# US 9,040,577 B2 · Continuous administration of L-dopa, dopa decarboxylase inhibitors, catechol-O-methyl transferase inhibitors and compositions for same

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- Number: US 9,040,577 B2
- Document ID: US9040577B2
- Status: Granted
- Kind: B2
- Application number: 14/243,625
- Filed: 2014-04-02
- Published: 2014-09-04
- Granted: 2015-05-26
- Earliest claimed: 2010-11-15
- Assignees: NeuroDerm, Ltd.
- Applicants: Neuroderm, Ltd.
- Inventors: Oron Yacoby-Zeevi; Mara Nemas
- Web page: https://patentgrep.com/patent/US9040577B2

## CPC

- 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 9/0014: {Skin, i.e. galenical aspects of topical compositions (non-active ingredients are additionally classified in A61K47/00; A61K9/0009, A61K9/0021, A61K9/7015, A61K9/7023 take precedence; cosmetic preparations A61K8/00, A61Q; preparations for wound dressings or bandages A61L26/00)}
- A61K 9/0019: {Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in an invasive manner (non-active ingredients are additionally classified in A61K47/00)}
- A61K 9/08: Solutions {(composition of solutions A61K47/00)}
- A61K 31/12: Ketones
- A61K 31/122: having the oxygen directly attached to a ring, e.g. quinones, vitamin K1, anthralin
- A61K 31/133: having hydroxy groups, e.g. sphingosine
- A61K 31/195: having an amino group
- A61K 31/197: the amino and the carboxyl groups being attached to the same acyclic carbon chain, e.g. gamma-aminobutyric acid [GABA], beta-alanine, epsilon-aminocaproic acid or pantothenic acid (carnitine A61K31/205)
- A61K 31/277: having a ring, e.g. verapamil
- A61K 47/18: Amines; Amides; Ureas; Quaternary ammonium compounds; Amino acids; Oligopeptides having up to five amino acids
- A61K 47/183: {Amino acids, e.g. glycine, EDTA or aspartame}
- A61K 47/20: containing sulfur, e.g. dimethyl sulfoxide [DMSO], docusate, sodium lauryl sulfate or aminosulfonic acids
- A61K 47/22: Heterocyclic compounds, e.g. ascorbic acid, tocopherol or pyrrolidones
- A61K 47/26: Carbohydrates, e.g. sugar alcohols, amino sugars, nucleic acids, mono-, di- or oligo-saccharides; Derivatives thereof, e.g. polysorbates, sorbitan fatty acid esters or glycyrrhizin
- A61P 25/00: Drugs for disorders of the nervous system
- A61P 25/14: for treating abnormal movements, e.g. chorea, dyskinesia
- A61P 25/16: Anti-Parkinson drugs
- A61P 39/06: Free radical scavengers or antioxidants
- A61P 43/00: Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
- 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

Provided herein, in part, is a method of treating a neurological or movement disorder in a patient in need thereof, comprising subcutaneously administering to said patient a pharmaceutically acceptable composition comprising levodopa and optionally carbidopa and optionally entacapone or tolcapone, or pharmaceutically acceptable salts thereof, wherein said composition is administered substantially continuously, and compositions that can be used in the disclosed methods.

## Claims

### Claim 1

A pharmaceutically acceptable liquid composition comprising:
(a) active components comprising:
(i) about 2% to about 12% by weight levodopa; and
(ii) carbidopa; and
(b) about 5% to about 30% by weight arginine, meglumine, or a combination thereof wherein the liquid composition has a pH of about 9.1 to about 9.8 at 25° C.

### Claim 2 (depends on 1)

The composition of claim 1 comprising about 4% to about 7% levodopa.

### Claim 3 (depends on 2)

The composition of claim 2 comprising about 6% levodopa.

### Claim 4 (depends on 1)

The composition of claim 1 comprising about 9% to about 16% arginine and/or meglumine.

### Claim 5 (depends on 4)

The composition of claim 4 comprising about 15 to 16% by weight arginine and/or meglumine.

### Claim 6 (depends on 1)

The composition of claim 1 comprising about 0.5% to about 3% carbidopa.

### Claim 7 (depends on 6)

The composition of claim 6 comprising about 0.5% to about 1.5% carbidopa.

### Claim 8 (depends on 1)

The composition of claim 1 further comprising ascorbic acid or a salt thereof.

### Claim 9 (depends on 8)

The composition of claim 8, wherein said salt of ascorbic acid is selected from the group consisting of sodium ascorbate, potassium ascorbate, calcium ascorbate, ascorbyl stearate, and ascorbyl palmitate.

### Claim 10 (depends on 1)

The composition of claim 1 comprising ascorbic acid or sodium ascorbate.

### Claim 11 (depends on 10)

The composition of claim 10 comprising ascorbic acid.

### Claim 12 (depends on 11)

The composition of claim 11 comprising about 0.2% to about 2% ascorbic acid.

### Claim 13 (depends on 12)

The composition of claim 12 comprising about 0.5% to about 1% ascorbic acid.

### Claim 14 (depends on 13)

The composition of claim 13 comprising about 0.5% ascorbic acid.

### Claim 15 (depends on 1)

The composition of claim 1 further comprising L-cysteine or N-acetylcysteine (NAC).

### Claim 16

A pharmaceutically acceptable liquid composition comprising:
(a) about 4% to about 7% by weight levodopa;
(b) about 0.5% to about 3% by weight carbidopa; and
(c) about 9% to about 16% by weight arginine and/or meglumine, wherein said composition has a pH of about 9.1 to about 9.8 at 25° C.

### Claim 17 (depends on 16)

The composition of claim 16 further comprising about 0.2% to about 2% by weight ascorbic acid.

### Claim 18 (depends on 16)

The composition of claim 16 further comprising L-cysteine or NAC.

### Claim 19 (depends on 18)

The composition of claim 18 comprising:
(a) about 6% levodopa;
(b) about 0.5% to about 3% carbidopa;
(c) about 15% to about 16% arginine;
(d) about 0.5% ascorbic acid; and
(e) L-cysteine or NAC.

### Claim 20 (depends on 19)

The composition of claim 19 comprising about 0.5% to about 1.5% carbidopa.

### Claim 21 (depends on 20)

An infusion pump comprising the composition of claim 20.
