# US 12,109,202 B2 · Fixed dose combination of cholinesterase inhibitor and a quaternary ammonium antimuscarinic agent to treat neurodegenerative cognitive disorders

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- Number: US 12,109,202 B2
- Document ID: US12109202B2
- Status: Granted
- Kind: B2
- Application number: 17/163,010
- Filed: 2021-01-29
- Published: 2022-08-04
- Granted: 2024-10-08
- Earliest claimed: 2021-01-29
- Assignees: Qaam Pharmaceuticals, LLC
- Applicants: QAAM Pharmaceuticals, LLC
- Inventors: Steven A Rich
- Web page: https://patentgrep.com/patent/US12109202B2

## CPC

- A61K 31/27: of carbamic or thiocarbamic acids, meprobamate, carbachol, neostigmine
- A61K 31/438: The ring being spiro-condensed with carbocyclic or heterocyclic ring systems
- A61K 9/0053: {Mouth and digestive tract, i.e. intraoral and peroral administration}
- A61K 9/4825: {Proteins, e.g. gelatin (gelatin capsule shells with substantial amounts of other macromolecular substances A61K9/4816)}
- A61K 9/4866: {Organic macromolecular compounds}
- A61K 9/7023: {Transdermal patches and similar drug-containing composite devices, e.g. cataplasms (galenical aspects of iontophoretic devices A61K9/0009; microneedle arrays A61K9/0021; buccal patches A61K9/006)}
- A61K 31/165: having aromatic rings, e.g. colchicine, atenolol, progabide
- A61K 31/40: having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
- A61K 31/4015: having oxo groups directly attached to the heterocyclic ring, e.g. piracetam, ethosuximide
- A61K 31/46: 8-Azabicyclo [3.2.1] octane; Derivatives thereof, e.g. atropine, cocaine
- A61K 45/06: Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
- A61P 25/28: for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
- A61K 9/4808: {characterised by the form of the capsule or the structure of the filling; Capsules containing small tablets; Capsules with outer layer for immediate drug release (capsules filled with granules or microparticles A61K9/16; filled with microcapsules or coated microparticles A61K9/50; with mixture of different granules, microcapsules, (coated) microparticles A61K9/5084)}
- 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 includes a method for improving cognitive function in a human suffering from a neurodegenerative cognitive disorder. The method comprises administering to a patient a total daily dose of a cholinesterase inhibitor and a quaternary ammonium antimuscarinic compound. The total daily dose is divided into one or more doses administered before food intake. The quaternary ammonium antimuscarinic compound is administered in a first drug delivery element configured for rapid absorption into a body of the patient, and the cholinesterase inhibitor is administered in a second drug delivery element configured for a slower or delayed absorption into the body of the patient.

## Claims

### Claim 1

A drug delivery element comprising:
a first portion configured to release a therapeutic amount of 2-8 mg of a quaternary ammonium antimuscarinic compound into the human body, the first portion having a first dissolve rate; and
a second portion configured to release a therapeutic amount of 3-48 mg of a cholinesterase inhibitor into a human body, the second portion having a second dissolve rate,
wherein the first dissolve rate is faster than the second dissolve rate.

### Claim 2 (depends on 1)

The drug delivery element of claim 1, wherein the cholinesterase inhibitor includes rivastigmine, and the quaternary ammonium antimuscarinic compound includes glycopyrrolate or trospium.

### Claim 3 (depends on 1)

The drug delivery element of claim 1, wherein the first portion is
configured for rapid dissolution, and the second portion is enclosed, acid resistant, and
configured for delayed release in a small intestine of the human body.

### Claim 4 (depends on 1)

The drug delivery element of claim 1, wherein the first portion includes a gelatin capsule and the second portion includes a hydroxypropylmethylcellulose capsule.

### Claim 5 (depends on 1)

The drug delivery element of claim 1, wherein the first portion is a first capsule and the second portion is a second capsule contained within the first capsule.