Pharmaceutical formulations

• US 20050232997A1
• Filed: 05/07/2003
• Published: 10/20/2005
• Est. Priority Date: 05/07/2002
• Status: Active Grant

• Current Assignee: Ferring BV (Ferring Holding SA)
• Original Assignee: Ferring BV (Ferring Holding SA)
• Inventors: Wittendorff, Jorgen, Nilsson, Andres, Lindner, Hans
• Granted Patent: US 7,560,429 B2
• Time in Patent Office: Days
• US Class Current: 424/484
• 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 by means of 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.

2. A dosage form as claimed in claim 1, which is an orodispersible solid pharmaceutical dosage form.

11. A dosage form as claimed in claim 1 for use in medicine.

12. A dosage form as claimed in claim 1 for use in voiding postponement, or the treatment or prevention of incontinence, primary nocturnal enuresis (PNE), nocturia or central diabetes insipidus.

3. A solid pharmaceutical dosage form comprising desmopressin and an open matrix network carrying the desmopressin, the open matrix network being comprised of a water-soluble or water-dispersible carrier material that is inert towards desmopressin.

4. A dosage form as claimed in claim 3, wherein the open matrix network comprises gelatin.

5. A dosage form as claimed in claim 4, wherein the gelatin is fish gelatin.

6. A dosage form as claimed in claim 5, wherein the fish gelatin is non-gelling.

7. A process for preparing a solid pharmaceutical dosage form comprising subliming solvent from a composition comprising desmopressin and a solution of carrier material in a solvent, the composition being in the solid state in a mould.

8. A process as claimed in claim 7, wherein the sublimation is carried out by freeze drying a composition comprising desmopressin and a solution of the carrier material in a solvent.

9. A process as claimed in claim 7, wherein the solvent is water.

10. A process as claimed in claim 7, wherein the pH of the solution is within the range of from 3 to 6, preferably from 3.5 to 5.5, and most preferably from 4 to 5.

13. The use of desmopressin in the manufacture of an orodispersible pharmaceutical dosage form.

14. A method of treating or preventing a disease or condition which is treatable or preventable by desmopressin, the method comprising administering in an orodispersible pharmaceutical dosage form an effective and generally non-toxic amount of desmopressin to a subject.

15. A method as claimed in claim 14, which is a method of postponing voiding, or treating or preventing incontinence, primary nocturnal enuresis (PNE), nocturia and/or central diabetes insipidus.

16. A pack comprising an orodispersible pharmaceutical dosage form of desmopressin together with instructions to place the dosage form in a patient'"'"'s mouth.

17. A method for preparing a packaged dosage form of desmopressin, the method comprising bringing into association an orodispersible pharmaceutical dosage form of desmopressin and instructions to place the dosage form in a patient'"'"'s mouth.

18. An orodispersible pharmaceutical dosage form of a pharmaceutically active peptide.

19. A dosage form as claimed in claim 18, which is an orodispersible solid pharmaceutical dosage form.

21. A dosage form as claimed in claim 18, wherein the peptide is somatostatin or an analogue thereof, an enkephalin, an oxytocin analogue, an LH-RH analogue, a GnRH analogues or a vasopressin analogue.

27. A dosage form as claimed in claim 18 for use in medicine

20. A solid pharmaceutical dosage form comprising a pharmaceutically active peptide and an open matrix network carrying the peptide, the open matrix network being comprised of a water-soluble or water-dispersible carrier material that is inert towards the peptide.

22. A dosage form as claimed in claim 20, wherein the open matrix network comprises gelatin.

23. A dosage form as claimed in claim 22, wherein the gelatin is fish gelatin.

24. A dosage form as claimed in claim 23, wherein the fish gelatin is non-gelling.

25. A process for preparing a solid pharmaceutical dosage form comprising a pharmaceutically active peptide, the process comprising subliming solvent from a composition comprising the peptide and a solution of carrier material in a solvent, the composition being in the solid state in a mould.

26. A process as claimed in claim 25, wherein the sublimation is carried out by freeze drying a composition comprising the peptide and a solution of the carrier material in a solvent.