Sustained-release composition containing peptides as active ingredient

Patent metadata

Field	Value
Publication number	US-9415012-B2
Application number	US-201214126365-A
Country	US
Kind code	B2
Filing date	Jun 13, 2012
Priority date	Jun 14, 2011
Publication date	Aug 16, 2016
Grant date	Aug 16, 2016

Abstract

The present invention relates to a sustained-release drug composition consisting essentially of microparticles of a peptide as the active substance and a biocompatible water-soluble polymer, in particular peptide as meianocortin receptor ligand. The present invention relates also to an injection formulation comprising the sustained-release drug composition suspended in an injection medium.

First claim

The invention claimed is:

1. A sustained-release drug composition comprising microparticles comprising:
a peptide of formula (I),
Ac-Arg-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-NH 2   (I),

or a pharmaceutically-acceptable salt thereof; and
a biocompatible water-soluble polymer;
wherein the peptide and the biocompatible water-soluble polymer are at least 90% by weight of the microparticles and the peptide is present at a concentration of from about 20% to about 70% by weight of the microparticles.

2. The composition of claim 1 , wherein the biocompatible water-soluble polymer is a biodegradable water-soluble polymer.

3. The composition of claim 1 , wherein the biocompatible water-soluble polymer is a polysaccharide.

4. The composition of claim 3 , wherein the polysaccharide has a molecular weight (Mw) lower than 2,000 kDa.

5. The composition of claim 3 , wherein the polysaccharide is hyaluronic acid or a salt thereof.

6. The composition of claim 5 , wherein the hyaluronic salt is sodium hyaluronate and the weight ratio of the peptide to sodium hyaluronate in the microparticles is from 3 to 0.25.

7. The composition of claim 1 , wherein the microparticles are spray-dried.

8. The composition of claim 1 , wherein the average size of the microparticles from 2 to 50 μm.

9. The composition of claim 1 , wherein the peptide is present at a concentration of from 25 to 60% by weight of the microparticles.

10. The composition of claim 1 , wherein the peptide is present at a concentration of from 30 to 50% by weight of the microparticles.

11. The composition of claim 4 , wherein the polysaccharide has a molecular weight (Mw) lower than 1,800 kDa.

12. The composition of claim 6 , wherein the hyaluronic salt is sodium hyaluronate and the weight ratio of peptide to sodium hyaluronate in the microparticles is from 1 to 0.33.

13. The composition of claim 8 , wherein the average size of the microparticles is from 5 to 30 μm.

14. An injectable formulation comprising the composition of claim 1 , wherein the composition is suspended in a liquid injectable vehicle used as a suspension medium.

15. The injectable formulation of claim 14 , wherein the injectable vehicle is a lipophilic suspension medium.

16. The injectable formulation of claim 14 , wherein the injectable vehicle comprises a dispersing agent.

17. The injectable formulation of claim 14 , wherein the injectable formulation provides a sustained release of the peptide for at least 3 hours.

18. The injectable formulation of claim 17 , wherein the formulation provides a sustained release of the peptide for at least 6 hours.

Assignees

• RICHARD JOëL
• Laredj Faïza
• Baronnet Marie-Madeleine
• Nourrisson Didier
• Harnett Jeremiah
• Hacher Béatrice
• Mondoly Nathalie
• Bertocchi Laurent
• Ipsen Pharma Sas

Inventors

• RICHARD JOëL
• Laredj Faïza
• Baronnet Marie-Madeleine
• Nourrisson Didier
• Harnett Jeremiah
• Hacher Béatrice
• Mondoly Nathalie
• Bertocchi Laurent

Classifications

• A61P5/06

  of the anterior pituitary hormones, e.g. TSH, ACTH, FSH, LH, PRL, GH · CPC title

• A61P43/00

  Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00 · CPC title

• A61P7/00

  Drugs for disorders of the blood or the extracellular fluid · CPC title

• A61P3/04

  Anorexiants; Antiobesity agents · CPC title

• A61K47/38

  Cellulose; Derivatives thereof · CPC title