# US 12,213,985 B2 · Oral cannabinoid formulations

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- Number: US 12,213,985 B2
- Document ID: US12213985B2
- Status: Granted
- Kind: B2
- Application number: 17/689,245
- Filed: 2022-03-08
- Published: 2022-11-17
- Granted: 2025-02-04
- Earliest claimed: 2016-07-01
- Assignees: Jazz Pharmaceuticals Research UK Limited
- Applicants: Jazz Pharmaceuticals Research UK Limited
- Inventors: Harshit Shah
- Web page: https://patentgrep.com/patent/US12213985B2

## CPC

- A61K 31/658: {o-phenolic cannabinoids, e.g. cannabidiol, cannabigerolic acid, cannabichromene or tetrahydrocannabinol}
- 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 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 47/14: Esters of carboxylic acids, e.g. fatty acid monoglycerides, medium-chain triglycerides, parabens or PEG fatty acid esters
- A61K 47/183: {Amino acids, e.g. glycine, EDTA or aspartame}
- A61K 47/44: Oils, fats or waxes according to two or more groups of A61K47/02-A61K47/42; Natural or modified natural oils, fats or waxes, e.g. castor oil, polyethoxylated castor oil, montan wax, lignite, shellac, rosin, beeswax or lanolin (synthetic glycerides, e.g. medium-chain triglycerides, A61K47/14)
- A61P 25/08: Antiepileptics; Anticonvulsants
- 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)
- A61P: SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS

## Abstract

The present invention relates to a cannabinoid containing oral solution. Preferably the oral solution comprises a cannabinoid, a lipid solvent, a sweetener and ethanol, characterised in that the sweetener is an ultrahigh potency sweetener.

## Claims

### Claim 1

A method of treating a disease or disorder, the method comprising orally administering to a subject in need thereof a therapeutically effective amount of a pharmaceutical formulation comprising:
cannabidiol (CBD);
a lipid solvent;
an ultrahigh potency sweetener; and
ethanol, wherein ethanol has a concentration of less than about 3% v/v, and
wherein the disease or disorder is epilepsy or a syndrome associated therewith, schizophrenia, tuberous sclerosis complex, brain tumors, neuropathic pain, cannabis use disorder. post-traumatic stress disorder, anxiety, early psychosis, Alzheimer's Disease, or autism.

### Claim 2 (depends on 1)

The method of claim 1, wherein the ultrahigh potency sweetener has a sweetness intensity that is 1000× greater than a sweetness intensity of sucrose.

### Claim 3 (depends on 1)

The method of claim 1, wherein the ultrahigh potency sweetener has a sweetness intensity that is 5000× greater than a sweetness intensity of sucrose.

### Claim 4 (depends on 1)

The method of claim 1, wherein the ultrahigh potency sweetener is (N—[N-(3,3-dimethylbutyl)-L-α-aspartyl]-L-phenylalanine 1-methyl ester) (neotame).

### Claim 5 (depends on 1)

The method of claim 1, wherein the ultrahigh potency sweetener is N—[N-3-(3-hydroxy-4methoxyphenyl)propyl-α-L-aspartyl]-L-phenylalanine 1-methyl ester) (advantame).

### Claim 6 (depends on 1)

The method of claim 1, further comprising a flavorant.

### Claim 7 (depends on 6)

The method of claim 6, wherein the CBD is present in an amount of from 5 to 40% (w/v), the ethanol is present in an amount of less than 2% (v/v), the ultrahigh potency sweetener is present in an amount of less than 0.05% (w/v), the flavorant is present in an amount of less 0.2% (w/v) and the lipid solvent is q.s. to 100%.

### Claim 8 (depends on 7)

The method of claim 7, wherein the ultrahigh potency sweetener is Neotame, the flavorant is strawberry flavor and the lipid solvent is sesame oil.

### Claim 9 (depends on 1)

The method of claim 1, wherein the formulation is stable in climatic zones I and II for up to 24 months at 25° C.

### Claim 10 (depends on 1)

The method of claim 1, wherein the formulation is stable in climatic zones III and IV for up to 18 months at 30° C.

### Claim 11 (depends on 1)

The method of claim 1, wherein the solution lacks a stabilizing agent.

### Claim 12 (depends on 8)

The method of claim 8, wherein the formulation is stable in climatic zones I and II for up to 24 months at 25° C.

### Claim 13 (depends on 8)

The method of claim 8, wherein the formulation is stable in climatic zones III and IV for up to 18 months at 30° C.

### Claim 14 (depends on 8)

The method of claim 8, wherein the solution lacks a stabilizing agent.

### Claim 15 (depends on 1)

The method of claim 1, the ultrahigh potency sweetener is Neotame, and the lipid solvent is sesame oil.

### Claim 16 (depends on 1)

The method of claim 1, wherein the concentration of ethanol is less than about 2% (v/v).

### Claim 17 (depends on 1)

The method of claim 1, wherein the concentration of ethanol ranges from about 0.5% (v/v) to 3% (v/v).

### Claim 18 (depends on 1)

The method of claim 1, wherein the lipid solvent is sesame oil.

### Claim 19 (depends on 1)

The method of claim 1, wherein:
the CBD is present in an amount ranging from 5 to 40% (w/v);
the ethanol is present in an amount ranging from 0.5% (v/v) to 2% (v/v);
the ultrahigh potency sweetener is present in an amount ranging from 0.01% (w/v) to 0.0025%;
flavorant is present in an amount of less 0.2% (w/v); and
sesame oil is q.s. to 100%.

### Claim 20 (depends on 1)

The method of claim 1, wherein the CBD is present in an extract.

### Claim 21 (depends on 1)

The method of claim 1, wherein the subject is a human.

### Claim 22 (depends on 1)

The method of claim 1, wherein the disease or disorder is epilepsy or a syndrome associated therewith.

### Claim 23 (depends on 22)

The method of claim 22, wherein the syndrome associated with epilepsy is Dravet Syndrome, Lennox Gastaut Syndrome, myoclonic seizures, juvenile myoclonic epilepsy, refractory epilepsy, juvenile spasms, West syndrome, infantile spasms, or refractory infantile spasms.

### Claim 24 (depends on 23)

The method of claim 23, wherein the syndrome is associated with epilepsy is Dravet Syndrome.

### Claim 25 (depends on 23)

The method of claim 23, wherein the syndrome is associated with epilepsy is Lennox Gastaut Syndrome.

### Claim 26 (depends on 23)

The method of claim 23, wherein the syndrome is associated with epilepsy is tuberous sclerosis complex.

### Claim 27 (depends on 23)

The method of claim 23, wherein the syndrome is associated with epilepsy is myoclonic seizures.