# US 11,077,119 B2 · Enhanced brain bioavailability of galantamine by selected formulations and transmucosal administration of lipophilic prodrugs

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- Number: US 11,077,119 B2
- Document ID: US11077119B2
- Status: Granted
- Kind: B2
- Application number: 16/287,413
- Filed: 2019-02-27
- Published: 2019-08-29
- Granted: 2021-08-03
- Earliest claimed: 2012-07-27
- Assignees: Neurodyn Life Sciences Inc.
- Applicants: Neurodyn Life Sciences Inc.
- Inventors: Alfred Maelicke
- Web page: https://patentgrep.com/patent/US11077119B2

## CPC

- A61K 31/55: having seven-membered rings, e.g. azelastine, pentylenetetrazole
- A61K 9/0043: {Nose}
- A61K 9/006: {Oral mucosa, e.g. mucoadhesive forms, sublingual droplets; Buccal patches or films; Buccal sprays}
- A61K 9/1075: {Microemulsions or submicron emulsions; Preconcentrates or solids thereof; Micelles, e.g. made of phospholipids or block copolymers (A61K9/0026 takes precedence)}
- A61K 9/14: Particulate form, e.g. powders, {Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles (microspheres A61K9/16; microcapsules A61K9/50; nanocapsules, nanoparticles of the matrix type A61K9/51)}
- A61K 9/2072: {characterised by shape, structure or size; Tablets with holes, special break lines or identification marks; Partially coated tablets; Disintegrating flat shaped forms (A61K9/0004, A61K9/0056, A61K9/0065 take precedence)}
- A61K 9/2086: {Layered tablets, e.g. bilayer tablets; Tablets of the type inert core-active coat (active cores with a complete drug-free outer coat A61K9/28)}
- A61K 9/2846: {Poly(meth)acrylates}
- A61K 9/2886: {having two or more different drug-free coatings; Tablets of the type inert core-drug layer-inactive layer (of the type active core-drug layer-inactive layer A61K9/209)}
- A61K 31/00: Medicinal preparations containing organic active ingredients
- A61P 25/00: Drugs for disorders of the nervous system
- Y02A 50/30: Against vector-borne diseases, e.g. mosquito-borne, fly-borne, tick-borne or waterborne diseases whose impact is exacerbated by climate change
- 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
- Y02A: TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE

## Abstract

A method of treating a subject for a brain disease associated with cognitive impairment, including administering to a subject a chemical substance according to GLN-1062 or salt thereof: wherein the treatment includes transmucosal administration of a therapeutically effective amount of GLN 1062 or salt thereof in the oral cavity of the subject.

## Claims

### Claim 1

A method of treating a subject for a brain disease associated with cognitive impairment, comprising administering to a subject a chemical substance according to GLN 1062 or salt thereof:
wherein said treatment comprises sublingual administration of a therapeutically effective amount of GLN 1062 or salt thereof in the oral cavity of the subject.

### Claim 2 (depends on 1)

The method according to claim 1, wherein GLN1062 is administered as a salt.

### Claim 3 (depends on 1)

The method according to claim 1, wherein the salt comprises stoichiometric and/or non-stoichiometric salts and/or hydrates of GLN 1062, whereby the salt is described as: GLN 1062.n HX.m H2O:
whereby n, m=0-5 and n and m can be the same or different, and HX=an acid.

### Claim 4 (depends on 2)

The method according to claim 2, wherein the GLN1062 salt is a gluconate salt.

### Claim 5 (depends on 2)

The method according to claim 2, wherein the GLN1062 salt is a saccharate salt.

### Claim 6 (depends on 2)

The method according to claim 2, wherein the GLN1062 salt is a maleate salt.

### Claim 7 (depends on 2)

The method according to claim 2, wherein the GLN1062 salt is a lactate salt.

### Claim 8 (depends on 2)

The method according to claim 2, wherein the GLN1062 salt has a solubility in water of at least 10% weight per volume (w/v).

### Claim 9 (depends on 1)

The method according to claim 1, wherein GLN1062 or salt thereof is administered at a dosage of 1 to 100 mg one to three times daily.

### Claim 10 (depends on 1)

The method according to claim 1, wherein GLN1062 or salt thereof is administered at a dosage of 2 to 40 mg twice daily.

### Claim 11 (depends on 1)

The method according to claim 1, wherein the sublingual administration is carried out by administering a therapeutically effective amount of GLN1062 or salt thereof under the tongue by placing a sub-lingual tablet, one or more drops of a solution, or an amount of particulate in the form of freeze-dried powder or emulsion underneath the tongue and/or by spraying the underside of the tongue with a preselected volume of a liquid composition comprising the chemical substance.

### Claim 12 (depends on 11)

The method according to claim 11, wherein the sublingual tablet comprises:
lactose monohydrate, corn starch, polyvinylpyrrolidone (PVP) and/or magnesium stearate, and optionally with a flavouring agent, or
mannitol, sodium starch glycolate, croscarmellose, ascorbic acid and/or magnesium stearate, optionally with a flavouring agent.

### Claim 13 (depends on 1)

The method according to claim 1, wherein the brain disease to be treated is selected from the group consisting of Alzheimer's Disease, Parkinson's disease, dementia, schizophrenia, epilepsy, stroke, poliomyelitis, neuritis, myopathy, oxygen and nutrient deficiencies in the brain after hypoxia, anoxia, asphyxia, cardiac arrest, chronic fatigue syndrome, poisoning, anaesthesia, spinal cord disorders, central inflammatory disorders, postoperative delirium, subsyndronal postoperative delirium, neuropathic pain, abuse of alcohol or drugs, addictive alcohol craving, nicotine craving, and effects of radiotherapy.