Pharmaceutical formulations

• US 7,947,654 B2
• Filed: 06/18/2009
• Issued: 05/24/2011
• 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, Jørgen, Lindner, Hans
• Primary Examiner(s): Gupta; Anish
• Application Number:
  US12/487,116
• Publication Number:
  US 20090318665A1
• Time in Patent Office: 705 Days
• Field of Search: None
• US Class Current: 514/21.1
• 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. A solid orodispersible pharmaceutical dosage form comprising from 10 to 600 μ

g desmopressin acetate, measured as the free base, which solid orodispersible dosage form disintegrates in the mouth within 10 seconds.

2. The dosage form as claimed in claim 1, which is adapted for sublingual administration.

3. The dosage form as claimed in claim 1, wherein the dosage form is obtainable by subliming solvent from a composition comprising desmopressin acetate and a solution of carrier material in a solvent, the composition being in the solid state in a mold.

4. The dosage form as claimed in claim 3, wherein the sublimation is carried out by freeze drying a composition comprising desmopressin acetate and a solution of the carrier material in a solvent.

5. The dosage form as claimed in claim 1, which comprises an open matrix network carrying the desmopressin acetate, the open matrix network being comprised of a water-soluble or water-dispersable carrier material that is inert towards desmopressin.

6. The dosage form as claimed in claim 5, wherein the open matrix network comprises gelatin.

7. The dosage form as claimed in claim 6, wherein the gelatin is fish gelatin.

8. The dosage form as claimed in claim 7, wherein the fish gelatin is non-gelling.

9. A pack comprising an orodispersible solid pharmaceutical dosage form as defined in claim 1 together with instructions to place the dosage form in a patient'"'"'s mouth beneath the tongue (for sublingual administration).