Concentrated aqueous azalide formulations
View Patent ↗The present invention relates to formulations of concentrated azalide antibiotics and methods for making and using them. Specifically, the invention relates to a method of treating an infection comprising administering to a patient in need thereof, an effective amount of a concentrated aqueous azalide antibiotic formulation made according to the method comprising dissolving an azalide antibiotic in an aqueous solution comprising a strong acid. The invention also relates to methods for making concentrated aqueous azalide antibiotic formulations for use in pulmonary infection, a nasopharyngeal infection, an otic infection, an ocular infection, a dermal or a vaginal infection. The invention also relates to concentrated aqueous azalide antibiotic formulations made by dissolving an azalide antibiotic in an aqueous solution comprising a strong acid.
1. A method of making a concentrated aqueous azithromycin formulation comprising from about 2% to 20% azithromycin, said method comprising the steps of:
(a) preparing and sterilizing a first solution comprising a strong base to form a sterilized solution,
(b) dissolving the azithromycin in an aqueous solution comprising a strong acid, and
(c) adding the aqueous solution comprising the strong acid to the sterilized solution comprising the strong base,
wherein the strong acid has a pKa less than about −1.74.
2. The method of claim 1 wherein the strong acid is hydrochloric acid.
3. The method of claim 1 wherein the strong base is sodium hydroxide.
4. The method of claim 1 , wherein the aqueous solution further comprises a polymeric agent.
5. The method of claim 4 wherein the polymeric agent is Noveon AA-1.
6. The method of claim 1 wherein the aqueous azithromycin formulation comprises an anti-inflammatory agent.
7. The method of claim 6 wherein the anti-inflammatory agent is a dexamethasone.
8. The method of claim 7 , wherein the dexamethasone has a concentration of about 0.1%.