# US 2016/0250334 A1 · Acetylcysteine Compositions and Methods of use Thereof

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- Number: US 2016/0250334 A1
- Document ID: US20160250334A1
- Status: Published application
- Kind: A1
- Application number: 15/087,782
- Filed: 2016-03-31
- Published: 2016-09-01
- Earliest claimed: 2010-07-21
- Assignees: Cumberland Pharmaceuticals Inc.
- Applicants: Cumberland Pharmaceuticals, Inc.
- Inventors: Leo Pavliv; Amy Rock
- Web page: https://patentgrep.com/patent/US20160250334A1

## CPC

- A61K 47/02: Inorganic compounds
- 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 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 31/198: 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)
- A61P 1/16: for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
- A61P 39/02: Antidotes
- 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

A pharmaceutical composition and method for providing a reduction in side effects for human patients in need of therapy comprising the administration of a pharmaceutical composition comprising acetylcysteine is disclosed.

## Claims

### Claim 1

A method of treating a patient with a pharmaceutical composition, comprising:
administering to a patient in need thereof a therapeutically effective amount of a pharmaceutically acceptable composition comprising acetylcysteine and a pH adjusting agent, wherein the composition is substantially free of chelating agents, the pharmaceutical composition providing for a reduction in side effects as compared to an acetylcysteine composition containing chelating agents.

### Claim 2 (depends on 1)

The method of claim 1, wherein the composition contains from about 0.1% to about 50% of acetylcysteine.

### Claim 3 (depends on 2)

The method of claim 2, wherein the composition comprised from about 1.0% to about 25% acetylcysteine.

### Claim 4 (depends on 3)

The method of claim 3, wherein the composition contains about 20% acetylcysteine.

### Claim 5 (depends on 3)

The method of claim 3, wherein the composition contains about 10% acetylcysteine.

### Claim 6 (depends on 2)

The method of claim 2, wherein the composition contains less than about 0.05% chelating agent.

### Claim 7 (depends on 1)

The method of claim 1, wherein the pH adjusting agent is present in an amount to provide a pH of the composition of about 6 to about 8.

### Claim 8 (depends on 7)

The method of claim 7, wherein the pH adjusting agent is present in an amount to provide a pH of the composition of about 6.8.

### Claim 9 (depends on 1)

The method of claim 1, wherein the reduction of side effect is selected from the group consisting of tachycardia, nausea, vomiting, pharyngitis, rhinorrhea, rhonci, pruritis, rash, flushing, anaphylaxis, and combinations thereof.

### Claim 10 (depends on 1)

The method of claim 1, wherein the composition is administered to treat acetaminophen overdose and the therapeutically effective amount is administered intravenously at a dose of about 200 mg/kg over a period of about 3 to about 5 hours followed by a second dose at 100 mg/kg over 16 hours.

### Claim 11 (depends on 10)

The method of claim 10, wherein the composition is administered intravenously at a dose of about 200 mg/kg over a period of about 4 hours followed by a second dose at 100 mg/kg over 16 hours.

### Claim 12

A method of treatment, comprising intravenously administering a 300 mg/kg dose of acetylcysteine to a patient in need of treatment with acetylcysteine over 20 hours via a 2-bag infusion regimen comprising a first dose of 200 mg/kg delivered over a time period from about 3 to about 5 hours, followed by a second dose of 100 mg/kg over 16 hours.

### Claim 13 (depends on 12)

The method of claim 12, further comprising determining if the patient has achieved clinically significant improvement in liver function over the course of the 20 hour treatment, and if not, continuing the administration of acetylcysteine to the patient beyond 21 hours to achieve significant clinical improvement in liver function.

### Claim 14 (depends on 12)

The method of claim 12, further comprising administering to the patient either a repeat course of the entire treatment protocol (300 mg/kg over 21 hours) or a repeat course of the maintenance dose (100 mg/kg over 16 hours).

### Claim 15 (depends on 12)

The method of claim 12, further comprising continuing the treatment with an acetylcysteine infusion at 6.25 mg/kg per hour beyond 21 hours.

### Claim 16 (depends on 12)

The method of claim 12, wherein the first dose is administered over a time period of about 4 hours.

### Claim 17

An improvement in a method of intravenously administering a 300 mg/kg dose of acetylcysteine to a patient in need of treatment with acetylcysteine over 20 hours, the improvement comprising decreasing the initial rate of acetylcysteine infusion to 50 mg/kg per hour and maintaining that rate of infusion for 4 hours.

### Claim 18 (depends on 17)

The method of claim 17, further comprising thereafter intravenously delivering a second dose of 100 mg/kg acetylcysteine to the patient over 16 hours.

### Claim 19 (depends on 18)

The method of claim 18, further comprising determining if the patient has achieved clinically significant improvement in liver function over the course of the 20 hour treatment, and if not, continuing the administration of acetylcysteine to the patient beyond 21 hours to achieve significant clinical improvement in liver function.

### Claim 20 (depends on 19)

The method of claim 19, further comprising administering to the patient either a repeat course of the entire treatment protocol (300 mg/kg over 21 hours) or a repeat course of the maintenance dose (100 mg/kg over 16 hours).

### Claim 21 (depends on 20)

The method of claim 20, further comprising continuing the treatment with an acetylcysteine infusion at 6.25 mg/kg per hour beyond 21 hours.

### Claim 22

A pharmaceutical composition, consisting of comprising 6 g acetylcysteine, an effective amount of sodium hydroxide to provide a pH in the range from about 6.0 to about 7.5, and a sufficient amount of sterile water for injection, USP to provide a total volume of 30 mL (200 mg/mL).

### Claim 23 (depends on 22)

The pharmaceutical composition of claim 22, having a pH from about 6.0 to about 7.0.

### Claim 24 (depends on 23)

The pharmaceutical composition of claim 23, which is packaged in 30-mL glass vials.

### Claim 25

A pharmaceutical composition, consisting of an amount of acetylcysteine effective to provide a dose of 200 mg per kg of weight of a human patient, an effective amount of sodium hydroxide to provide a pH in the range from about 6.0 to about 7.5, sterile water for injection, in 1000 mL 0.45% Sodium Chloride Injection.

### Claim 26

A pharmaceutical composition, consisting of an amount of acetylcysteine effective to provide a dose of 100 mg per kg of weight of a human patient, an effective amount of sodium hydroxide to provide a pH in the range from about 6.0 to about 7.5, sterile water for injection, in 500 mL 0.45% Sodium Chloride Injection.

### Claim 27

A pharmaceutical composition, consisting of an amount of acetylcysteine effective to provide an effective dose of acetylcysteine to a human patient, an effective amount of sodium hydroxide to provide a pH in the range from about 6.0 to about 7.5, sterile water for injection, and sodium chloride.

### Claim 28 (depends on 27)

The pharmaceutical composition of claim 27, which contains from about 10 to about 400 mg/mL acetylcysteine.