IP Library Granted Patent US 9,844,530
Granted Patent B1
US 9,844,530 · App. 15/728,283 · Granted Dec 19, 2017

Ophthalmic solutions for glaucoma and conjunctivitis treatment

Inventors: George Anastassov (New York, NY); Lekhram Changoer (Ridderkerk, NL)
Assignee: Axim Biotechnologies, Inc.
A61K31/352A61K9/0048A61K31/05A61K9/08
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Quick Facts
Patent No.
US 9,844,530
App. No.
15/728,283
Granted
Dec 19, 2017
Kind
B1
Abstract

This invention generally relates to methods of treatment of glaucoma and symptomatic relief of conjunctival inflammation. An ophthalmic solution comprising cannabinoids for the treatment of glaucoma and an ophthalmic solution comprising cannabinoids for these purposes are disclosed. Cannabinoids are selected to achieve the specific purpose of the respective ophthalmic solution.

Claims (39)

1. A method to treat glaucoma in a human subject in need thereof, comprising the steps of:

(a) placing between 1 to 5 drops of an ophthalmic solution in each of the eyes of a human subject having glaucoma, the ophthalmic solution comprising:

Δ 9 -tetrahydrocannabinols at 0.1 to 0.5 weight percent, cannabidiol at 0.1 to 0.5 weight percent, and cannabigerol at 0.05 to 0.5 weight percent;

a thickener selected from the group consisting of cyclodextrins, hydroxymethyl cellulose, hydroxylpropyl methyl cellulose, hydroxylpropyl cellulose, polyvinyl alcohol, carboxyvinyl polymer, polyvinylpyrrolidone, carboxymethyl cellulose, polyacrylic acid, sodium polyacrylate, and sodium alginate;

a solubilizer selected from the group consisting of polysorbate 80, polyoxyethylene hydrogenated castor oil 60, macrogol 4000, polyvinyl alcohol, tyloxapol, polyoxyethylene, polyoxypropylene glycol, and soybean oil;

a buffer selected from the group consisting of sodium phosphate, sodium dihydrogen phosphate, sodium dihydrogen phosphate dihydrate, disodium hydrogen phosphate, disodium hydrogen phosphate dodecahydrate, potassium phosphate, potassium dihydrogen phosphate, dipotassium hydrogen phosphate, sodium borate, potassium acetate, sodium acetate, sodium citrate, disodium citrate, sodium carbonate, and sodium hydrogen carbonate; and

water;

(b) the human subject closing his or her eyelids for at least 10 seconds; and

(c) repeating the application twice daily.

2. The method of claim 1 , wherein the ophthalmic solution comprises:

(a) Δ 9 -tetrahydrocannabinols is present in the ophthalmic solution at 0.1 to 0.2 weight percent;

(b) cannabidiol is present in the ophthalmic solution at 0.15 to 0.3 weight percent; and

(c) cannabigerol is present in ophthalmic solution at 0.1 to 0.3 weight percent.

3. The method of claim 1 , wherein Δ 9 -tetrahydrocannabinols, cannabidiol, and cannabigerol are encapsulated in liposomal capsules.

4. The method of claim 1 , wherein Δ 9 -tetrahydrocannabinols, cannabidiol, and cannabigerol are complexed with β-cyclodextrin.

5. The method of claim 1 , wherein the thickener in the ophthalmic solution is present at 0.1 to 2 weight percent.

6. The method of claim 1 , wherein the solubilizer in the ophthalmic solution is present at 0.5 to 3 weight percent.

7. The method of claim 1 , wherein the ophthalmic solution further comprises an antiseptic agent.

8. The method of claim 7 , wherein the antiseptic agent is selected from the group consisting of benzalkonium chloride, benzodecinium bromide, chlorhexidine gluconate, benzethonium chloride, sorbic acid, potassium sorbate, methyl parahydroxybenzoate, ethyl parahydroxybenzoate, and butyl parahydrobenzoate.

9. The method of claim 7 , wherein the ophthalmic solution further comprises a pH adjusting agent.

10. The method of claim 9 , wherein the pH adjusting agent is selected from the group consisting of lactic acid, citric acid, phosphoric acid, acetic acid, sodium hydroxide, potassium hydroxide, sodium carbonate, and sodium hydrogen carbonate.

11. A method to treat conjunctivitis in a human subject in need thereof comprising the steps of:

(a) applying between 1 to 3 drops of an ophthalmic solution in the eye of a human subject presenting with conjunctivitis, the ophthalmic solution comprising:

cannabidiol at 0.05 to 0.5 weight percent and cannabigerol at 0.05 to 0.5 weight percent;

a thickener selected from the group consisting of cyclodextrins, hydroxymethyl cellulose or any other macrocyclic olygosaccharide, hydroxylpropyl methyl cellulose, hydroxylpropyl cellulose, polyvinyl alcohol, carboxyvinyl polymer, polyvinylpyrrolidone, carboxymethyl cellulose, polyacrylic acid, sodium polyacrylate, and sodium alginate;

a solubilizer selected from the group consisting of polysorbate 80, polyoxyethylene hydrogenated castor oil 60, macrogol 4000, polyvinyl alcohol, tyloxapol, polyoxyethylene, polyoxypropylene glycol, and soybean oil;

a buffer selected from the group consisting of sodium phosphate, sodium dihydrogen phosphate, sodium dihydrogen phosphate dihydrate, disodium hydrogen phosphate, disodium hydrogen phosphate dodecahydrate, potassium phosphate, potassium dihydrogen phosphate, dipotassium hydrogen phosphate, sodium borate, potassium acetate, sodium acetate, sodium citrate, disodium citrate, sodium carbonate, and sodium hydrogen carbonate; and

a balanced saline solution;

(b) the human subject closing his or her eyelids for at least 5 seconds; and

(c) repeating the application twice daily.

12. The method of claim 11 , wherein:

(a) cannabidiol in the ophthalmic solution is present at 0.1 to 0.3 weight percent; and

(b) cannabigerol in the ophthalmic solution is present at 0.1 to 0.3 weight percent.

13. The method of claim 11 , wherein cannabidiol and cannabigerol are encapsulated in liposomal capsules.

14. The method of claim 11 , wherein cannabidiol and cannabigerol are complexed with β-cyclodextrin.

15. The method of claim 11 , wherein the thickener in the ophthalmic solution is present at 0.1 to 2 weight percent.

16. The method of claim 11 , wherein the solubilizer in the ophthalmic solution is present at 0.5 to 3 weight percent.

17. The method of claim 11 , wherein the ophthalmic solution further comprises a pH adjusting agent.

18. The method of claim 17 , wherein the pH adjusting agent is selected from the group consisting of lactic acid, citric acid, phosphoric acid, acetic acid, sodium hydroxide, potassium hydroxide, sodium carbonate, and sodium hydrogen carbonate.

Assignments (2)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded May 26, 2020
From: AXIM BIOTECHNOLOGIES, INC.
To: APIRX PHARMACEUTICAL USA, LLC
Reel/Frame 052752/0519 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Nov 15, 2017
From: ANASTASSOV, GEORGE; CHANGOER, LEKHRAM
To: AXIM BIOTECHNOLOGIES, INC.
Reel/Frame 044131/0803 →
Continuity (2)
Division 14982610 · Dec 29, 2015
Provisional Application 62098007 · Dec 30, 2014