Compositions and methods for the treatment of presbyopia
The invention provides compositions and methods for the treatment of presbyopia. The compositions preferably use aceclidine separate or together with a cycloplegic agent and/or with a nonionic surfactant and viscosity enhancer, and or with low concentrations of a selective α-2 adrenergic receptor agonist.
1. An ophthalmological composition for the treatment of presbyopia comprising aceclidine at a concentration from about 0.25% to about 2.0% w/v and a cycloplegic agent at a concentration from about 0.025% to about 0.1% w/v, wherein w/v denotes weight by volume.
2. The ophthalmological composition according to claim 1 ,
wherein the cycloplegic agent is tropicamide.
3. The ophthalmological composition according to claim 1 , further comprising brimonidine.
4. The ophthalmological composition according to claim 1 further comprising a surfactant selected from the group consisting of an anionic surfactant, a nonionic surfactant, and a combination thereof.
5. The ophthalmological composition according to claim 4 further comprising a viscosity enhancer.
6. The ophthalmological composition according to claim 5 wherein:
the viscosity enhancer is carboxymethyl cellulose or hydroxypropylmethyl cellulose;
the anionic surfactant is selected from the group consisting of a gamma cyclodextrin, sulfobutylether β-cyclodextrin, 2-hydroxypropyl cyclodextrin, sodium lauryl sulfate and sodium ester lauryl sulfate; and the nonionic surfactant is selected from the group consisting of polyoxyl stearate, a poloxamer, a polysorbate, sorbitan monolaurate, sorbitan monopalmitate, sorbitan monostearate, sorbitan monooleate, a polyoxyl alkyl, a polyoxyl stearate, a cyclodextrin and derivatives thereof.
7. The ophthalmological composition according to claim 2 wherein aceclidine is at a concentration from about 1.35% to about 1.55% w/v and tropicamide is at a concentration of about 0.042% w/v.
8. A method of treating presbyopia comprising administering to a subject in need thereof aceclidine at a concentration from about 0.25% to about 2.0% w/v and further comprising administering concurrently or sequentially an ophthalmological composition comprising a cycloplegic agent at a concentration from about 0.025% to about 0.1% w/v, wherein w/v denotes weight by volume.
9. The method of claim 8 wherein the cycloplegic agent is tropicamide at a concentration of 0.042% w/v and wherein the ophthalmological composition further comprises:
hydroxypropylmethyl cellulose;
sodium chloride at a concentration from about 0.05% to about 1.1% w/v;
glycerin at a concentration of about 0.2% w/v; and
citrate at a concentration of about 0.2% w/v or a phosphate buffer at a concentration from about 5 to about 10 millimoles, and
wherein w/v denotes weight by volume.
10. The method of claim 8 wherein the cycloplegic agent is tropicamide at a concentration of 0.042% w/v and wherein the ophthalmological composition further comprises:
hydroxypropylmethyl cellulose;
sodium chloride at a concentration from about 0.05% to about 1.1% w/v;
polyoxyl 40 stearate at a concentration of about 5.5% w/v; and
citrate at a concentration of about 0.2% w/v or a phosphate buffer at a concentration from about 5 to about 10 millimoles, and
wherein w/v denotes weight by volume.
11. The method of claim 8 wherein the aceclidine and the ophthalmological composition are administered from one device with at least two chambers and wherein the aceclidine resides in a first chamber and the ophthalmological composition resides in a second chamber and wherein the aceclidine first contacts the ophthalmological composition at the time of administration.
12. The method of claim 8 wherein the aceclidine resides in a first vial and the ophthalmological composition resides in a second vial and the aceclidine first contacts the ophthalmological composition at the time of administration.
13. The ophthalmological composition according to claim 7 further comprising a surfactant at a concentration of about 5.5% w/v.
14. The ophthalmological composition according to claim 13 wherein the surfactant is polyoxyl 40 stearate.
15. An ophthalmological composition for the treatment of presbyopia comprising aceclidine at a concentration from about 1.40 to about 1.45% w/v, tropicamide at a concentration of about 0.042% w/v, polyoxyl 40 stearate at a concentration of about 5.5% w/v, and hydroxypropylmethyl cellulose, wherein w/v denotes weight by volume.