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 composition, comprising:
a dimesylate salt of (S)-4-(3-amino-1-(isoquinolin-6-ylamino)-1-oxopropan-2-yl)benzyl 2,4-dimethylbenzoate;
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;
wherein the ophthalmic composition is free of benzalkonium chloride, thimerosal, chlorobutanol, methyl paraben, propyl paraben, phenylethyl alcohol, and sorbic acid.
2. The ophthalmic composition of claim 1 , having a pH from about 3.5 to about 5.5.
3. The ophthalmic composition of claim 1 , having a pH from about 4.5 to about 5.2.
4. The ophthalmic composition of claim 1 , wherein the ophthalmic composition is free of benzalkonium chloride, thimerosal, chlorobutanol, methyl paraben, propyl paraben, phenylethyl alcohol, edetate disodium, and sorbic acid.
5. The ophthalmic composition of claim 1 , further comprising an emulsifying agent.
6. The ophthalmic composition of claim 1 , further comprising polyoxyl 40 stearate, polyethoxylated castor oil, or a combination thereof.
7. The ophthalmic composition of claim 1 , wherein the tonicity agent comprises mannitol.
8. The ophthalmic composition of claim 1 , wherein the buffer comprises boric acid or a salt thereof.
9. The ophthalmic composition of claim 1 , further comprising water.
10. The ophthalmic composition of claim 1 , further comprising a pH adjusting agent.
11. The ophthalmic composition of claim 1 , further comprising a second ophthalmic active compound.
12. The free ophthalmic composition of claim 1 , further comprising a prostaglandin analog.
13. The free ophthalmic composition of claim 1 , further comprising latanoprost or travoprost.
14. The ophthalmic composition of claim 1 , comprising about 0.02% weight/volume to about 0.03% weight/volume of the dimesylate salt of (S)-4-(3-amino-1-(isoquinolin-6-ylamino)-1-oxopropan-2-yl)benzyl 2,4-dimethylbenzoate.
15. The ophthalmic composition of claim 1 , comprising about 4.7% weight/volume of mannitol.
16. The ophthalmic composition of claim 1 , comprising about 0.05% weight/volume of boric acid.
17. The free ophthalmic composition of claim 1 , further comprising about 0.005% weight/volume of latanoprost or travoprost.
18. The ophthalmic composition of claim 1 , comprising:
a dimesylate salt of (S)-4-(3-amino-1-(isoquinolin-6-ylamino)-1-oxopropan-2-yl)benzyl 2,4-dimethylbenzoate;
boric acid; and
mannitol;
wherein the ophthalmic composition has a pH from about 4.5 to about 5.2.
19. The ophthalmic composition of claim 1 , comprising:
a dimesylate salt of (S)-4-(3-amino-1-(isoquinolin-6-ylamino)-1-oxopropan-2-yl)benzyl 2,4-dimethylbenzoate;
boric acid; and
mannitol;
wherein the ophthalmic composition has a pH from about 4.5 to about 5.2, and
wherein the ophthalmic composition is free of benzalkonium chloride, thimerosal, chlorobutanol, methyl paraben, propyl paraben, phenylethyl alcohol, and sorbic acid.
20. The ophthalmic composition of claim 1 , comprising:
a dimesylate salt of (S)-4-(3-amino-1-(isoquinolin-6-ylamino)-1-oxopropan-2-yl)benzyl 2,4-dimethylbenzoate;
boric acid;
mannitol; and
latanoprost.
21. The ophthalmic composition of claim 1 , comprising:
a dimesylate salt of (S)-4-(3-amino-1-(isoquinolin-6-ylamino)-1-oxopropan-2-yl)benzyl 2,4-dimethylbenzoate;
boric acid;
mannitol; and
latanoprost;
wherein the ophthalmic composition is free of benzalkonium chloride, thimerosal, chlorobutanol, methyl paraben, propyl paraben, phenylethyl alcohol, and sorbic acid.
22. The ophthalmic composition of claim 1 , comprising:
about 0.02% weight/volume to about 0.03% weight/volume of a dimesylate salt of (S)-4-(3-amino-1-(isoquinolin-6-ylamino)-1-oxopropan-2-yl)benzyl 2,4-dimethylbenzoate;
about 0.05% weight/volume of boric acid; and
about 4.7% weight/volume of mannitol;
wherein the ophthalmic composition has a pH from about 4.5 to about 5.2.
23. The ophthalmic composition of claim 1 , comprising:
about 0.02% weight/volume to about 0.03% weight/volume of a dimesylate salt of (S)-4-(3-amino-1-(isoquinolin-6-ylamino)-1-oxopropan-2-yl)benzyl 2,4-dimethylbenzoate;
about 0.05% weight/volume of boric acid; and
about 4.7% weight/volume of mannitol;
wherein the ophthalmic composition has a pH from about 4.5 to about 5.2, and
wherein the ophthalmic composition is free of benzalkonium chloride, thimerosal, chlorobutanol, methyl paraben, propyl paraben, phenylethyl alcohol, and sorbic acid.
24. The ophthalmic composition of claim 1 , comprising:
about 0.02% weight/volume to about 0.03% weight/volume of a dimesylate salt of (S)-4-(3-amino-1-(isoquinolin-6-ylamino)-1-oxopropan-2-yl)benzyl 2,4-dimethylbenzoate;
about 0.05% weight/volume of boric acid;
about 4.7% weight/volume of mannitol; and
about 0.005% weight/volume of latanoprost.
25. The ophthalmic composition of claim 1 , comprising:
about 0.02% weight/volume to about 0.03% weight/volume of a dimesylate salt of (S)-4-(3-amino-1-(isoquinolin-6-ylamino)-1-oxopropan-2-yl)benzyl 2,4-dimethylbenzoate;
about 0.05% weight/volume of boric acid;
about 4.7% weight/volume of mannitol; and
about 0.005% weight/volume of latanoprost;
wherein the ophthalmic composition is free of benzalkonium chloride, thimerosal, chlorobutanol, methyl paraben, propyl paraben, phenylethyl alcohol, and sorbic acid.
26. The ophthalmic composition of claim 1 , which is a topical ophthalmic composition.
27. The ophthalmic composition of claim 1 , which is packaged in a unit dose form.
28. The ophthalmic composition of claim 1 , which is packaged in a multidose form.
29. The ophthalmic composition of claim 1 , which is in a plastic storage container.