Compositions for treating glaucoma or reducing intraocular pressure
Described herein are compounds and compositions for treating glaucoma and/or reducing intraocular pressure. Compositions may comprise an isoquinoline compound and a prostaglandin or a prostaglandin analog. Compounds described herein include those in which an isoquinoline compound is covalently linked to a prostaglandin or a prostaglandin analog, and those in which an isoquinoline compound and a prostaglandin free acid together form a salt.
1. A pharmaceutical composition comprising about 0.01% (w/v) to about 1.0% (w/v) of a dimesylate salt of (S)-4-(3-amino-1-(isoquinolin-6-ylamino)-1-oxopropan-2-yl)benzyl 2,4-dimethylbenzoate and at least one excipient.
2. The pharmaceutical composition of claim 1 , wherein the at least one excipient is a tonicity agent.
3. The pharmaceutical composition of claim 2 , wherein the tonicity agent is mannitol.
4. The pharmaceutical composition of claim 3 , wherein the mannitol is D-mannitol.
5. The pharmaceutical composition of claim 4 , wherein the D-mannitol is about 4.7% (w/v) of the pharmaceutical composition.
6. The pharmaceutical composition of claim 2 , further comprising a buffer.
7. The pharmaceutical composition of claim 6 , wherein the buffer is boric acid and the pH of the pharmaceutical composition is about 5.0.
8. The pharmaceutical composition of claim 7 , wherein the boric acid is about 0.05% (w/v) of the pharmaceutical composition.
9. The pharmaceutical composition of claim 5 , further comprising a buffer.
10. The pharmaceutical composition of claim 9 , wherein the buffer is boric acid and the pH of the pharmaceutical composition is about 5.0.
11. The pharmaceutical composition of claim 10 , wherein the boric acid is about 0.05% (w/v) of the pharmaceutical composition.
12. The pharmaceutical composition of claim 6 , further comprising a preservative.
13. The pharmaceutical composition of claim 12 , wherein the preservative is benzalkonium chloride.
14. The pharmaceutical composition of claim 13 , wherein the benzalkonium chloride is about 0.015% (w/v) of the pharmaceutical composition.
15. The pharmaceutical composition of claim 11 , further comprising a preservative.
16. The pharmaceutical composition of claim 15 , wherein the preservative is benzalkonium chloride.
17. The pharmaceutical composition of claim 16 , wherein the benzalkonium chloride is about 0.015% (w/v) of the pharmaceutical composition.
18. The pharmaceutical composition of claim 1 , comprising at least about 0.020% (w/v) to less than about 0.05% (w/v) of the dimesylate salt of (S)-4-(3-amino-1-(isoquinolin-6-ylamino)-1-oxopropan-2-yl)benzyl 2,4-dimethylbenzoate.
19. A pharmaceutical composition comprising:
(a) about 0.01% (w/v) to about 1.0% (w/v) of a dimesylate salt of (S)-4-(3-amino-1-(isoquinolin-6-ylamino)-1-oxopropan-2-yl)benzyl 2,4-dimethylbenzoate;
(b) boric acid;
(c) mannitol; and
(d) benzalkonium chloride.
20. The pharmaceutical composition of claim 19 , comprising at least about 0.020% (w/v) to less than about 0.05% (w/v) of the dimesylate salt of (S)-4-(3-amino-1-(isoquinolin-6-ylamino)-1-oxopropan-2-yl)benzyl 2,4-dimethylbenzoate.
21. A pharmaceutical composition comprising:
(a) about 0.01% (w/v) to about 1.0% (w/v) of a dimesylate salt of (S)-4-(3-amino-1-(isoquinolin-6-ylamino)-1-oxopropan-2-yl)benzyl 2,4-dimethylbenzoate;
(b) about 0.05% (w/v) boric acid;
(c) about 4.7% (w/v) D-mannitol; and
(d) about 0.015% (w/v) benzalkonium chloride,
wherein the pharmaceutical composition has a pH of about 5.0.
22. The pharmaceutical composition of claim 21 , comprising at least about 0.020% (w/v) to less than about 0.05% (w/v) of the dimesylate salt of (S)-4-(3-amino-1-(isoquinolin-6-ylamino)-1-oxopropan-2-yl)benzyl 2,4-dimethylbenzoate.