Pharmaceutical compositions comprising polymeric binders with non-hydrolysable covalent bonds and their use in treating celiac disease

• US 8,784,792 B2
• Filed: 05/01/2012
• Issued: 07/22/2014
• Est. Priority Date: 11/14/2005
• Status: Expired due to Fees

• Current Assignee: Valorisation-Recherche, Limited Partnership
• Original Assignee: Valorisation HSJ
• Inventors: Leroux, Jean-Christophe, Nasser Eddine, Mohamad
• Primary Examiner(s): Hartley, Michael G
• Assistant Examiner(s): RIDER, LANCE W
• Application Number:
  US13/461,468
• Publication Number:
  US 20120244105A1
• Time in Patent Office: 812 Days
• US Class Current: 424/78.18
• CPC Class Codes: A21D 2/28 Organic sulfur compounds
• CPC Class Codes: A23L 33/25 Synthetic polymers, e.g. vinylic or acrylic polymers
• CPC Class Codes: A61K 31/74 Synthetic polymeric materials
• CPC Class Codes: A61K 31/795 Polymers containing sulfur
• CPC Class Codes: A61P 1/00 Drugs for disorders of the alimentary tract or the digestive system
• CPC Class Codes: A61P 1/02 Stomatological preparations, e.g. drugs for caries, aphtae, periodontitis
• CPC Class Codes: A61P 1/12 Antidiarrhoeals
• CPC Class Codes: A61P 19/08 for bone diseases, e.g. rachitism, Paget's disease
• CPC Class Codes: A61P 25/04 Centrally acting analgesics, e.g. opioids
• CPC Class Codes: A61P 3/00 Drugs for disorders of the metabolism of the blood or the extracellular fluid A61P7/00
• CPC Class Codes: A61P 37/00 Drugs for immunological or allergic disorders
• CPC Class Codes: A61P 37/02 Immunomodulators
• CPC Class Codes: A61P 37/06 Immunosuppressants, e.g. drugs for graft rejection

Abstract

A pharmaceutical composition comprising a polymeric binder including a high molecular weight synthetic polymer having a backbone constituted of non hydrolysable covalent bonds, said polymer being able to form electrostatic bonds at a pH lower than the isoelectric point of gluten and peptides derived from the degradation of gluten, and being able to bind to gluten or peptides derived from the degradation of gluten in the gastrointestinal tract, and a pharmaceutically acceptable carrier. Methods of using the polymeric binder for binding gluten or a peptide derived from the degradation of gluten, for decreasing the degradation of gluten into toxic peptides or for decreasing interaction of gluten or peptides derived from the degradation of gluten with the gastrointestinal mucosa.

Claims

1. A pharmaceutical composition comprising a pharmaceutically effective amount of a polymeric binder including a high molecular weight synthetic linear copolymer, said synthetic linear copolymer comprising a linear copolymer of hydroxyethyl methacrylate (HEMA) and 4-styrene sulfonic acid or a salt thereof, wherein said linear copolymer has a molar percentage ratio of HEMA:

4-styrene sulfonic acid or a salt thereof of from between about 82.4;

17.6 mol % to about 28;

72 mol %, and a pharmaceutically acceptable carrier, wherein the pharmaceutical composition is formulated for oral administration.

2. The pharmaceutical composition of claim 1, wherein said synthetic linear copolymer has a backbone constituted of non-hydrolysable covalent bonds.

3. The pharmaceutical composition of claim 1, wherein said synthetic linear copolymer is able to form electrostatic bonds at a pH lower than the isoelectric point of gluten and peptides derived from the degradation of gluten.

4. The pharmaceutical composition of claim 1, wherein said synthetic linear copolymer is able to form hydrophobic interactions with gluten or peptides derived from the degradation of gluten.

5. The pharmaceutical composition of claim 1, wherein said synthetic linear copolymer is able to form hydrogen bonds.

6. The pharmaceutical composition of claim 1, wherein said synthetic linear copolymer is able to specifically bind to gluten or peptides derived from the degradation of gluten in the gastrointestinal tract.

7. The pharmaceutical composition of claim 1, wherein said synthetic linear copolymer is able to bind to gluten or peptides derived from the degradation of gluten in the intestinal tract.

8. The pharmaceutical composition of claim 1, wherein said salt of 4-styrene sulfonic acid is 4-styrene sulfonic acid sodium salt (SStNa).

9. The pharmaceutical composition of claim 1, wherein said salt of 4-styrene sulfonic acid is 4-styrene sulfonic acid sodium salt hydrate (SStNa).

10. The pharmaceutical composition of claim 9, wherein said copolymer of HEMA and SStNa has a HEMA/SStNa molar percentage ratio of (51.5/48.5 mol %).

11. The pharmaceutical composition of claim 9, wherein said copolymer of HEMA and SStNa has a HEMA/SStNa molar percentage ratio of (43/57 mol %).

12. The pharmaceutical composition of claim 9, wherein said copolymer of HEMA and SStNa contains about 50% SStNa.