Sustained-release composition containing peptides as active ingredient
View Patent ↗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.
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.