EXTENDED-RELEASE PHARMACEUTICAL COMPOSITIONS FOR TREATING EYE CONDITIONS
The present disclosure encompasses methods and compositions for extended-release formulations for treating ophthalmic conditions. These formulations comprise a pharmaceutical agent, a cationic polymer, a non-ionic polymer, and a pharmaceutical carrier and are essentially preservative free. The formulations provided herein are particularly useful for sustained and controlled release of drugs and have low side effects.
1 . A sterile pharmaceutical composition for contacting an ocular surface of a mammal, the sterile pharmaceutical composition comprising:
a pharmaceutical agent,
a cationic polymer,
a non-ionic polymer, and
a pharmaceutical carrier,
wherein the duration of the clinical effect stemming from the sterile pharmaceutical composition is greater than 6 hours.
2 . The sterile pharmaceutical composition of claim 1 , wherein the pharmaceutical agent is a pharmaceutical agent for the treatment of myopia.
3 . The sterile pharmaceutical composition of claim 1 , further comprising one or more additional non-ionic polymers.
4 . The sterile pharmaceutical composition of claim 1 , further comprising an anionic polymer.
5 . The sterile pharmaceutical composition of claim 4 , wherein the anionic polymer is selected from a group consisting of polycarbophil, carbomer and combinations thereof.
6 . The sterile pharmaceutical composition of claim 5 , wherein the anionic polymer has a concentration of about 0.2% w/v to about 2.0% w/v.
7 . The sterile pharmaceutical composition of claim 1 , wherein the cationic polymer has a concentration of about 0.01% w/v to about 2.0% w/v.
8 . The sterile pharmaceutical composition of claim 1 , wherein the non-ionic polymer has a concentration of about 0.1% w/v to about 4.0% w/v.
9 . The sterile pharmaceutical composition of claim 1 , wherein the pharmaceutical carrier comprises one or more pharmaceutically acceptable buffers.
10 . The sterile pharmaceutical composition of claim 1 , wherein the pharmaceutical carrier comprises one or more tonicity adjusting agents.
11 . The sterile pharmaceutical composition of claim 1 , wherein the pharmaceutical carrier comprises one or more stabilizers.
12 . The sterile pharmaceutical composition of claim 1 , wherein the pharmaceutical carrier comprises water.
13 . The sterile pharmaceutical composition of claim 1 , wherein the pharmaceutical composition does not comprise a preservative.
14 . The sterile pharmaceutical composition of claim 1 , wherein the pharmaceutical agent comprises at least one of a cholinesterase inhibitor, a muscarinic receptor agonist, a muscarinic receptor antagonist, and an alpha-adrenergic agonist.
15 . The sterile pharmaceutical composition of claim 14 , wherein the pharmaceutical agent comprises a cholinesterase inhibitor having a concentration of about 0.001% w/v to about 0.1% w/v.
16 . The sterile pharmaceutical composition of claim 14 , wherein the pharmaceutical agent comprises a muscarinic receptor agonist having a concentration of about 0.001% w/v to about 1% w/v.
17 . The sterile pharmaceutical composition of claim 14 , wherein the pharmaceutical agent comprises a muscarinic receptor antagonist is selected from the group consisting of atropine, scopolamine, glycopyrrolate, ipratropium bromide and any combination thereof or any pharmaceutically acceptable salt thereof.
18 . The sterile pharmaceutical composition of claim 17 , wherein the muscarinic receptor antagonist has a concentration of about 0.001% w/v to about 3% w/v.
19 . The pharmaceutical composition of claim 17 , wherein the muscarinic receptor antagonist is atropine, and wherein the pharmaceutical composition has a tropic acid concentration of less than 0.01 mg/ml after 180 days of storage in a sealed container at a temperature of 25° C. (±2) and 60% (±5%) relative humidity.
20 . The sterile pharmaceutical composition of claim 1 , wherein the pharmaceutical composition is stable for at least 60 days, 120 days, or 180 days of storage in a sealed container at a temperature of 25° C. (±2) and 60% (±5%) relative humidity.
21 . The sterile pharmaceutical composition of claim 1 , wherein the pharmaceutical composition is packaged in multi-dose bottles.
22 . The sterile pharmaceutical composition of claim 1 , wherein the cationic polymer comprises chitosan.
23 . The sterile pharmaceutical composition of claim 1 , wherein the non-ionic polymer is selected from the group consisting of polyvinyl pyrrolidone (Povidine K30), a poly(oxyethylene-co-oxypropylene) block copolymer (Poloxamer 407), or combination thereof.
24 . A packaged sterile pharmaceutical composition for contacting an ocular surface of a mammal for the treatment of myopia, the sterile pharmaceutical composition comprising:
a pharmaceutical agent,
a cationic polymer, and
a non-ionic polymer,
wherein the duration of the clinical effect stemming from the sterile pharmaceutical composition is greater than 6 hours.