Claims for Patent: 10,052,313

Summary for Patent: 10,052,313

Title:	Compositions and methods for the treatment of presbyopia
Abstract:	The invention provides compositions and methods for the treatment of presbyopia. The compositions preferably comprise aceclidine and a polyol. The compositions optionally contain a cycloplegic agent, a surfactant, a viscosity enhancer, an osmolarity modifier and a preservative.
Inventor(s):	Gerald Horn, Lee Nordan
Assignee:	Lenz Therapeutics Operations Inc
Application Number:	US15/235,431
Patent Claims:	1. An ophthalmological composition for the treatment of presbyopia comprising: an active agent selected from the group consisting of about 1.75% w/v aceclidine and a mixture of about 1.75% w/v aceclidine and tropicamide; and about 2.5% w/v mannitol, wherein w/v denotes weight by volume of the total composition. 2. The ophthalmological composition of claim 1, further comprising: about 1.0% to about 6.0% w/v of a nonionic surfactant; and about 0.1% to about 2.25% w/v hydroxypropylmethyl cellulose. 3. The ophthalmological composition of claim 2, further comprising: about 0.10% to about 0.12% w/v sorbic acid; and about 0.005% to about 0.02% w/v benzalkonium chloride. 4. The ophthalmological composition of claim 3, further comprising one or more antioxidants selected from the group consisting of ethylenediaminetetraacetic acid (EDTA), ethylenediaminetetraacetic acid dihydrate, sodium citrate and citrate buffer. 5. The ophthalmological composition of claim 4, wherein the one or more antioxidants consist of: ethylenediaminetetraacetic acid dihydrate; and sodium citrate or citrate buffer. 6. The ophthalmological composition of claim 2, wherein the nonionic surfactant is selected from a polysorbate, tyloxapol, a poloxamer, a cyclodextrin, vitamin E TPGS and a polyoxyl. 7. The ophthalmological composition of claim 2, wherein the nonionic surfactant is polysorbate 80. 8. The ophthalmological composition of claim 7, wherein the concentration of polysorbate 80 is from about 1.0% to about 5.0% w/v and the concentration of hydroxypropylmethyl cellulose is from about 0.75% to about 1.5% w/v. 9. The ophthalmological composition of claim 7, wherein the concentration of polysorbate 80 is from about 2.0% to about 4.0% w/v and the concentration of hydroxypropylmethyl cellulose is from about 1.0% to about 1.25% w/v. 10. The ophthalmological composition of claim 1 wherein the active agent is a mixture of 1.75% w/v aceclidine and tropicamide and wherein tropicamide is at a concentration from: about 0.004% to 0.015% w/v. 11. A method of treating presbyopia comprising administering to a subject in need thereof the ophthalmological composition of claim 1. 12. A method of treating irregular astigmatism, keratoconic ectasia, night vision halos/starbursts, night vision reduced contrast, and low myopia, or hyperopia, with or without astigmatism, comprising administering to a subject in need thereof the ophthalmological composition of claim 1. 13. An ophthalmological composition for the treatment of presbyopia comprising: an exclusive active agent selected from the group consisting of about 1.75% w/v aceclidine and a mixture of about 1.75% w/v aceclidine and about 0.01% w/v tropicamide; about 2.5% w/v mannitol; about 4.0% w/v polysorbate 80; about 1.25% w/v hydroxypropylmethyl cellulose; about 0.12% w/v sorbic acid; about 0.1% w/v ethylenediaminetetraacetic acid dihydrate; about 0.02% w/v benzalkonium chloride; and about 0.1% w/v sodium citrate or citrate buffer, wherein w/v denotes weight by volume of the total composition. 14. A method of treating presbyopia comprising administering to a subject in need thereof the ophthalmological composition of claim 13. 15. A method of treating presbyopia comprising administering to a subject in need thereof the ophthalmological composition of claim 13, wherein near vision acuity of the subject is improved by at about 4 lines of resolution or more for at least 8 hours. 16. A method of treating irregular astigmatism, keratoconic ectasia, night vision halos/starbursts, night vision reduced contrast and low myopia, or hyperopia, with or without astigmatism, comprising administering to a subject in need thereof the ophthalmological composition of claim 13. 17. A method of stabilizing aceclidine comprising providing a first composition comprising about 1.75% w/v aceclidine and about 2.5% w/v mannitol in a first chamber and a second composition comprising about 0.01% w/v tropicamide, about 4.0% w/v polysorbate 80, about 1.25% w/v hydroxypropylmethyl cellulose, about 0.12% w/v sorbic acid, about 0.1% w/v ethylenediaminetetraacetic acid dihydrate, about 0.02% w/v benzalkonium chloride and about 0.1% w/v sodium citrate or citrate buffer in a second chamber, wherein upon mixing the first composition and the second composition the efficacy of aceclidine is maintained for at least one month, wherein w/v denotes weight by total volume after mixing of the first and second composition. 18. A method of inhibiting microbial and fungal growth comprising the following steps: (i) providing an ophthalmological composition comprising about 1.75% w/v aceclidine, (ii) about 2.5% w/v mannitol, about 0.01% w/v tropicamide, about 4.0% w/v polysorbate (iii) 80 and about 1.25% w/v hydroxypropylmethyl cellulose; (iv) adding from about 0.10% to 0.12% w/v sorbic acid; and (v) adding one or more of about 0.1% w/v ethylenediaminetetraacetic acid dihydrate and about 0.1% w/v sodium citrate or citrate buffer, wherein w/v denotes weight by volume of the total composition.