FORMULATION
Stable formulations of Olopatadine, methods of making such formulations and methods of treatment using such formulations are provided.
1 . A pharmaceutical composition comprising an aqueous solution of 11-(3 dimethylaminopropylidene)-6,11-dihydrodibenz(b,e) oxepin-2-acetic acid or a pharmaceutically acceptable salt thereof, and polyvinyl alcohol at a concentration of greater than 0.50% w/w and less than 1.75% w/w, wherein the pH is between 5.0 and 8.0, preferably between 6.8 and 7.2, and the osmolality is between 260 and 340 mOsm/kg.
2 . The pharmaceutical composition of claim 1 , wherein the 11-(3 dimethylamino)propylidene]-6-11-dihydrodibenz[b,e]oxepin-2-acetic acid is 11-([Z]-3 dimethylaminopropylidene)-6-11dihydrodibenz(b,e) oxepin-2-acetic acid.
3 . The pharmaceutical composition of claim 1 , wherein the 11-(3 dimethylaminopropylidene)-6,11-dihydrodibenz(b,e) oxepin-2-acetic acid is present in an amount between 0.5 mg/mL and 3.0 mg/mL.
4 . The pharmaceutical composition of claim 1 , wherein the 11-(3 dimethylaminopropylidene)-6,11-dihydrodibenz(b,e) oxepin-2-acetic acid is present in an amount between 1.5 mg/mL and 2.5 mg/mL.
5 . The pharmaceutical composition of claim 1 , further comprising a chelating agent.
6 . The pharmaceutical composition of claim 1 , further comprising a buffer.
7 . The pharmaceutical composition of claim 6 , further wherein the buffer is disodium phosphate and sodium chloride.
8 . The pharmaceutical composition of claim 1 , wherein the formulation is free of benzalkonium chloride.
9 . The pharmaceutical composition of claim 1 , wherein the formulation is free of polymeric quaternary ammonium compounds.
10 . The pharmaceutical composition of claim 1 , wherein the formulation is free of any preservative.
11 . The pharmaceutical composition of claim 1 , wherein the formulation is free of povidone.
12 . The pharmaceutical composition of claim 1 , wherein the formulation is free of benzalkonium chloride and free of povidone.
13 . The pharmaceutical composition of claim 1 , wherein the polyvinyl alcohol is at a concentration of between 0.60 and 1.50% w/w.
14 . The pharmaceutical composition of claim 1 , wherein the polyvinyl alcohol is at a concentration of between 0.75 and 1.35% w/w.
15 . A pharmaceutical composition comprising an aqueous solution containing 11-[(Z)-3-(Dimethylamino)propylidene]-6-11-dihydrodibenz[b,e]oxepin-2-acetic acid present in an amount between 1.5 mg/mL and 2.5 mg/mL, polyvinyl alcohol at a concentration of between 0.50 and 1.75% w/w, disodium phosphate, sodium chloride, and EDTA, and wherein the pH of the composition is between 5.0 and 8.0, preferably between 6.8 and 7.2, and the osmolality is between 260 and 340 mOsm/kg.
16 . The pharmaceutical composition of claim 15 , wherein the pharmaceutical composition is free of benzalkonium chloride and free of povidone.
17 . The pharmaceutical composition of claim 16 , wherein the pharmaceutical composition is free of any preservative.
18 . A method of treating an allergic condition comprising administering topically to the eye a pharmaceutical composition of claim 1 .
19 . A method of treating an allergic condition comprising administering topically to the eye a pharmaceutical composition of claim 15 .