# US 12,213,954 B2 · Colchicine solution

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- Number: US 12,213,954 B2
- Document ID: US12213954B2
- Status: Granted
- Kind: B2
- Application number: 18/681,394
- Filed: 2022-08-08
- Published: 2024-08-22
- Granted: 2025-02-04
- Earliest claimed: 2021-08-06
- Assignees: Pharma-Data Research and Development Single Member S.A.
- Applicants: Pharma-Data Research and Development Single Member S.A.
- Inventors: Ioannis Psarrakis; Konstantinos Lioumis
- Web page: https://patentgrep.com/patent/US12213954B2

## CPC

- A61K 9/0095: {Drinks; Beverages; Syrups; Compositions for reconstitution thereof, e.g. powders or tablets to be dispersed in a glass of water; Veterinary drenches (A61K9/0007 takes precedence; eatable gels or foams A61K9/0056; oral mucosa adhesive forms A61K9/006)}
- A61K 31/165: having aromatic rings, e.g. colchicine, atenolol, progabide
- A61K 9/08: Solutions {(composition of solutions A61K47/00)}
- A61K 47/10: Alcohols; Phenols; Salts thereof, e.g. glycerol; Polyethylene glycols [PEG]; Poloxamers; PEG/POE alkyl ethers
- A61K 47/12: Carboxylic acids; Salts or anhydrides thereof
- A61K 47/14: Esters of carboxylic acids, e.g. fatty acid monoglycerides, medium-chain triglycerides, parabens or PEG fatty acid esters
- A61K 47/36: Polysaccharides; Derivatives thereof, e.g. gums, starch, alginate, dextrin, hyaluronic acid, chitosan, inulin, agar or pectin
- A61K 47/38: Cellulose; Derivatives thereof
- A61K: PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES (devices or methods specially adapted for bringing pharmaceutical products into particular physical or administering forms A61J3/00; chemical aspects of, or use of materials for deodorisation of air, for disinfection or sterilisation, or for bandages, dressings, absorbent pads or surgical articles A61L; soap compositions C11D)

## Abstract

Described is a stable buffered aqueous colchicine solution or suspension being free of benzyl alcohol, comprising colchicine, a water miscible solvent and a preservative, characterized in that the solution comprises 0.01-1.0 w/v % colchicine, 2.5-15.0 w/v % glycerol and 0.05-1 w/v % preservative, the pH of the solution or suspension being 4.5-7.0. A method for the preparation thereof is also disclosed.

## Claims

### Claim 1

A buffered aqueous colchicine solution or suspension being free of benzyl alcohol, propylene glycol and thickener, comprising colchicine, a water miscible solvent and a preservative, wherein the solution or suspension comprises 0.02-1.0 w/v % colchicine, 2.5-15.0 w/v % glycerol and 0.05-1 w/v % preservative, the pH of the solution or suspension being 3.5-7.0.

### Claim 2 (depends on 1)

Buffered aqueous colchicine solution or suspension of claim 1, comprising 0.022-0.035 w/v % colchicine.

### Claim 3 (depends on 1)

Buffered aqueous colchicine solution or suspension of claim 1, comprising 5-12 w/v % glycerol.

### Claim 4 (depends on 1)

Buffered aqueous colchicine solution or suspension of claim 1, comprising 0.10-0.40 w/v % preservative.

### Claim 5 (depends on 1)

Buffered aqueous colchicine solution or suspension of claim 1, wherein the preservative is chosen from the group, consisting of methyl paraben, ethyl paraben, propyl paraben, butyl paraben, sorbic acid, potassium sorbate, and combinations thereof.

### Claim 6 (depends on 1)

Buffered aqueous colchicine solution or suspension of claim 1, having a pH of 4.5-6.5.

### Claim 7 (depends on 1)

Buffered aqueous colchicine solution or suspension of claim 1, comprising 0.05-2.0 w/v % buffering agent.

### Claim 8 (depends on 1)

Buffered aqueous colchicine solution or suspension of claim 1, comprising a buffering agent chosen from the group consisting of hydrochloric acid, acetic acid, ammonia solutions, monoethanolamine, diethanolamine, triethanolamine, meglumine, sodium citrate, citric acid, lactic acid, phosphoric acid, propionic acid, sulphuric acid, tartaric acid, potassium bicarbonate, potassium citrate, potassium hydroxide, sodium bicarbonate, sodium borate, and sodium hydroxide.

### Claim 9 (depends on 1)

Buffered aqueous colchicine solution or suspension of claim 1, comprising 1.0 w/v % or less antioxidant.

### Claim 10 (depends on 9)

Buffered aqueous colchicine solution or suspension of claim 9, wherein the antioxidant is chosen from the group, consisting of butylated hydroxyl anisole, butylated hydroxyl toluene, tocopherol, ascorbyl palmitate, ascorbic acid, sodium metabisulfite, sodium sulphite, sodium thiosulfate, propyl gallate, and combinations thereof.

### Claim 11 (depends on 1)

Buffered aqueous colchicine solution or suspension of claim 1, being free of antioxidant.

### Claim 12 (depends on 1)

Buffered aqueous colchicine solution or suspension of claim 1, comprising a sweetening agent, wherein the amount of sweetening agent in the solution or suspension has a sweetening power that corresponds with the sweetening power of 20-500 w/v % saccharose.

### Claim 13 (depends on 12)

Buffered aqueous colchicine solution or suspension of claim 12, wherein the sweetening agent is an artificial sweetening agent, chosen from the group consisting of sucralose, sodium saccharin, aspartame, alitame, acesulfame-K, cyclamate, stevioside, glycyrrhizin, neohesperidin, dihydrochalcone, thaumatin, and combinations thereof.

### Claim 14 (depends on 1)

Buffered aqueous colchicine solution or suspension of claim 1, comprising 0.05-0.3 w/v % sweetener.

### Claim 15 (depends on 1)

Buffered aqueous colchicine solution or suspension of claim 1, comprising, in addition to glycerol, a water-miscible organic solvent selected from the group consisting of polyols, alcohols, acetone, phthalates, dimethyl sulfoxide, dimethylacetamide, glycofurol, isopropyl myristate, isopropyl palmitate, propylene carbonate, pyrrolidine, glycerine triacetate, triethyl citrate, triolein, and a combination of two or more thereof.

### Claim 16 (depends on 15)

Buffered aqueous colchicine solution or suspension of claim 15, wherein the ratio of the water-miscible organic solvent with glycerol is 1-5:10 glycerol.

### Claim 17 (depends on 1)

Buffered aqueous colchicine solution or suspension of claim 1, comprising 0.05-0.2 w/v % flavouring agent.

### Claim 18 (depends on 17)

Buffered aqueous colchicine solution or suspension of claim 17, wherein the flavouring agent is selected from the group consisting of forest fruits flavour, grapefruit, orange, lime, lemon, mandarin, pineapple, strawberry, raspberry, mango, passion fruit, kiwi, apple, pear, peach, apricot, cherry, grapes, banana, cranberry, blueberry, black currant, red currant, gooseberry, lingonberries, cumin, thyme, basil, chamomile, valerian, fennel, parsley, camomile, tarragon, lavender, dill, bergamot, salvia, aloe vera balsam, spearmint, peppermint, eucalyptus, and combinations of two or more thereof.

### Claim 19 (depends on 1)

Buffered aqueous colchicine solution or suspension of claim 1, wherein the solution or suspension comprises at least 95% colchicine after 24 months storage at 25° C. at a relative humidity of 60% as compared to the amount of colchicine at the beginning of the storage.

### Claim 20 (depends on 1)

Buffered aqueous colchicine solution or suspension of claim 1, wherein the solution or suspension comprises less than 3% total impurities after 24 months storage at 25° C. at a relative humidity of 60%.

### Claim 21 (depends on 15)

Buffered aqueous colchicine solution or suspension of claim 15, wherein the water miscible organic solvent is selected from the group consisting of alkane triols, alkane diols, polyethylene glycol, ethanol, isopropyl alcohol, acetone, dibutyl phthalate, diethyl phthalate, dimethyl phthalate, dimethyl sulfoxide, dimethylacetamide, glycofurol, isopropyl myristate, isopropyl palmitate, propylene carbonate, pyrrolidine, glycerine triacetate, triethyl citrate, triolein, and a combination of two or more thereof.