preparation according to claim 2 , wherein the pharmaceutical preparation further comprises a pharmacologically acceptable additive.
14 . The pharmaceutical preparation according to claim 13 , wherein the pharmacologically acceptable additive is an antioxidant.
15 . The pharmaceutical preparation according to claim 2 , wherein the pharmaceutical preparation contains a single solvent.
16 . A method for administering the pharmaceutical preparation according to claim 2 to a patient, comprising nebulizing the pharmaceutical preparation in an inhaler, wherein the inhaler includes a block function and counter.
17 . A method for administering the pharmaceutical preparation according to claim 2 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.
18 . The method according to claim 17 , wherein the defined amount of the pharmaceutical preparation ranges from about 5 to about 30 microliters.
19 . The pharmaceutical preparation according to claim 17 , which has an aerosol MMAD of less than about 10 μm.
20 . The pharmaceutical preparation according to claim 17 , which has an aerosol D50 of less than about 10 μm.
21 . A method of treating asthma or COPD in a patient, comprising administering to the patient the pharmaceutical preparation according to claim 2 .
22 . The method of claim 16 , wherein the patient has asthma or COPD.
23 . A method for administering the pharmaceutical preparation according to claim 13 to a patient, comprising nebulizing the pharmaceutical preparation in an inhaler, wherein the inhaler includes a block function and counter.
24 . A method for administering the pharmaceutical preparation according to claim 15 to a patient, comprising nebulizing the pharmaceutical preparation in an inhaler, wherein the inhaler includes a block function and counter.
25 . The method of claim 23 , wherein the patient has asthma or COPD.
26 . The method of claim 24 , wherein the patient has asthma or COPD.
27 . The pharmaceutical preparation according to claim 1 , wherein the pharmaceutical preparation is suitable for delivery by soft mist inhalation or nebulization inhalation.
28 . A method for administering the pharmaceutical preparation according to claim 2 to a patient, comprising administering the pharmaceutical preparation using a soft mist inhaler.
29 . A method for administering the pharmaceutical preparation according to claim 2 to a patient, comprising administering the pharmaceutical preparation using a nebulization inhaler.