AEROSOL FORMULATION FOR COPD
Stable aerosol solution formulations comprising glycopyrronium bromide are useful for administration to patients with COPD and other respiratory conditions.
1 . A pharmaceutical composition for use with a pressurized metered dose inhaler, comprising glycopyrronium bromide dissolved in HFA-134a and ethanol, wherein:
the composition comprises an amount of hydrochloric acid equivalent to 0.187 to 0.248 μg/μl of 1M hydrochloric acid;
the composition comprises glycopyrronium bromide in an amount of 0.015 to 0.04% w/w of the composition;
the composition comprises ethanol in an amount of 10 to 15% w/w of the composition;
the composition comprises HFA-134a in an amount of 85 to 90% w/w of the composition;
the composition comprises formoterol fumarate; and
the composition comprises beclometasone dipropionate.
2 . A composition according to claim 1 , comprising water in an amount less than 0.5% w/w of the composition.
3 . A composition according to claim 1 , comprising water in an amount 0.005 to 0.5% w/w of the composition.
4 . A composition according to claim 1 , wherein the concentration of ethanol in the pharmaceutical composition is 12% w/w.
5 . A composition according to claim 2 , wherein the concentration of ethanol in the pharmaceutical composition is 12% w/w.
6 . A composition according to claim 3 , wherein the concentration of ethanol in the pharmaceutical composition is 12% w/w.
7 . A pharmaceutical composition for use with a pressurized metered dose inhaler, comprising glycopyrronium bromide dissolved in HFA-134a and ethanol, wherein:
the composition comprises an amount of hydrochloric acid equivalent to 0.222 μg/μl of 1M hydrochloric acid;
the composition comprises glycopyrronium bromide in an amount of 0.015 to 0.04% w/w of the composition;
the composition comprises ethanol in an amount of 10 to 15% w/w of the composition;
the composition comprises HFA-134a in an amount of 85 to 90% w/w of the composition;
the composition comprises formoterol fumarate; and
the composition comprises beclometasone dipropionate.
8 . A composition according to claim 7 , comprising water in an amount less than 0.5% w/w of the composition.
9 . A composition according to claim 7 , comprising water in an amount 0.005 to 0.5% w/w of the composition.
10 . A composition according to claim 7 , wherein the concentration of ethanol in the pharmaceutical composition is 12% w/w.
11 . A composition according to claim 8 , wherein the concentration of ethanol in the pharmaceutical composition is 12% w/w.
12 . A composition according to claim 9 , wherein the concentration of ethanol in the pharmaceutical composition is 12% w/w.
13 . A pressurized metered dose inhaler, comprising a pharmaceutical composition according to claim 1 .
14 . A pressurized metered dose inhaler, comprising a pharmaceutical composition according to claim 2 .
15 . A pressurized metered dose inhaler, comprising a pharmaceutical composition according to claim 5 .
16 . A pressurized metered dose inhaler, comprising a pharmaceutical composition according to claim 6 .
17 . A pressurized metered dose inhaler, comprising a pharmaceutical composition according to claim 8 .
18 . A pressurized metered dose inhaler, comprising a pharmaceutical composition according to claim 12 .
19 . A pressurized metered dose inhaler according to claim 13 , comprising a metering valve capable of delivering a volume of about 63 μl per actuation.
20 . A pressurized metered dose inhaler according to claim 14 , comprising a metering valve capable of delivering a volume of about 63 μl per actuation.
21 . A pressurized metered dose inhaler according to claim 18 , comprising a metering valve capable of delivering a volume of about 63 μl per actuation.
22 . A method for treatment of asthma, comprising administering an effective amount of a composition according to claim 1 to a subject in need thereof.
23 . A method for treatment of asthma, comprising administering an effective amount of a composition according to claim 2 to a subject in need thereof.
24 . A method for treatment of asthma, comprising administering an effective amount of a composition according to claim 5 to a subject in need thereof.
25 . A method for treatment of asthma, comprising administering an effective amount of a composition according to claim 6 to a subject in need thereof.
26 . A method for treatment of asthma, comprising administering an effective amount of a composition according to claim 8 to a subject in need thereof.
27 . A method for treatment of asthma, comprising administering an effective amount of a composition according to claim 12 to a subject in need thereof.
28 . A method for treatment of chronic obstructive pulmonary disease, comprising administering an effective amount of a composition according to claim 1 to a subject in need thereof.
29 . A method for treatment of chronic obstructive pulmonary disease, comprising administering an effective amount of a composition according to claim 2 to a subject in need thereof.
30 . A method for treatment of chronic obstructive pulmonary disease, comprising administering an effective amount of a composition according to claim 5 to a subject in need thereof.
31 . A method for treatment of chronic obstructive pulmonary disease, comprising administering an effective amount of a composition according to claim 6 to a subject in need thereof.
32 . A method for treatment of chronic obstructive pulmonary disease, comprising administering an effective amount of a composition according to claim 8 to a subject in need thereof.
33 . A method for treatment of chronic obstructive pulmonary disease, comprising administering an effective amount of a composition according to claim 12 to a subject in need thereof.
34 . A method for treatment of asthma, comprising inhalation administration of an effective amount of a pharmaceutical composition according to claim 1 to a subject in need thereof via two actuations of a pressurized metered dose inhaler containing said pharmaceutical composition, wherein the pressurized metered dose inhaler has a metering valve that delivers a volume of about 63 ml of pharmaceutical composition per actuation.
35 . A method for treatment of asthma, comprising inhalation administration of an effective amount of a pharmaceutical composition according to claim 2 to a subject in need thereof via two actuations of a pressurized metered dose inhaler containing said pharmaceutical composition, wherein the pressurized metered dose inhaler has a metering valve that delivers a volume of about 63 ml of pharmaceutical composition per actuation.
36 . A method for treatment of asthma, comprising inhalation administration of an effective amount of a pharmaceutical composition according to claim 5 to a subject in need thereof via two actuations of a pressurized metered dose inhaler containing said pharmaceutical composition, wherein the pressurized metered dose inhaler has a metering valve that delivers a volume of about 63 ml of pharmaceutical composition per actuation.
37 . A method for treatment of asthma, comprising inhalation administration of an effective amount of a pharmaceutical composition according to claim 6 to a subject in need thereof via two actuations of a pressurized metered dose inhaler containing said pharmaceutical composition, wherein the pressurized metered dose inhaler has a metering valve that delivers a volume of about 63 ml of pharmaceutical composition per actuation.
38 . A method for treatment of asthma, comprising inhalation administration of an effective amount of a pharmaceutical composition according to claim 8 to a subject in need thereof via two actuations of a pressurized metered dose inhaler containing said pharmaceutical composition, wherein the pressurized metered dose inhaler has a metering valve that delivers a volume of about 63 ml of pharmaceutical composition per actuation.
39 . A method for treatment of asthma, comprising inhalation administration of an effective amount of a pharmaceutical composition according to claim 12 to a subject in need thereof via two actuations of a pressurized metered dose inhaler containing said pharmaceutical composition, wherein the pressurized metered dose inhaler has a metering valve that delivers a volume of about 63 ml of pharmaceutical composition per actuation.
40 . A method for treatment of chronic obstructive pulmonary disease, comprising inhalation administration of an effective amount of a pharmaceutical composition according to claim 1 to a subject in need thereof via two actuations of a pressurized metered dose inhaler containing said pharmaceutical composition, wherein the pressurized metered dose inhaler has a metering valve that delivers a volume of about 63 ml of pharmaceutical composition per actuation.
41 . A method for treatment of chronic obstructive pulmonary disease, comprising inhalation administration of an effective amount of a pharmaceutical composition according to claim 2 to a subject in need thereof via two actuations of a pressurized metered dose inhaler containing said pharmaceutical composition, wherein the pressurized metered dose inhaler has a metering valve that delivers a volume of about 63 ml of pharmaceutical composition per actuation.
42 . A method for treatment of chronic obstructive pulmonary disease, comprising inhalation administration of an effective amount of a pharmaceutical composition according to claim 5 to a subject in need thereof via two actuations of a pressurized metered dose inhaler containing said pharmaceutical composition, wherein the pressurized metered dose inhaler has a metering valve that delivers a volume of about 63 ml of pharmaceutical composition per actuation.
43 . A method for treatment of chronic obstructive pulmonary disease, comprising inhalation administration of an effective amount of a pharmaceutical composition according to claim 6 to a subject in need thereof via two actuations of a pressurized metered dose inhaler containing said pharmaceutical composition, wherein the pressurized metered dose inhaler has a metering valve that delivers a volume of about 63 ml of pharmaceutical composition per actuation.
44 . A method for treatment of chronic obstructive pulmonary disease, comprising inhalation administration of an effective amount of a pharmaceutical composition according to claim 8 to a subject in need thereof via two actuations of a pressurized metered dose inhaler containing said pharmaceutical composition, wherein the pressurized metered dose inhaler has a metering valve that delivers a volume of about 63 ml of pharmaceutical composition per actuation.
45 . A method for treatment of chronic obstructive pulmonary disease, comprising inhalation administration of an effective amount of a pharmaceutical composition according to claim 12 to a subject in need thereof via two actuations of a pressurized metered dose inhaler containing said pharmaceutical composition, wherein the pressurized metered dose inhaler has a metering valve that delivers a volume of about 63 ml of pharmaceutical composition per actuation.
46 - 62 . (canceled)