# US 11,439,611 B2 · Administration of serine protease inhibitors to the stomach

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- Number: US 11,439,611 B2
- Document ID: US11439611B2
- Status: Granted
- Kind: B2
- Application number: 16/989,148
- Filed: 2020-08-10
- Published: 2021-06-17
- Granted: 2022-09-13
- Earliest claimed: 2010-09-23
- Assignees: Leading BioSciences, Inc.; The Regents of the University of California
- Applicants: Leading Biosciences, Inc.; The Regents of the University of California
- Inventors: Geert W. Schmid-Schonbein; Yung-Tsai (Andrew) Lee; Jeng Wei
- Web page: https://patentgrep.com/patent/US11439611B2

## CPC

- A61K 31/195: having an amino group
- A61K 9/0053: {Mouth and digestive tract, i.e. intraoral and peroral administration}
- A61K 31/10: Sulfides; Sulfoxides; Sulfones
- A61K 31/145: having sulfur, e.g. thiurams (>N—C(S)—S—C(S)—N< and >N—C(S)—S—S—C(S)—N<), Sulfinylamines (—N=SO), Sulfonylamines (—N=SO2) (isothiourea A61K31/155)
- A61K 31/155: Amidines ([IMAGE cpc-sch-A61K-1029.gif]), e.g. guanidine (H2N—C(=NH)—NH2), isourea (N=C(OH)—NH2), isothiourea (—N=C(SH)—NH2)
- A61K 31/185: Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids (hydroxamic acids A61K31/16; peroxy acids A61K31/327)
- A61K 31/19: Carboxylic acids, e.g. valproic acid (salicylic acid A61K31/60)
- A61K 31/216: of acids having aromatic rings, e.g. benactizyne, clofibrate
- A61K 31/24: having an amino or nitro group
- A61K 31/661: Phosphorus acids or esters thereof not having P—C bonds, e.g. fosfosal, dichlorvos, malathion {or mevinphos}
- A61K 31/765: Polymers containing oxygen
- A61K 38/1722: {Plasma globulins, lactoglobulins}
- A61K 38/57: from animals; from humans {(A61K38/553, A61K38/556 take precedence)}
- A61K 47/02: Inorganic compounds
- A61K 47/10: Alcohols; Phenols; Salts thereof, e.g. glycerol; Polyethylene glycols [PEG]; Poloxamers; PEG/POE alkyl ethers
- A61P 1/00: Drugs for disorders of the alimentary tract or the digestive system
- A61P 9/00: Drugs for disorders of the cardiovascular system
- A61P 25/00: Drugs for disorders of the nervous system
- A61K 9/08: Solutions {(composition of solutions A61K47/00)}
- 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

The inventors have unexpectedly discovered that shock and/or potential multi-organ failure due to shock can be effectively treated by administration of liquid high-dose protease inhibitor formulations to a location upstream of where pancreatic proteases are introduced into the gastrointestinal tract. Most preferably, administration is directly to the stomach, for example, via nasogastric tube under a protocol effective to treat shock by such administration without the need of providing significant quantities of the protease inhibitor to the jejunum and/or ileum.

## Claims

### Claim 1

A liquid formulation comprising from 0.16 wt % to 1.8 wt % of tranexamic acid, polyethylene glycol, and electrolytes; wherein the liquid formulation is an isotonic aqueous solution and the liquid formulation has a volume of 250 ml to 1000 ml.

### Claim 2 (depends on 1)

The liquid formulation of claim 1, wherein the polyethylene glycol is polyethylene glycol 3350.

### Claim 3 (depends on 1)

The liquid formulation of claim 1 having a volume from 500 ml to 1000 ml.