Aerosol pirfenidone and pyridone analog compounds and uses thereof
First Claim
1. A method of decreasing IL-1β
- levels in the lungs of a mammal diagnosed with pulmonary fibrosis comprising administering by inhalation an aqueous solution of pirfenidone to the mammal diagnosed with pulmonary fibrosis, wherein the pirfenidone solution consists of a prifenidone concentration from about 0.1 mq/mL to about 20 mg/mL;
sodium citrate;
citric acid;
sodium chloride; and
sodium saccharin wherein the molar ratio of sodium saccharin to pirfenidone is between 1 to 53.9 and 1 to 215.9;
wherein the osmolality of the aqueous solution is from about 200 mOsmol/kg to about 500 mOsmol/kg; and
wherein the pH of the solution is about 5 to about 6, and wherein the administration of the aqueous solution to the mammal decreases IL-1β
levels in the bronchial lavage fluid (BAL) of the mammal by at least 20%.
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Accused Products
Abstract
Disclosed herein are formulations of pirfenidone or pyridone analog compounds for aerosolization and use of such formulations for aerosol administration of pirfenidone or pyridone analog compounds for the prevention or treatment of various fibrotic and inflammatory diseases, including disease associated with the lung, heart, kidney, liver, eye and central nervous system. In some embodiments, pirfenidone or pyridone analog compound formulations and delivery options described herein allow for efficacious local delivery of pirfenidone or pyridone analog compound. Compositions include all formulations, kits, and device combinations described herein. Methods include inhalation procedures, indications and manufacturing processes for production and use of the compositions described.
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Citations
13 Claims
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1. A method of decreasing IL-1β
- levels in the lungs of a mammal diagnosed with pulmonary fibrosis comprising administering by inhalation an aqueous solution of pirfenidone to the mammal diagnosed with pulmonary fibrosis, wherein the pirfenidone solution consists of a prifenidone concentration from about 0.1 mq/mL to about 20 mg/mL;
sodium citrate;
citric acid;
sodium chloride; and
sodium saccharin wherein the molar ratio of sodium saccharin to pirfenidone is between 1 to 53.9 and 1 to 215.9;
wherein the osmolality of the aqueous solution is from about 200 mOsmol/kg to about 500 mOsmol/kg; and
wherein the pH of the solution is about 5 to about 6, and wherein the administration of the aqueous solution to the mammal decreases IL-1β
levels in the bronchial lavage fluid (BAL) of the mammal by at least 20%. - View Dependent Claims (2)
- levels in the lungs of a mammal diagnosed with pulmonary fibrosis comprising administering by inhalation an aqueous solution of pirfenidone to the mammal diagnosed with pulmonary fibrosis, wherein the pirfenidone solution consists of a prifenidone concentration from about 0.1 mq/mL to about 20 mg/mL;
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3. A method for the treatment of lung disease in a mammal comprising:
administering by inhalation a dose of the aqueous solution of pirfenidone to the mammal in need thereof on a continuous dosing schedule, wherein the pirfenidone solution consists of a concentration of pirfenidone of from about 0.1 mg/mL to about 20 mg/mL;
sodium citrate;
citric acid;
sodium chloride; and
sodium saccharin wherein the molar ratio of sodium saccharin to pirfenidone is between 1 to 53.9 and 1 to 215.9;
wherein the osmolality of the aqueous solution is from about 200 mOsmol/kg to about 500 mOsmol/kg; and
wherein the pH of the solution is about 5 to about 6.- View Dependent Claims (4, 5, 6, 7, 8, 9, 10, 11, 12, 13)
Specification