Sustained release formulation of a peptide
View Patent ↗This invention is directed to a sustained release composition comprised of Compound (A) having the formula or a pharmaceutically acceptable salt thereof, and a copolymer comprised of poly-(I)-lactic-glycolic-tartaric acid wherein the amino group of Compound (A) is ionically bound to a carboxyl group of the copolymer and wherein further the composition may be made into a sustained release pharmaceutical composition with pharmaceutically acceptable carrier(s).
1. A composition comprising a complex comprised of Compound (A) having the formula
and a polymer wherein the polymer comprises 71% to 73% lactide units, 26% to 28% glycolide units and 1% to 3% tartaric acid units and the amino group of Compound (A) is ionically bonded to a carboxylic group of the acid units of the polymer.
2. A composition according to claim 1 , wherein the polymer consists of 72% lactide units, 27% glycolide units and 1% tartaric acid units.
3. A composition according to claim 2 , wherein the percentage of Compound (A) in the composition is about 8% to about 12%.
4. A composition according to claim 1 , wherein said composition is in the form of microparticles.
5. Microparticles according to claim 4 , wherein the mean microparticle size is about 10 microns to about 100 microns.
6. Microparticles according to claim 5 , wherein the mean microparticle size is about 40 microns to about 70 microns.
7. Microparticles according to claim 6 , wherein said microparticles exhibit a zero-order release profile of Compound (A).
8. A pharmaceutical composition comprising microparticles of claim 4 and a pharmaceutically acceptable carrier, diluent or adjuvant.