# US 11,298,330 B2 · Magnesium compositions and methods of use

> Agents: this data is available as JSON from the patentgrep API and MCP server — see https://patentgrep.com/llms.txt

- Number: US 11,298,330 B2
- Document ID: US11298330B2
- Status: Granted
- Kind: B2
- Application number: 16/663,993
- Filed: 2019-10-25
- Published: 2020-04-23
- Granted: 2022-04-12
- Earliest claimed: 2017-04-26
- Assignees: Neurocentria, Inc.
- Applicants: Neurocentria, Inc.
- Inventors: Guosong Liu; Fei Mao; Jason Weinger
- Web page: https://patentgrep.com/patent/US11298330B2

## CPC

- A61K 31/191: having two or more hydroxy groups, e.g. gluconic acid
- A61K 31/198: Alpha-amino acids, e.g. alanine or edetic acid [EDTA] (betaine A61K31/205; proline A61K31/401; tryptophan A61K31/405; histidine A61K31/4172; peptides not degraded to individual amino acids A61K38/00)
- A61K 9/20: Pills, tablets, {discs, rods (A61K9/0004, A61K9/0007, A61K9/0056, A61K9/0065 take precedence; for reconstitution of a drink A61K9/0095)}
- A61K 33/06: Aluminium, calcium or magnesium; Compounds thereof {, e.g. clay}
- 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: 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 provides a method of administering magnesium threonate to a subject in need of supplementing magnesium. At least a portion of magnesium (Mg) and threonate (T) is present in a salt form of MgT2. The method may comprise administration of magnesium threonate at two different time points per day. The method may comprise administering, at a first time point, a first oral dosage form comprising magnesium threonate. The method may comprise administering, at a second time point, a combination of the first oral dosage form and a second oral dosage form comprising magnesium threonate. The first and second oral dosage forms may exhibit different dissolution profiles in a dissolution medium.

## Claims

### Claim 1

A method of administering magnesium threonate to a subject in need of supplementing magnesium, wherein at least a portion of magnesium (Mg) and threonate (T) of said magnesium threonate is present in a salt form of MgT2, the method comprising:
(a) administering a first oral dosage form comprising magnesium threonate; and
(b) administering a combination of (i) said first oral dosage form and (ii) a second oral dosage form comprising magnesium threonate, wherein said first and second oral dosage forms exhibit different in vitro dissolution profiles in a dissolution medium,
wherein said first oral dosage form and said combination of said first and second oral dosage forms are administered at two different time points per day, and
wherein magnesium threonate is present in an amount between about 200 mg to 2000 mg in each of said first and second oral dosage forms.

### Claim 2 (depends on 1)

The method of claim 1, wherein a first in vitro dissolution profile of said first oral dosage form in said dissolution medium is slower than a second in vitro dissolution profile of said second oral dosage form in said dissolution medium.

### Claim 3 (depends on 2)

The method of claim 2, wherein:
(a) said first in vitro dissolution profile ranges between (i) about 10% to 35% in about 1 hour, (ii) about 20% to 50% in about 2 hours, (iii) greater than about 80% in about 4 hours, (iv) greater than about 90% in about 6 hours, and (v) greater or equal to about 95% in about 8 hours as measured using a USP type II (paddle) dissolution system at 75 rpm, at a temperature of about 37° C.;
(b) said second in vitro dissolution profile ranges between (i) greater than or equal to about 50% in about 0.5 hour and (ii) greater or equal to about 80% in about 1 hour as measured using a USP type II (paddle) dissolution system at 75 rpm, at a temperature of about 37° C.; and
(c) said combination of said first and second oral dosage forms exhibits a third in vitro dissolution profile ranging between (i) about 50% to 75% in about 1 hour, (ii) greater than about 60% in about 2 hours, and (iii) greater than about 80% in about 4 hours as measured using a USP type II (paddle) dissolution system at 75 rpm, at a temperature of about 37° C.

### Claim 4 (depends on 1)

The method of claim 1, wherein a first in vitro dissolution profile of said first oral dosage form in said dissolution medium is faster than a second in vitro dissolution profile of said second oral dosage form in said dissolution medium.

### Claim 5 (depends on 4)

The method of claim 4, wherein:
(a) said first in vitro dissolution profile ranges between (i) greater than or equal to about 50% in about 0.5 hour and (ii) greater or equal to about 80% in about 1 hour as measured using a USP type II (paddle) dissolution system at 75 rpm, at a temperature of about 37° C.;
(b) said second in vitro dissolution profile ranges between (i) about 10% to 35% in about 1 hour, (ii) about 20% to 50% in about 2 hours, (iii) greater than about 80% in about 4 hours, (iv) greater than about 90% in about 6 hours, and (v) greater or equal to about 95% in about 8 hours as measured using a USP type II (paddle) dissolution system at 75 rpm, at a temperature of about 37° C.; and
(c) said combination of said first and second oral dosage forms exhibits a third in vitro dissolution profile ranging between (i) about 50% to 75% in about 1 hour, (ii) greater than about 60% in about 2 hours, and (iii) greater than about 80% in about 4 hours as measured using a USP type II (paddle) dissolution system at 75 rpm, at a temperature of about 37° C.

### Claim 6 (depends on 1)

The method of claim 1, wherein magnesium threonate is present in at least an amount to improve a Mini-Mental State Examination (MMSE) score of said subject.

### Claim 7 (depends on 1)

The method of claim 1, wherein said first and second oral dosage forms have substantially the same amount of magnesium threonate.

### Claim 8 (depends on 1)

The method of claim 1, wherein each of said first and second oral dosage forms is liquid, semi-liquid, semi-solid, or solid.

### Claim 9 (depends on 1)

The method of claim 1, wherein each of said first and second oral dosage forms further comprises an additional agent.

### Claim 10 (depends on 9)

The method of claim 9, wherein said additional agent is a pharmaceutically acceptable carrier selected from the group consisting of micelles, liposomes, microspheres, nanofibers, and any combination thereof.

### Claim 11 (depends on 9)

The method of claim 9, wherein said additional agent is a pharmaceutically acceptable excipient selected from the group consisting of a binder, filler, lubricant, dissolution aid, and any combination thereof.

### Claim 12 (depends on 9)

The method of claim 9, wherein said additional agent is a nutritionally active agent.

### Claim 13 (depends on 1)

The method of claim 1, wherein said subject suffers from magnesium deficiency, mild cognitive impairment, short-term memory loss, long-term memory loss, Alzheimer's disease, Parkinson's disease, Huntington's disease, autism, schizophrenia, cognitive decline, depression, dementia, attention deficit hyperactivity disorder (ADHD), amyotrophic lateral sclerosis (ALS), diabetes, cardiovascular disease, hypertension, migraine, glaucoma, mood disorder, stress, anxiety, depression, sleep disorder, metabolic disorder, fatigue, cancer, HIV, hepatitis, spinal cord injury, post-surgery recovery, post-traumatic stress disorder, arthritis, neuropathic pain, inflammation, and/or tremor.

### Claim 14

A kit for administering magnesium threonate to a subject in need of supplementing magnesium, wherein at least a portion of magnesium (Mg) and threonate (T) of said magnesium threonate is present in a salt form of MgT2, the kit comprising:
(a) two of a first oral dosage form comprising magnesium threonate;
(b) one of a second oral dosage form comprising magnesium threonate; and
(c) a set of instructions for instructing said subject on (i) consuming said first oral dosage form in daytime, and (ii) consuming a combination of said first and second oral dosage forms at once in nighttime,
wherein said first and second oral dosage forms (i) contain magnesium threonate in an amount between about 200 mg to 2000 mg, and (ii) exhibit different in vitro dissolution profiles in a dissolution medium.

### Claim 15 (depends on 14)

The kit of claim 14, formulated such that the kit provides an amount of said first and second oral dosage forms to be utilized by said subject for at least one month.

### Claim 16 (depends on 14)

The kit of claim 14, wherein a first in vitro dissolution profile of said first oral dosage form in said dissolution medium is slower than a second in vitro dissolution profile of said second oral dosage form in said dissolution medium.

### Claim 17 (depends on 16)

The kit of claim 16, wherein:
(a) said first in vitro dissolution profile ranges between (i) about 10 to 35% in about 1 hour, (ii) about 20% to 50% in about 2 hours, (iii) greater than about 80% in about 4 hours, (iv) greater than about 90% in about 6 hours, and (v) greater or equal to about 95% in about 8 hours as measured using a USP type II (paddle) dissolution system at 75 rpm, at a temperature of about 37° C.;
(b) said second in vitro dissolution profile ranges between (i) greater than or equal to about 50% in about 0.5 hour and (ii) greater or equal to about 80% in about 1 hour as measured using a USP type II (paddle) dissolution system at 75 rpm, at a temperature of about 37° C.; and
(c) said combination of said first and second oral dosage forms exhibits a third in vitro dissolution profile ranging between (i) about 50% to 75% in about 1 hour, (ii) greater than about 60% in about 2 hours, and (iii) greater than about 80% in about 4 hours as measured using a USP type II (paddle) dissolution system at 75 rpm, at a temperature of about 37° C.

### Claim 18 (depends on 14)

The kit of claim 14, wherein a first in vitro dissolution profile of said first oral dosage form in said dissolution medium is faster than a second in vitro dissolution profile of said second oral dosage form in said dissolution medium.

### Claim 19 (depends on 14)

The kit of claim 14, wherein:
(a) said first in vitro dissolution profile ranges between (i) greater than or equal to about 50% in about 0.5 hour and (ii) greater or equal to about 80% in about 1 hour as measured using a USP type II (paddle) dissolution system at 75 rpm, at a temperature of about 37° C.;
(b) said second in vitro dissolution ranges between (i) about 10% to 35% in about 1 hour, (ii) about 20% to 50% in about 2 hours, (iii) greater than about 80% in about 4 hours, (iv) greater than about 90% in about 6 hours, and (v) greater or equal to about 95% in about 8 hours as measured using a USP type II (paddle) dissolution system at 75 rpm, at a temperature of about 37° C.; and
(c) said combination of said first and second oral dosage forms exhibits a third in vitro dissolution profile ranging between (i) about 50% to 75% in about 1 hour, (ii) greater than about 60% in about 2 hours, and (iii) greater than about 80% in about 4 hours as measured using a USP type II (paddle) dissolution system at 75 rpm, at a temperature of about 37° C.