Compositions and methods for the treatment of presbyopia

1. An ophthalmological composition for the treatment of presbyopia comprising from about 0.5% to about 2.5% w/v pilocarpine or a pharmaceutically acceptable salt, ester, or prodrug thereof, tropicamide, a surfactant and a viscosity enhancer, wherein w/v denotes weight by volume.

2. The composition of claim 1 wherein:

(i) the surfactant is selected from polyoxyl 40 stearate, a gamma cyclodextrin, sulfobutylether β-cyclodextrin, 2-hydroxypropyl cyclodextrin, sodium lauryl sulfate, sodium ester lauryl sulfate, a poloxamer, a polysorbate, sorbitan monolaurate, sorbitan monopalmitate, sorbitan monostearate, sorbitan monooleate, a polyoxyl alkyl, a cyclodextrin and combinations thereof; and

(ii) the viscosity enhancer is selected from the group consisting of guar gum, hydroxypropyl-guar, xanthan gum, alginate, chitosan, gellan gum, hyauluronic acid, dextran, and a carbomer.

3. The composition of claim 2 wherein the surfactant is polyoxyl 40 stearate and the viscosity enhancer is carbomer 940.

4. The composition of claim 3 wherein:

tropicamide is at a concentration from about 0.010% to about 0.1% w/v;

polyoxyl 40 stearate is at a concentration from about 2.0% to about 10.0% w/v; and

carbomer 940 is at a concentration from about 0.01% to about 1.0% w/v.

5. The composition of claim 4 wherein:

pilocarpine is at a concentration of about 1% w/v;

tropicamide is at a concentration of about 0.015% w/v;

polyoxyl 40 stearate is at a concentration of about 5.5% w/v; and

carbomer 940 is at a concentration of about 0.5% w/v.

6. The composition of claim 3 further comprising an antioxidant selected from the group consisting of citrate, citric acid monohydrate, ethylenediaminetetraacetic acid, disodium ethylenediaminetetraacetic acid, dicalcium diethylenetriamine pentaacetic acid and combinations thereof and a buffer selected from the group consisting of acetate buffer, citrate buffer, phosphate buffer and citrophosphate buffer.

7. The composition of claim 6 wherein the antioxidant is citric acid monohydrate and the buffer is acetate buffer.

8. The composition of claim 7 wherein citric acid monohydrate is at a concentration from about 0.1% to about 0.2% w/v and acetate buffer is at a concentration from about 1 millimolar to about 5 millimolar.

9. The composition of claim 8 wherein:

pilocarpine is at a concentration of about 1.5% w/v;

tropicamide is at a concentration of about 0.035% w/v;

polyoxyl 40 stearate is at a concentration of about 5.5% w/v;

carbomer 940 is at a concentration of about 0.5% w/v;

citric acid monohydrate is at a concentration of about 0.1% w/v; and

acetate buffer is at a concentration of about 3 millimolar.

10. The composition of claim 8 wherein:

pilocarpine is at a concentration of about 1.5% w/v;

tropicamide is at a concentration of about 0.038% w/v;

polyoxyl 40 stearate is at a concentration of about 5.5% w/v;

carbomer 940 is at a concentration of about 0.85% w/v;

citric acid monohydrate is at a concentration of about 0.1% w/v; and

acetate buffer is at a concentration of about 3 millimolar.

11. A method of treating presbyopia comprising administering a therapeutically effective amount of a composition of claim 1 to a patient in need thereof.

12. The method of claim 11 wherein distance vision acuity of the patient is not reduced.

13. An ophthalmological composition for the treatment of presbyopia comprising:

pilocarpine or a pharmaceutically acceptable salt, ester, or prodrug thereof at a concentration of about 1.5% w/v;

tropicamide at a concentration of about 0.035% w/v;

polyoxyl 40 stearate at a concentration of about 5.5% w/v;

carbomer 940 at a concentration of about 0.85% w/v;

citric acid monohydrate at a concentration of about 0.1% w/v; and

acetate buffer at a concentration of about 3 millimolar, wherein w/v denotes weight by volume.

14. The composition of claim 13 wherein the composition has a pH from about 4 to about 7.

15. The composition of claim 13 wherein the pH is about 5.

16. A method of treating presbyopia comprising administering a therapeutically effective amount of a composition of claim 13 to a patient in need thereof.

17. The method of claim 16 wherein distance vision acuity of the patient is not reduced.

18. An ophthalmological composition for the treatment of presbyopia comprising:

pilocarpine or a pharmaceutically acceptable salt, ester, or prodrug thereof at a concentration of about 0.95% w/v;

tropicamide at a concentration of about 0.012% w/v;

polyoxyl 40 stearate at a concentration of about 3.85% w/v;

carbomer 940 at a concentration of about 0.50% w/v;

citric acid monohydrate at a concentration of about 0.1% w/v; and

acetate buffer at a concentration of about 3.0 millimolar, wherein w/v denotes weight by volume.

19. A method of treating presbyopia comprising administering a therapeutically effective amount of a composition of claim 18 to a patient in need thereof.

20. The method of claim 19 wherein distance vision acuity of the patient is not reduced.