Pharmaceutical compositions and methods of using the same

• US 10,894,012 B1
• Filed: 06/17/2020
• Issued: 01/19/2021
• Est. Priority Date: 02/07/2017
• Status: Active Grant

• Current Assignee: Noden Pharma Designated Activity Company
• Original Assignee: Genus Lifesciences, Inc. (Vyteris, Inc.)
• Inventors: Moshal, Jeffrey M., Libman, Michael
• Primary Examiner(s): Anderson, James D.
• Application Number:
  US16/903,558
• Time in Patent Office: 216 Days
• CPC Class Codes: A61B 1/233 for the nose, i.e. nasoscopes , e.g. testing of patency of Eustachian tubes
• CPC Class Codes: A61B 17/24 for use in the oral cavity, larynx, bronchial passages or nose for medical inspection of cavities or tubes in the body A61B1/00; Tongue scrapers
• CPC Class Codes: A61B 2017/246 for cleaning of the nose
• CPC Class Codes: A61K 31/46 8-Azabicyclo [3.2.1] octane; Derivatives thereof, e.g. atropine, cocaine
• CPC Class Codes: A61K 47/12 Carboxylic acids; Salts or anhydrides thereof
• CPC Class Codes: A61K 9/0043 Nose
• CPC Class Codes: A61K 9/08 Solutions composition of solutions A61K47/00
• CPC Class Codes: A61M 19/00 Local anaesthesia syringes therefor A61M5/00; Hypothermia A61M5/42 takes precedence; cooling blood in a bypass of the arterial system A61M1/36
• CPC Class Codes: A61P 23/02 Local anaesthetics

Abstract

Novel pharmaceutical compositions including cocaine hydrochloride and methods of treating patients using those pharmaceutical compositions are described.

Claims

1. A method of providing induction of local anesthesia of mucous membranes in an adult patient comprising:

soaking four pledgets in about 4 mL of a pharmaceutical composition comprising about 36 mg/mL to about 44 mg/mL of cocaine hydrochloride, 1.2 mg/mL to 1.4 mg/mL citric acid, 0.7 mg/mL to 1.3 mg/mL sodium benzoate, and water;

placing a maximum of two pledgets of the four pledgets in each nasal cavity of an adult patient for about 10 minutes to about 20 minutes, provided that the method results in an AUC_inf in a range from about 25.0 ng*h/mL to about 370 ng*h/mL of cocaine in the adult patient; and

performing a diagnostic or surgical procedure on or through the nasal cavities in the adult patient;

provided that the method results in a reduction in pain equivalent to achieving a visual numeric rating score of 0 upon von Frey filament testing.

2. The method of claim 1, wherein the procedure is a nasal laryngoscopy.

3. The method of claim 1, wherein the procedure is a nasopharyngeal laryngoscopy.

4. The method of claim 1, wherein the procedure is a nasal endoscopy.

5. The method of claim 1, wherein a length of each of the four pledgets is about 3.0 cm.

6. The method of claim 1, wherein each of the four pledgets has an absorbency sufficient to absorb about 1 mL of the pharmaceutical composition.

7. The method of claim 1, wherein each of the four pledgets is removed from the nasal cavity and retains between about 70% and about 80% of the pharmaceutical composition.

8. A method of providing induction of local anesthesia of mucous membranes in an adult patient comprising:

soaking four pledgets in about 4 mL of a pharmaceutical composition comprising about 36 mg/mL to about 44 mg/mL of cocaine hydrochloride, 1.2 mg/mL to 1.4 mg/mL citric acid, 0.7 mg/mL to 1.3 mg/mL sodium benzoate, and water;

placing a maximum of two pledgets of the four pledgets in each nasal cavity of the adult patient for about 10 minutes to about 20 minutes, provided that the method results in an AUC_inf in a range from about 25.0 ng*h/mL to about 370 ng*h/mL of cocaine in the adult patient;

provided that the method results in a T_max ranging from about 0.02 hours to about 1.00 hours; and

performing a diagnostic or surgical procedure on or through the nasal cavities in the adult patient;

provided that the method results in a reduction in pain equivalent to achieving a visual numeric rating score of 0 upon von Frey filament testing.

9. The method of claim 8, wherein the procedure is a nasal laryngoscopy.

10. The method of claim 8, wherein the procedure is a nasopharyngeal laryngoscopy.

11. The method of claim 8, wherein the procedure is a nasal endoscopy.

12. The method of claim 8, wherein a length of each of the four pledgets is about 3.0 cm.

13. The method of claim 8, wherein each of the four pledgets has an absorbency sufficient to absorb about 1 mL of the pharmaceutical composition.

14. The method of claim 8, wherein each of the four pledgets is removed from the nasal cavity and retains between about 70% and about 80% of the pharmaceutical composition.