Aqueous pharmaceutical compositions comprising benzyl atropine and uses thereof
AssigneeAlcon Inc.
InventorsHoward Allen Ketelson, Rekha Rangarajan
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Abstract
The present disclosure is directed, in part, to aqueous pharmaceutical solutions comprising benzyl atropine or a pharmaceutically acceptable salt or prodrug thereof, at least one buffer, at least one tonicity agent, and at least one solubilizing agent, processes of preparing an aqueous solution comprising benzyl atropine, the products of such processes, and methods of preventing myopia, treating myopia, reducing myopia progression, or preventing myopia progression in a subject in need thereof, by administering to the eye of the subject a therapeutically effective amount of such an aqueous pharmaceutical solution.
Claims13
An aqueous pharmaceutical solution comprising benzyl atropine of Formula I:
- or a pharmaceutically acceptable salt or prodrug thereof, at least one buffer, at least one additional buffer, at least one tonicity agent, and at least one solubilizing agent, wherein the concentration of the benzyl atropine or a pharmaceutically acceptable salt or prodrug thereof is from about 0.01 to about 0.2% wt/wt, wherein the at least one buffer comprises at least one phosphate buffer and the at least one additional buffer comprises at least one acetate buffer, and wherein the at least one solubilizing agent comprises polyethylene glycol-400, polyethylene glycol-35/castor oil, polypropylene glycol, polysorbate-80, polyethylene glycol-40 stearate, poloxamer-407, dimethyl sulfoxide, or hydroxypropyl-β-cyclodextrin, or any combination thereof.
A process of preparing an aqueous solution comprising benzyl atropine of Formula I:
- or a pharmaceutically acceptable salt or prodrug thereof, comprising:
- providing an aqueous solution comprising at least one acetate buffer and at least one phosphate buffer, at least one solubilizing agent, and at least one additional solubilizing agent, wherein the aqueous solution has a pH value from about 4 to about 5;
- and
- adding to the aqueous solution the benzyl atropine or a pharmaceutically acceptable salt or prodrug thereof, wherein the benzyl atropine or a pharmaceutically acceptable salt or prodrug thereof dissolves in the aqueous solution, thereby providing an aqueous solution of benzyl atropine or a pharmaceutically acceptable salt or prodrug thereof, and
- wherein the concentration of the benzyl atropine or a pharmaceutically acceptable salt or prodrug thereof in the aqueous solution is from about 0.01 to about 0.2% wt/wt and wherein the aqueous solution has a pH value of greater than about 5.
Dependencies are inferred from the claim text.