FORMULATIONS COMPRISING POLYETHYLENE GLYCOL

• US 20130225692A1
• Filed: 11/04/2011
• Published: 08/29/2013
• Est. Priority Date: 11/04/2010
• Status: Abandoned Application

• Current Assignee: Norgine B.V.
• Original Assignee: Jorg Plessl
• Inventors: Stein, Peter, Jones, Leighton, Smith, Samuel, Cox, Ian, Plessl, Jrg
• Application Number:
  US13/883,153
• Publication Number:
  US 20130225692A1
• Time in Patent Office: Days
• US Class Current: 514/723
• CPC Class Codes: A61K 31/08 acyclic, e.g. paraformaldehyde
• CPC Class Codes: A61K 31/77 of oxiranes
• CPC Class Codes: A61K 47/10 Alcohols; Phenols; Salts thereof, e.g. glycerol; Polyethylene glycols [PEG]; Poloxamers; PEG/POE alkyl ethers
• 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 47/36 Polysaccharides; Derivatives thereof, e.g. gums, starch, alginate, dextrin, hyaluronic acid, chitosan, inulin, agar or pectin
• CPC Class Codes: A61K 9/0053 Mouth and digestive tract, i.e. intraoral and peroral administration rectal administration A61K9/0031
• 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 9/2018 Sugars, or sugar alcohols, e.g. lactose, mannitol; Derivatives thereof, e.g. polysorbates
• CPC Class Codes: A61K 9/2031 obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyethylene glycol, polyethylene oxide, poloxamers
• CPC Class Codes: A61P 1/00 Drugs for disorders of the alimentary tract or the digestive system
• CPC Class Codes: A61P 1/10 Laxatives

Abstract

The present invention concerns a solid formulation for oral administration as a solid comprising polyethylene glycol and a further solid such as mannitol. The formulation may be used to prevent gastrointestinal disorders such as constipation in healthy subjects. In some embodiments, the solid formulation is chewable or suckable.

Claims

1. A solid formulation for oral administration as a solid, comprising:

(a) 50-90% w/w polyethylene glycol (PEG) having an average molecular weight within the range 2,000 to 10,000 Da; and

(b) 10-40% w/w of a solid.

2. A solid formulation of claim 1 wherein the solid of component (b) is sorbitol, lactose, dextrates, cellulose, xylitol, maltitol, mannitol.

3. A solid formulation of claim 2 wherein the group further comprises lactose and starch (e.g. a compound comprising lactose monohydrate and maize starch such as Starlac®

).

4. A solid formulation of claim 1 wherein the solid of component (b) is selected from sorbitol, lactose, lactose and starch (e.g. a compound comprising lactose monohydrate and maize starch such as Starlac®

), dextrates, cellulose, xylitol, maltitol and mannitol.

5. A solid formulation of claim 1 comprising 82 to 84% w/w PEG.

6. A solid formulation of claim 1 comprising 10 to 20% w/w of solid of component (b).

7. A solid formulation of claim 1 wherein the solid of component (b) is mannitol, (for example granular mannitol), xylitol, lactose and starch, or sorbitol.

8. A solid formulation of claim 7 wherein the solid of component (b) is mannitol, for example granular mannitol.

9. A solid formulation of claim 1 wherein the PEG has an average molecular weight of between 3,000 and 4,100 Da.

11. A solid formulation of claim 1, comprising:

(a) 70-90% w/w polyethylene glycol (PEG) having an average molecular weight within the range 2,000 to 10,000 Da;

(b) 10-20% w/w of the solid such as mannitol;

(c) 0-2.0% w/w lubricant; and

(d) 0-2.0% w/w flavouring.

12. A solid formulation of claim 1, comprising PEG and mannitol in a weight ratio of PEG:

mannitol=3;

1 to 9;

1.

13. A solid formulation of claim 1 comprising a lubricant in an amount of 2.0% w/w or less, for example 0.2 to 0.8% w/w, for example 0.5% w/w.

14. A solid formulation as claimed in claim 13 wherein the lubricant is magnesium stearate.

15. A solid formulation of claim 1 comprising a flavouring.

17. A solid formulation of claim 1 that is substantially free from electrolytes (e.g. sodium chloride, potassium chloride, bicarbonates such as sodium bicarbonate, sulphates such as sodium sulphate, or phosphates).

18. A solid formulation of claim 1 that has a mass of 0.5 to 10 g, for example 1.0 to 5.0 g.

19. A solid formulation as claimed in claim 18 that has a mass of 2.0 to 3.5 g and comprises:

(a) 1.00-3.15 g polyethylene glycol (PEG) having an average molecular weight within the range 2,000 to 10,000;

(b) 0.20-1.40 g mannitol.

20. A solid formulation as claimed in claim 1 that comprises;

(a) 2273 to 2284 mg polyethylene glycol (PEG) having an average molecular weight within the range 3,000 to 4,000 Da;

(b) 420 to 446 mg of solid such as mannitol;

(c) 13.5 to 13.75 mg magnesium stearate; and

(d) 11 to 42 mg flavour, such as peppermint or raspberry/lemon flavouring.

22. A method of therapeutically or non-therapeutically preventing gastrointestinal disorders or maintaining gastrointestinal health, by for example preventing dehydration of the stool, softening the stool for ease of defaecation, preventing constipation and allowing regular gastrointestinal transit, in a subject (e.g. human) comprising administering a solid formulation as claimed in claim 1 to the subject.

23. The method of claim 22 wherein the subject is healthy (that is has normal bowel movement).

25. A method as claimed in claim 22 wherein the subject (e.g. human) consumes a sufficient amount of formulation to receive up to 6 g (or thereabout) per day of PEG.

10. (canceled)

16. (canceled)

21. (canceled)

24. (canceled

26. (canceled)

27. A chewable or suckable solid formulation for oral administration as a solid comprising;

(a) 2.0 to 3.5 g PEG (for example 2.1 to 2.5 g) having an average molecular weight of 3000 to 4000 Da;

(b) 250 to 500 mg (for example 420 to 450 mg) of a solid such as mannitol;

(c) optional flavouring which if present is in an amount of 5 to 75 mg;

(d) optional lubricant such as magnesium stearate which if present is in an amount of 5 to 25 mg.

28. A method of preventing dehydration of the stool, softening the stool for ease of defecation, preventing constipation, allowing regular gastrointestinal transit comprising administering a solid formulation as claimed in claim 27.

29. (canceled)

30. A pack comprising a plurality of units of solid formulations comprising

(a) 50-90% w/w polyethylene glycol (PEG) having an average molecular weight within the range 2,000 to 10,000 Da;

and

(b) 10-40% w/w of a solid;

or

(a) 2.0 to 3.5 g PEG (for example 2.1 to 2.5 g) having an average molecular weight of 3000 to 4000 Da;

(b) 250 to 500 mg (for example 420 to 450 mg) of a solid such as mannitol;

(c) optional flavouring which if present is in an amount of 5 to 75 mg;

(d) optional lubricant such as magnesium stearate which if present is in an amount of 5 to 25 mg.

31-32. -32. (canceled)