More potent and less toxic formulations of epinephrine and methods of medical use

• US 9,283,197 B1
• Filed: 08/15/2014
• Issued: 03/15/2016
• Est. Priority Date: 08/15/2014
• Status: Active Grant

• Current Assignee: Belcher Pharmaceuticals LLC, Eton Pharmaceuticals, Inc.
• Original Assignee: Jugal K. Taneja
• Inventors: Taneja, Jugal K.
• Primary Examiner(s): Padmanabhan, Sreeni
• Assistant Examiner(s): Karol, Jody
• Application Number:
  US14/460,845
• Time in Patent Office: 578 Days
• US Class Current: 1/1
• CPC Class Codes: A61K 31/137 Arylalkylamines, e.g. amphetamine, epinephrine, salbutamol, ephedrine or methadone
• CPC Class Codes: 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

Abstract

The present invention provides pharmaceutical formulations of levorotatory-epinephrine, l-epinephrine, more potent and less toxic than existing pharmaceutical formulations of epinephrine, along with methods of producing and using these pharmaceutical formulations of l-epinephrine.

Claims

1. A liquid pharmaceutical formulation of preservative-free and sulfite-free, 1 mg per mL l-epinephrine sterile solution for uses including injection;

said liquid pharmaceutical formulation having a pH between 2.8 and 3.3;

said liquid pharmaceutical formulation compounded in an aqueous solution as 1.0 to 1.06 mg/mL l-epinephrine, and further including a tonicity agent;

said liquid pharmaceutical formulation having no more than 6.5% total impurities at release, including no more than 6% d-epinephrine and no more than 0.5% adrenalone, and no more than 12.5% total impurities over a shelf-life of at least 12 months, including no more than 12% d-epinephrine and no more than 0.5% adrenalone;

said liquid pharmaceutical formulation stored in a container with an inert gas prior to use.

2. The said liquid pharmaceutical formulation of claim 1 compounded in an aqueous solution preferably as 1.03 mg/mL l-epinephrine.

3. The said liquid pharmaceutical formulation of claim 1 further having no more than 12.5% total impurities over a shelf-life of at least 15 months, including no more than 12% d-epinephrine and no more than 0.5% adrenalone.

4. A liquid pharmaceutical formulation of preservative-free and sulfite-free, 1 mg per mL l-epinephrine sterile solution for uses including injection;

said liquid pharmaceutical formulation having a pH between 2.8 and 3.3;

said liquid pharmaceutical formulation compounded as 1.0 to 1.06 mg/mL l-epinephrine, along with 8.6 mg/mL sodium chloride as the tonicity agent, 7.26 mg/mL of 1 Normal hydrochloric acid as the dissolution agent, 987.11 mg/mL water for injection as a solvent, and with additional hydrochloric acid to adjust pH;

said liquid pharmaceutical formulation having less than 6.5% total impurities at release, including less than 6% d-epinephrine and less than 0.5% adrenalone, and less than 12.5% total impurities over a shelf-life of at least 12 months, including less than 12% d-epinephrine and less than 0.5% adrenalone.

5. The said liquid pharmaceutical formulation of claim 4 compounded in an aqueous solution as 1.03 mg/mL l-epinephrine.

6. An injectable liquid pharmaceutical formulation of l-epinephrine sterile solution;

said liquid pharmaceutical formulation having a pH between 2.8 and 3.3;

said injectable liquid pharmaceutical formulation compounded in an aqueous solution as 1.0 to 1.06 mg/mL l-epinephrine, and further including a tonicity agent;

said liquid pharmaceutical formulation including no more than about 6% d-epinephrine and no more than about 0.5% adrenalone at release, and no more than about 12% d-epinephrine and no more than about 0.5% adrenalone over a shelf-life of at least 12 months.

7. The said injectable liquid pharmaceutical formulation of claim 6 further having a concentration of 1 mg per mL l-epinephrine.