Pharmaceutical formulations of desmopressin

• US 9,919,025 B2
• Filed: 10/25/2016
• Issued: 03/20/2018
• 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, Jrgen
• Primary Examiner(s): Russel, Jeffrey E.
• Application Number:
  US15/333,503
• Publication Number:
  US 20170112895A1
• Time in Patent Office: 511 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

Described herein are orodispersible pharmaceutical dosage forms of desmopressin comprising desmopressin free base or a pharmaceutically acceptable salt thereof, and one or more carriers, wherein at least one carrier is hydrolyzed gelatin in an open matrix network structure. Also described are methods of making and using such desmopressin orodispersible pharmaceutical dosage forms.

Claims

1. A method of treating a disease or condition selected from the group consisting of voiding postponement, incontinence, primary nocturnal enuresis (PNE), nocturia, and central diabetes insipidus, said method comprising administering to a subject an orodispersible pharmaceutical dosage form comprising desmopressin in a form selected from one or more of the free base of desmopressin and a pharmaceutically acceptable salt thereof;

and one or more carriers, wherein at least one carrier is hydrolyzed gelatin in an open matrix network structure, wherein the amount of desmopressin in the dosage form is selected from 25 μ

g and 50 μ

g, measured as the free base, and wherein the method achieves a maximum plasma concentration of desmopressin in about 0.5 to 2 hours after administration.

2. The method according to claim 1, wherein the disease or condition is primary nocturnal enuresis (PNE).

3. The method according to claim 1, wherein the disease or condition is nocturia.

4. The method according to claim 1, wherein the method results in a desmopressin bioavailability of from greater than 0.1% to 0.38%.

5. The method according to claim 1, wherein the method results in a desmopressin bioavailability of from 0.23% to 0.38%.

6. The method according to claim 1, wherein the method results in a desmopressin bioavailability of 0.30%.

7. A method of treating a disease or condition selected from the group consisting of voiding postponement, incontinence, primary nocturnal enuresis (PNE), nocturia, and central diabetes insipidus, said method comprising administering to a subject an orodispersible pharmaceutical dosage form comprising desmopressin in a form selected from one or more of the free base of desmopressin and a pharmaceutically acceptable salt thereof;

and one or more carriers, wherein at least one carrier is hydrolyzed gelatin in an open matrix network structure, wherein the amount of desmopressin in the dosage form is selected from 25 μ

g and 50 μ

g, measured as the free base, and wherein the method achieves a mean elimination half-life of desmopressin of about 2.8 to 3 hours after the maximum plasma concentration is reached.

8. The method according to claim 7, wherein the disease or condition is primary nocturnal enuresis (PNE).

9. The method according to claim 7, wherein the disease or condition is nocturia.

10. The method according to claim 7, wherein the method results in a desmopressin bioavailability of from greater than 0.1% to 0.38%.

11. The method according to claim 7, wherein the method results in a desmopressin bioavailability of from 0.23% to 0.38%.

12. A method of treating a disease or condition selected from the group consisting of voiding postponement, incontinence, primary nocturnal enuresis (PNE), nocturia, and central diabetes insipidus, said method comprising administering to a subject an orodispersible pharmaceutical dosage form comprising desmopressin in a form selected from one or more of the free base of desmopressin and a pharmaceutically acceptable salt thereof;

and one or more carriers, wherein at least one carrier is hydrolyzed gelatin in an open matrix network structure, wherein the amount of desmopressin in the dosage form is selected from 25 μ

g and 50 μ

g, measured as the free base, and wherein the method results in a desmopressin bioavailability of from greater than 0.1% to 0.38%.

13. The method according to claim 12, wherein the method achieves a maximum plasma concentration of desmopressin in 0.5 to 2 hours after administration.

14. The method according to claim 12, wherein the disease or condition is primary nocturnal enuresis (PNE).

15. The method according to claim 12, wherein the disease or condition is nocturia.

16. The method according to claim 12, wherein the method achieves a maximum plasma concentration of desmopressin in about 2.8 to 3 hours after administration.

17. A method of treating a disease or condition selected from the group consisting of voiding postponement, incontinence, primary nocturnal enuresis (PNE), nocturia, and central diabetes insipidus, said method comprising administering to a subject an orodispersible pharmaceutical dosage form comprising desmopressin in a form selected from one or more of the free base of desmopressin and a pharmaceutically acceptable salt thereof;

and one or more carriers, wherein at least one carrier is hydrolyzed gelatin in an open matrix network structure, wherein the amount of desmopressin in the dosage form is selected from 25 μ

g and 50 μ

g, measured as the free base, and wherein the method results in a desmopressin bioavailability of from 0.23% to 0.38%.

18. The method according to claim 17, wherein the disease or condition is primary nocturnal enuresis (PNE).

19. The method according to claim 17, wherein the disease or condition is nocturia.

20. The method according to claim 17, wherein the method achieves a maximum plasma concentration of desmopressin in 0.5 to 2 hours after administration.

21. The method according to claim 17, wherein the method achieves a maximum plasma concentration of desmopressin in about 2.8 to 3 hours after administration.