Methods using desmopressin acetate in orodispersible form

• US 9,220,747 B2
• Filed: 07/09/2014
• Issued: 12/29/2015
• 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, Wittendorff, Jrgen, Lindner, Hans
• Primary Examiner(s): Russel, Jeffrey E
• Application Number:
  US14/326,939
• Publication Number:
  US 20150150938A1
• Time in Patent Office: 538 Days
• Field of Search: None
• US Class Current: 1/1
• 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 are orodispersible solid dosage forms of desmopressin or a pharmaceutically acceptable salt thereof useful for treating diseases or conditions such as incontinence, primary nocturnal enuresis (PNE), nocturia, and central diabetes insipidus. The dosage forms disintegrate in the mouth within 10 seconds and provide good desmopressin bioavailability.

Claims

1. A method of treating a disease or condition selected from the group consisting of incontinence, primary nocturnal enuresis (PNE), nocturia, and central diabetes insipidus, comprising administering to a subject in need thereof an effective and generally non-toxic amount of desmopressin acetate in an orodispersible solid dosage form, wherein the dosage form (A) disintegrates in the mouth within 10 seconds and (B) comprises an amount of desmopressin acetate, measured as the free base, of from 0.5 μ

g to 75 μ

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

2. The method of claim 1, wherein the method results in a desmopressin bioavailability of about 0.23% to about 0.38%.

3. The method of claim 2, wherein the method results in a desmopressin bioavailability of about 0.30%.

4. The method of claim 1, wherein the dosage form comprises an amount of desmopressin acetate, measured as the free base, of from 1 μ

g to 50 μ

g.

5. The method of claim 1, wherein the dosage form further comprises an open matrix network carrying the desmopressin acetate, the open matrix network being comprised of a water-soluble or water-dispersible carrier material that is inert towards desmopressin.

6. The method of claim 5, wherein the open matrix network comprises gelatin.

7. The method of claim 6, wherein the gelatin is fish gelatin.

8. The method of claim 7, wherein the fish gelatin is non-gelling.

9. The method of claim 1, wherein the dosage form further comprises citric acid.

10. The method of claim 1, wherein the disease or condition is primary nocturnal enuresis (PNE).

11. The method of claim 1, wherein the disease or condition is nocturia.

12. The method of claim 1, wherein the dosage form disintegrates in the mouth within 5 seconds.

13. The method of claim 1, wherein the dosage form disintegrates in the mouth within 2 seconds.

14. The method of claim 1, wherein the dosage form is administered once per day.

15. The method of claim 1, wherein the dosage form is administered twice per day.

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

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

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