# US 11,110,059 B2 · Liquid formulations of hypoglycaemic sulfonamides

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- Number: US 11,110,059 B2
- Document ID: US11110059B2
- Status: Granted
- Kind: B2
- Application number: 14/380,080
- Filed: 2013-02-28
- Published: 2015-02-19
- Granted: 2021-09-07
- Earliest claimed: 2012-02-28
- Assignees: Ammtek
- Applicants: Ammtek
- Inventors: Marianne Berdugo Polak
- Web page: https://patentgrep.com/patent/US11110059B2

## CPC

- A61K 9/10: Dispersions; Emulsions
- A61K 9/0048: {Eye, e.g. artificial tears}
- A61K 31/64: Sulfonylureas, e.g. glibenclamide, tolbutamide, chlorpropamide
- A61K 47/38: Cellulose; Derivatives thereof
- A61P 3/00: Drugs for disorders of the metabolism (of the blood or the extracellular fluid A61P7/00)
- A61P 3/10: for hyperglycaemia, e.g. antidiabetics
- A61P 25/00: Drugs for disorders of the nervous system
- A61P 27/00: Drugs for disorders of the senses
- A61P 27/02: Ophthalmic agents
- A61P 27/16: Otologicals
- 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 present invention relates to a liquid pharmaceutical formulation of hypoglycaemic sulfonamide, intended for oral or ophthalmic administration. The present invention relates in particular to an oral formulation particularly suitable for paediatric use.

## Claims

### Claim 1

A liquid pharmaceutical formulation comprising between 0.5 and 7 mg/mL of micronized particles of glibenclamide, between 4.5 and 5.5 mg/mL of hydroxyethylcellulose, between 4.5 and 5.5 mg/mL of xanthan gum, a buffer system maintaining the pH of said formulation between 4.5 and 5.5, and between 4.5 and 5.5 mg/mL of sodium benzoate, wherein said formulation has osmolality below 400 mOsm/L, wherein the buffer system comprises lactic acid and between 6.75 and 8.25 mg/mL sodium citrate, wherein at least 90% of the micronized particles have a size less than 30 m, and wherein said formulation lacks a sugar-based sweetener.

### Claim 2 (depends on 1)

The formulation according to claim 1, wherein said formulation comprises between 0.6 and 6 mg/mL of glibenclamide, approximately 5 mg/mL of hydroxyethylcellulose, approximately 5 mg/mL of xanthan gum, approximately 5 mg/mL of sodium benzoate, and a buffer system composed of lactic acid and approximately 7.5 mg/mL sodium citrate and maintaining a pH at approximately 4.8.

### Claim 3 (depends on 1)

The liquid pharmaceutical formulation according to claim 1, said formulation lacking a flavouring agent and a colouring agent.

### Claim 4 (depends on 1)

The liquid pharmaceutical formulation of claim 1, wherein the formulation has a pH of approximately 4.8.

### Claim 5 (depends on 1)

A method of treating a disease selected from type 2 diabetes, monogenic diabetes mellitus, or transient neonatal hyperglycaemia in humans or animals comprising administering a formulation according to claim 1 to a human or animal having type 2 diabetes, monogenic diabetes mellitus, or transient neonatal hyperglycaemia.

### Claim 6 (depends on 5)

The method according to claim 5, wherein said formulation is administered to a human selected from the group consisting of an infant, a young child, a person suffering from swallowing disorders and an elderly person.

### Claim 7 (depends on 6)

The method according to claim 6, wherein the human is a premature infant.

### Claim 8 (depends on 5)

The method according to claim 5, wherein said disease is type 2 diabetes.

### Claim 9 (depends on 5)

The method according to claim 5, wherein said disease is monogenic diabetes mellitus and is selected from the group consisting of neonatal diabetes, juvenile diabetes involving the same molecular mechanisms as those of neonatal diabetes, and mitochondrial diabetes associated with deafness (MIDD) and MODY diabetes.

### Claim 10 (depends on 5)

The method according to claim 5, wherein said disease is transient neonatal hyperglycaemia.