Pharmaceutical formulations of desmopressin

• US 10,307,459 B2
• Filed: 01/26/2018
• Issued: 06/04/2019
• Est. Priority Date: 05/07/2002
• Status: Expired due to Term

• Current Assignee: Ferring BV (Ferring Holding SA)
• Original Assignee: Ferring BV (Ferring Holding SA)
• Inventors: Nilsson, Anders, Lindner, Hans, Wittendorff, Jorgen
• Primary Examiner(s): Russel, Jeffrey E.
• Application Number:
  US15/881,123
• Publication Number:
  US 20180280469A1
• Time in Patent Office: 494 Days
• CPC Class Codes: A61K 38/08 Peptides having 5 to 11 amino acids A61K38/043 - A61K38/046 take precedence
• CPC Class Codes: A61K 38/095 Oxytocins; Vasopressins; Related peptides
• CPC Class Codes: A61K 38/12 Cyclic peptides , e.g. bacitracins; Polymyxins; Gramicidins S, C; Tyrocidins A, B or C A61K38/043 - A61K38/046 take precedence
• CPC Class Codes: A61K 47/12 Carboxylic acids; Salts or anhydrides thereof
• CPC Class Codes: 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
• CPC Class Codes: 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
• CPC Class Codes: 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
• CPC Class Codes: A61K 9/2013 Organic compounds, e.g. phospholipids, fats
• CPC Class Codes: A61K 9/2018 Sugars, or sugar alcohols, e.g. lactose, mannitol; Derivatives thereof, e.g. polysorbates
• CPC Class Codes: A61K 9/2063 Proteins, e.g. gelatin
• CPC Class Codes: A61K 9/2095 Tabletting processes; Dosage units made by direct compression of powders or specially processed granules, by eliminating solvents, by melt-extrusion, by injection molding, by 3D printing mechanical aspects A61J3/00
• CPC Class Codes: A61P 1/12 Antidiarrhoeals
• CPC Class Codes: A61P 13/00 Drugs for disorders of the urinary system
• CPC Class Codes: A61P 13/02 of urine or of the urinary tract, e.g. urine acidifiers
• CPC Class Codes: A61P 13/10 of the bladder
• CPC Class Codes: A61P 3/10 for hyperglycaemia, e.g. antidiabetics
• CPC Class Codes: A61P 7/00 Drugs for disorders of the blood or the extracellular fluid
• CPC Class Codes: 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
• CPC Class Codes: A61P 7/10 Antioedematous agents; Diuretics
• CPC Class Codes: A61P 7/12 Antidiuretics, e.g. drugs for diabetes insipidus ADH A61P5/10

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

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 μ

g and 50 μ

g, 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.

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

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

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

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

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 μ

g and 50 μ

g, 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%.

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

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

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

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

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 μ

g and 50 μ

g, 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%.

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

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

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

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