Ophthalmic compositions
The present disclosure provides an ophthalmic composition comprising 4-(3-amino-1-(isoquinolin-6-ylamino)-1-oxopropan-2-yl)benzyl 2,4-dimethylbenzoate or its pharmaceutically acceptable salts; about 0.01% weight/volume to about 1.0% weight/volume of a buffer; and about 0.01% weight/volume to about 10% weight/volume of a tonicity agent.
1. An ophthalmic formulation, consisting of:
0.0285 weight/volume % of a dimesylate salt of 4-(3-amino-1-(isoquinolin-6-ylamino)-1-oxopropan-2-yl)benzyl 2,4-dimethylbenzoate;
0.05 weight/volume % of boric acid;
4.7 weight/volume % of mannitol;
water; and
a pH of 5.
2. The ophthalmic formulation of claim 1 , wherein the 4-(3-amino-1-(isoquinolin-6-ylamino)-1-oxopropan-2-yl)benzyl 2,4-dimethylbenzoate is (S)-4-(3-amino-1-(isoquinolin-6-ylamino)-1-oxopropan-2-yl)benzyl 2,4-dimethylbenzoate.
3. The ophthalmic formulation of claim 1 , wherein the mannitol is D-mannitol.
4. The ophthalmic formulation of claim 1 , which is a topical ophthalmic formulation.
5. The ophthalmic formulation of claim 1 , which is packaged in a unit dose form.
6. The ophthalmic formulation of claim 1 , which is packaged in a multidose form.
7. The ophthalmic formulation of claim 1 , which is in a plastic storage container.
8. The ophthalmic formulation of claim 1 , consisting of:
0.0285 weight/volume % of a dimesylate salt of (S)-4-(3-amino-1-(isoquinolin-6-ylamino)-1-oxopropan-2-yl)benzyl 2,4-dimethylbenzoate,
0.05 weight/volume % of boric acid,
4.7 weight/volume % of D-mannitol,
water, and
a pH of 5.
9. A method of treating glaucoma in a subject in need thereof, comprising topically administering to an eye of the subject an ophthalmic formulation consisting of:
0.0285 weight/volume % of a dimesylate salt of 4-(3-amino-1-(isoquinolin-6-ylamino)-1-oxopropan-2-yl)benzyl 2,4-dimethylbenzoate,
0.05 weight/volume % of boric acid,
4.7 weight/volume % of mannitol,
water, and
a pH of 5.
10. The method of claim 9 , wherein the 4-(3-amino-1-(isoquinolin-6-ylamino)-1-oxopropan-2-yl)benzyl 2,4-dimethylbenzoate is (S)-4-(3-amino-1-(isoquinolin-6-ylamino)-1-oxopropan-2-yl)benzyl 2,4-di methyl benzoate.
11. The method of claim 9 , wherein the mannitol is D-mannitol.
12. The method of claim 9 , wherein the ophthalmic formulation is a topical ophthalmic formulation.
13. The method of claim 9 , wherein the ophthalmic formulation is packaged in a unit dose form.
14. The method of claim 9 , wherein the ophthalmic formulation is packaged in a multidose form.
15. The method of claim 9 , wherein the ophthalmic formulation is in a plastic storage container.
16. The method of claim 9 , wherein the ophthalmic formulation consists of:
0.0285 weight/volume % of a dimesylate salt of (S)-4-(3-amino-1-(isoquinolin-6-ylamino)-1-oxopropan-2-yl)benzyl 2,4-dimethylbenzoate,
0.05 weight/volume % of boric acid,
4.7 weight/volume % of D-mannitol,
water, and
a pH of 5.