Compositions and methods for the treatment of presbyopia
The invention provides compositions and methods for the treatment of presbyopia. The methods preferably comprise storing an aceclidine composition in a container having a headspace at a temperature from about 2 to about 8 degrees Celsius. The methods further comprise filling the container under an inert gas overlay and/or enclosing the container an anti-leaching material or disposing the container in a second container containing an anti-leaching material.
1. A method of stabilizing a composition comprising about 1.75% w/w aceclidine hydrochloride, about 4.0% w/w polysorbate 80, about 2.5% w/w mannitol, about 1.25% w/w anhydrous hypromellose, about 0.1% w/w disodium edetate dihydrate, and from about 0.077% to about 0.1% w/w anhydrous sodium citrate comprising storing the composition in a container having a headspace at a temperature from about 2 degrees Celsius to about 8 degrees Celsius, wherein w/w denotes weight by total weight of the composition and wherein the composition has a pH from about 5.0 to about 6.0.
2. The method of claim 1 wherein the composition further comprises about 0.01% w/w tropicamide.
3. The method of claim 1 , wherein the composition is filled into the container under an inert gas overlay.
4. The method of claim 3 , wherein the headspace is purged with an inert gas.
5. The method of claim 1 , wherein the method provides at least 90% stability of aceclidine for at least 22 months.
6. A method of stabilizing a composition comprising about 1.75% w/w aceclidine hydrochloride, about 4.0% w/w polysorbate 80, about 2.5% w/w mannitol, about 1.25% w/w anhydrous hypromellose, about 0.1% w/w disodium edetate dihydrate, about 0.02% w/w benzalkonium chloride, about 0.12% w/w sorbic acid and about 0.1% w/w anhydrous sodium citrate comprising storing the composition in a container having a headspace at a temperature from about 2 degrees Celsius to about 8 degrees Celsius, wherein w/w denotes weight by total weight of the composition and wherein the composition has a pH of about 5.0.
7. The method of claim 6 , wherein the composition is filled into the container under an inert gas overlay.
8. The method of claim 7 , wherein the headspace is purged with an inert gas.
9. The method of claim 6 , wherein the method provides at least 90% stability of aceclidine for at least 22 months.
10. A container comprising aceclidine prepared by the process comprising the steps of:
a) providing a container;
b) filling the container with a composition comprising about 1.75% w/w aceclidine hydrochloride, about 4.0% w/w polysorbate 80, about 2.5% w/w mannitol, about 1.25% w/w anhydrous hypromellose, about 0.1% w/w disodium edetate dihydrate, and from about 0.077% to about 0.1% w/w anhydrous sodium citrate under an inert gas overlay;
c) purging a headspace created during the filling step b) with an inert gas; and
d) capping the container,
wherein w/w denotes weight by total weight of the composition and wherein the composition has a pH from about 5.0 to about 6.0.
11. The container of claim 10 , wherein the process further comprises the step of storing the container at a temperature from about 2 to about 8 degrees Celsius.
12. A container comprising aceclidine prepared by the process comprising the steps of:
a) providing a container;
b) filling the container with a composition comprising about 1.75% w/w aceclidine hydrochloride, about 4.0% w/w polysorbate 80, about 2.5% w/w mannitol, about 1.25% w/w anhydrous hypromellose, about 0.1% w/w disodium edetate dihydrate, about 0.02% w/w benzalkonium chloride, about 0.12% w/w sorbic acid and about 0.1% w/w anhydrous sodium citrate under an inert gas overlay;
c) purging a headspace created during the filling step b) with an inert gas; and
d) capping the container,
wherein w/w denotes weight by total weight of the composition and wherein the composition has a pH of about 5.0.
13. The container of claim 12 , wherein the process further comprises the step of storing the container at a temperature from about 2 to about 8 degrees Celsius.