# US 10,478,406 B2 · High-pH solid-state epinephrine formulation

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- Number: US 10,478,406 B2
- Document ID: US10478406B2
- Status: Granted
- Kind: B2
- Application number: 16/355,941
- Filed: 2019-03-18
- Published: 2019-07-11
- Granted: 2019-11-19
- Earliest claimed: 2019-03-18
- Assignees: HARC Therapeutics AG
- Applicants: HARC Therapeutics AG
- Inventors: Robert Chisholm
- Web page: https://patentgrep.com/patent/US10478406B2

## CPC

- A61K 31/137: Arylalkylamines, e.g. amphetamine, epinephrine, salbutamol, ephedrine {or methadone}
- A61K 9/1658: {Proteins, e.g. albumin, gelatin}
- A61K 9/2018: {Sugars, or sugar alcohols, e.g. lactose, mannitol; Derivatives thereof, e.g. polysorbates}
- A61K 9/2063: {Proteins, e.g. gelatin}
- A61K 9/2095: {Tabletting processes}
- A61K 9/1611: {Inorganic compounds}
- A61K 9/1623: {Sugars or sugar alcohols, e.g. lactose; Derivatives thereof; Homeopathic globules}
- A61K 9/19: lyophilised {, i.e. freeze-dried, solutions or dispersions (lyophilised products with subsequent particle size reduction A61K9/14; granules or pellets made by lyphilisation A61K9/1682; solid oral dosage forms made by lyophilisation A61K9/2095; lyophilisation additives A61K47/00)}
- A61K 9/2009: {Inorganic compounds}
- 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)

## Abstract

Epinephrine formulated in aqueous solvent at a basic pH of about 8.5 remains in solid state. My data show that epinephrine formulated at a pH of about 8.5 is surprisingly resistant to oxidation. I here teach how to formulate solid-state epinephrine in basic solution, and how to use solid-state epinephrine to make pharmaceutical dosage forms.

## Claims

### Claim 1

A process for manufacturing a solid-state epinephrine pharmaceutical dosage form, the process comprising: mixing epinephrine in an aqueous solvent and at least one basic-pH excipient to produce a mixture having a pH of about 8.5, whereby the epinephrine remains in solid state,
wherein the mixture comprises an antioxidant and a chelating agent,
wherein the process comprises the step of removing the aqueous solvent to produce a dry dosage form, and
wherein the dry dosage form is a tablet.