PHARMACEUTICAL FORMULATIONS

• US 20160175246A1
• Filed: 11/20/2015
• Published: 06/23/2016
• Est. Priority Date: 05/07/2002
• Status: Active Grant

• Current Assignee: Ferring BV (Ferring Holding SA)
• Original Assignee: Ferring BV (Ferring Holding SA)
• Inventors: NILSSON, Anders, LINDNER, Hans, WITTENDORFF, Jrgen
• Granted Patent: US 9,504,647 B2
• Time in Patent Office: Days
• 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

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 noctural enuresis (PNE), nocturia or central diabetes insipidus. Peptides other than desmopressin can also be formulated in this way.

Claims

1-27. -27. (canceled)

28. A solid orodispersible pharmaceutical dosage form of desmopressin acetate, comprising desmopressin acetate in an open matrix network carrying the desmopressin acetate, wherein the open matrix network comprises a water-soluble or water-dispersible carrier material inert to the desmopressin acetate that comprises gelatin, and wherein the dosage form disintegrates in the mouth within 10 seconds.

29. The dosage form of claim 28, wherein the gelatin comprises fish gelatin.

30. The dosage form of claim 28, wherein the gelatin comprises non-gelling fish gelatin.

31. The dosage form of claim 28, obtained by a process comprising sublimation of solvent from a composition comprising desmopressin acetate and a solution of the gelatin carrier material in a solvent.

32. The dosage form of claim 31, wherein the sublimation is carried out by freeze-drying the composition comprising desmopressin acetate and a solution of the gelatin carrier material in a solvent.

33. The dosage form of claim 31, wherein the composition is subject to sublimation in a mold.

34. The dosage form of claim 31, wherein the solvent is water.

35. The dosage form of claim 31, wherein the solution has a pH of from 3 to 6.

36. A blister pack comprising a solid orodispersible pharmaceutical dosage form of claim 28.

44. A method of administering desmopressin acetate to a subject in need thereof, comprising administering the solid orodispersible pharmaceutical dosage form of claim 28 to the subject.

45. The method of claim 44, wherein the subject is in need of voiding postponement and/or the treatment of incontinence, primary nocturnal enuresis (PNE), nocturia, and/or central diabetes insipidus.

37. A process for preparing a solid orodispersible pharmaceutical dosage form of desmopressin acetate which disintegrates in the mouth within 10 seconds, comprising sublimating solvent from a composition comprising desmopressin acetate and a solution of a water-soluble or water-dispersible carrier material inert to the desmopressin acetate that comprises gelatin in a solvent.

39. The dosage form of claim 37, wherein the gelatin comprises non-gelling fish gelatin.

40. The process of claim 37, wherein the subliming is carried out by freeze-drying a composition comprising desmopressin acetate and a solution of the gelatin carrier material in a solvent.

41. The process of claim 37, wherein the composition is subject to the subliming in a mold.

42. The process of claim 37, wherein the solvent is water.

43. The process of claim 37, wherein the pH of the solution is from 3 to 6.

38. The process of clam 37, wherein the gelatin comprises fish gelatin.