Concentrated aqueous azalide formulations
AssigneeInsite Vision Incorporated
InventorsLyle M. Bowman, Sui Yen Eddie Hou, Tang Nguyen
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Abstract
Provided is concentrated aqueous azithromycin formulation from about from about 2%-20%, and a method of making a concentrated aqueous azithromycin formulation which includes preparing and sterilizing a first solution comprising a strong base to form a sterilized solution, dissolving the azithromycin in an aqueous solution comprising an acid consisting essentially of a strong acid, and adding the aqueous solution comprising the strong acid to the sterilized solution comprising the strong base. The strong acid has a pKa less than about −1.74 and the method is carried out without addition or use of a weak acid.
Claims21
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 polymeric suspending agent the pH of which is adjusted with a strong base to form the first solution,
- (b) dissolving the azithromycin in an aqueous solution comprising an acid consisting essentially of a strong acid to form a second solution, and
- (c) adding the second solution comprising the strong acid to the first solution adjusted with the strong base,
- wherein the strong acid has a pKa less than about −1.74 and the method is carried out without addition or use of a weak acid.
A method of treating a condition of the eye comprising the steps of:
- preparing a concentrated aqueous azithromycin formulation comprising from about 2% to 20% azithromycin, by sterilizing a first solution comprising a polymeric suspending agent the pH of which is adjusted with a strong base to form the first solution;
- dissolving the azithromycin in an aqueous solution comprising an acid consisting essentially of a strong acid to form a second solution;
- and adding the second solution comprising the strong acid to the first solution adjusted with the strong base, wherein the strong acid has a pKa less than about −1.74 and the method is carried out without addition or use of a weak acid;
- and applying the formulation to the eye and/or tissue surrounding the eye in an amount effective to treat the eye.
A concentrated topical aqueous azalide antibiotic formulation comprising 2% to about 20% azithromycin and a polymeric suspending agent, said formulation made by dissolving azithromycin in a strong acid to form an azithromycin solution and then adding the azithromycin solution to a sterilized solution comprising the polymeric suspending agent, the pH of which is adjusted with a base, wherein the strong acid has a pKa less than about −1.74 and wherein the formulation is made in the absence of a weak acid.
Dependencies are inferred from the claim text.