# US 10,307,459 B2 · Pharmaceutical formulations of desmopressin

> Agents: this data is available as JSON from the patentgrep API and MCP server — see https://patentgrep.com/llms.txt

- Number: US 10,307,459 B2
- Document ID: US10307459B2
- Status: Granted
- Kind: B2
- Application number: 15/881,123
- Filed: 2018-01-26
- Published: 2018-10-04
- Granted: 2019-06-04
- Earliest claimed: 2002-05-07
- Assignees: Ferring B.V.
- Applicants: Ferring B.V.
- Inventors: Anders Nilsson; Hans Lindner; Jørgen Wittendorff
- Web page: https://patentgrep.com/patent/US10307459B2

## CPC

- A61K 47/42: Proteins; Polypeptides; Degradation products thereof; Derivatives thereof, e.g. albumin, gelatin or zein (oligopeptides having up to five amino acids {A61K47/183}; polyamino acids A61K47/34)
- A61K 9/0056: {Mouth soluble or dispersible forms; Suckable, eatable, chewable coherent forms; Forms rapidly disintegrating in the mouth; Lozenges; Lollipops; Bite capsules; Baked products; Baits or other oral forms for animals}
- A61K 38/08: Peptides having 5 to 11 amino acids {(A61K38/043 - A61K38/046 take precedence)}
- A61K 38/095: Oxytocins; Vasopressins; Related peptides
- A61K 38/12: Cyclic peptides {, e.g. bacitracins; Polymyxins; Gramicidins S, C; Tyrocidins A, B or C (A61K38/043 - A61K38/046 take precedence)}
- A61K 47/12: Carboxylic acids; Salts or anhydrides thereof
- A61K 47/26: Carbohydrates, e.g. sugar alcohols, amino sugars, nucleic acids, mono-, di- or oligo-saccharides; Derivatives thereof, e.g. polysorbates, sorbitan fatty acid esters or glycyrrhizin
- A61P 1/12: Antidiarrhoeals
- A61P 3/10: for hyperglycaemia, e.g. antidiabetics
- A61P 7/00: Drugs for disorders of the blood or the extracellular fluid
- A61P 7/08: Plasma substitutes; Perfusion solutions; Dialytics or haemodialytics; Drugs for electrolytic or acid-base disorders, e.g. hypovolemic shock (artificial tears A61P27/04)
- A61P 7/10: Antioedematous agents; Diuretics
- A61P 7/12: Antidiuretics, e.g. drugs for diabetes insipidus (ADH A61P5/10)
- A61P 13/00: Drugs for disorders of the urinary system
- A61P 13/02: of urine or of the urinary tract, e.g. urine acidifiers
- A61P 13/10: of the bladder
- A61K 9/2013: {Organic compounds, e.g. phospholipids, fats}
- 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: 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

Good bioavailability of desmopressin can be obtained with an orodispersible pharmaceutical dosage form. Preferred dosage forms comprise desmopressin and an open matrix network which is an inert water-soluble or water-dispersible carrier material. Desmopressin formulated in this way is useful for voiding postponement, or the treatment or prevention of incontinence, primary nocturnal enuresis (PNE), nocturia or central diabetes insipidus. Peptides other than desmopressin can also be formulated in this way.

## Claims

### Claim 1

An orodispersible pharmaceutical dosage form of desmopressin comprising:
desmopressin in a form selected from one or more of the free base of desmopressin and a pharmaceutically acceptable salt thereof, in an amount measured as the free base, selected from 25 μg and 50 μg, and
one or more carriers, wherein at least one carrier is gelatin in an open matrix network structure,
wherein the dosage form exhibits a mean elimination half-life of desmopressin after administration of about 2.8 to 3 hours after the maximum plasma concentration is reached.

### Claim 2 (depends on 1)

The dosage form according to claim 1, wherein the gelatin is fish gelatin.

### Claim 3 (depends on 1)

The dosage form according to claim 1, wherein the gelatin is non-gelling fish gelatin.

### Claim 4 (depends on 1)

The dosage form according to claim 1, further comprising mannitol.

### Claim 5 (depends on 1)

The dosage form according to claim 1, further comprising citric acid.

### Claim 6

An orodispersible pharmaceutical dosage form of desmopressin comprising:
desmopressin in a form selected from one or more of the free base of desmopressin and a pharmaceutically acceptable salt thereof, in an amount measured as the free base, selected from 25 μg and 50 μg, and
one or more carriers, wherein at least one carrier is gelatin in an open matrix network structure,
wherein the dosage form exhibits a desmopressin bioavailability after administration of from greater than 0.1% to 0.38%.

### Claim 7 (depends on 6)

The dosage form according to claim 6, wherein the gelatin is fish gelatin.

### Claim 8 (depends on 6)

The dosage form according to claim 6, wherein the gelatin is non-gelling fish gelatin.

### Claim 9 (depends on 6)

The dosage form according to claim 6, further comprising mannitol.

### Claim 10 (depends on 6)

The dosage form according to claim 6, further comprising citric acid.

### Claim 11

An orodispersible pharmaceutical dosage form of desmopressin comprising:
desmopressin in a form selected from one or more of the free base of desmopressin and a pharmaceutically acceptable salt thereof, in an amount measured as the free base, selected from 25 μg and 50 μg, and
one or more carriers, wherein at least one carrier is gelatin in an open matrix network structure,
wherein the dosage form exhibits a desmopressin bioavailability of from 0.23% to 0.38%.

### Claim 12 (depends on 11)

The dosage form according to claim 11, wherein the gelatin is fish gelatin.

### Claim 13 (depends on 11)

The dosage form according to claim 11, wherein the gelatin is non-gelling fish gelatin.

### Claim 14 (depends on 11)

The dosage form according to claim 11, further comprising mannitol.

### Claim 15 (depends on 11)

The dosage form according to claim 11, further comprising citric acid.