Sustained Release Formulation of a Peptide

Abstract

This invention pertains to a sustained release complex, Compound (I), which comprises Compound (A), having the formula or a pharmaceutically acceptable salt thereof, and a copolymer comprising poly-(I)-lactic-glycolic-tartaric acid (P(I)LGT), wherein the amino group of said Compound (A) is ionically bound to a carboxyl group of the P(I)LGT. The present invention further pertains to a process for making said sustained release complex. Further still, the present invention is directed to a pharmaceutical composition comprising said sustained release complex and a pharmaceutically acceptable carrier(s).

1 - 8 . (canceled) 
     
     
         9 . A method of treating a disease or condition in a patient in need thereof, which comprises administering to said patient an effective amount of Compound (A), 
       
         
           
           
               
               
           
         
       
       or a pharmaceutically acceptable salt thereof, wherein the disease or condition is selected from the group consisting of systemic sclerosis, pancreatic pseudocysts, pancreatic ascites, VIPoma, nesidoblastosis, hyperinsulinism, gastrinoma, Zollinger-Ellison Syndrome, hypersecretory diarrhea, scleroderma, irritable bowel syndrome, upper gastrointestinal bleeding, postprandial portal venous hypertension, complications of portal hypertension, small bowel obstruction, duodenogastric reflux, Cushing's Syndrome, gonadotropinoma, hyperparathyroidism, diabetic neuropathy, hypercalcemia of malignancy, Paget's disease, meningioma, cancer cachexia, psoriasis, hypotension and panic attacks. 
     
     
         10 . A method of treating a disease or condition in a patient in need thereof, which comprises administering to said patient an effective amount of Compound (I), which comprises Compound (A) having the formula 
       
         
           
           
               
               
           
         
       
       and a polymer, wherein the polymer comprises lactide units, glycolide units and tartaric acid units where the ratio in the polymer of the lactide units is from and including about 71% to about 73%, of the glycolide units is from and including about 26% to about 28%; and of the tartaric acid units is from and including about 1% to about 3%; and where the amino group of Compound (A) is ionically bonded to a carboxylic group of the acid units of the polymer, and wherein the disease or condition is selected from the group consisting of systemic sclerosis, pancreatic pseudocysts, pancreatic ascites, VIPoma, nesidoblastosis, hyperinsulinism, gastrinoma, Zollinger-Ellison Syndrome, hypersecretory diarrhea, scleroderma, irritable bowel syndrome, upper gastrointestinal bleeding, postprandial portal venous hypertension, complications of portal hypertension, small bowel obstruction, duodenogastric reflux, Cushing's Syndrome, gonadotropinoma, hyperparathyroidism, diabetic neuropathy, hypercalcemia of malignancy, Paget's disease, meningioma, cancer cachexia, psoriasis, hypotension and panic attacks. 
     
     
         11 . A method of treating a disease or condition in a patient in need thereof, which comprises administering to said patient an effective amount of Compound (I), which comprises Compound (A) having the formula 
       
         
           
           
               
               
           
         
       
       and a polymer, wherein the polymer comprises lactide units, glycolide units and tartaric acid units where the ratio in the polymer of the lactide units is from and including about 71% to about 73%, of the glycolide units is from and including about 26% to about 28%; and of the tartaric acid units is from and including about 1% to about 3%; and where the amino group of Compound (A) is ionically bonded to a carboxylic group of the acid units of the polymer, and wherein the Compound (I) is in the form of microparticles, and  4 , wherein the disease or condition is selected from the group consisting of systemic sclerosis, pancreatic pseudocysts, pancreatic ascites, VIPoma, nesidoblastosis, hyperinsulinism, gastrinoma, Zollinger-Ellison Syndrome, hypersecretory diarrhea, scleroderma, irritable bowel syndrome, upper gastrointestinal bleeding, postprandial portal venous hypertension, complications of portal hypertension, small bowel obstruction, duodenogastric reflux, Cushing's Syndrome, gonadotropinoma, hyperparathyroidism, diabetic neuropathy, hypercalcemia of malignancy, Paget's disease, meningioma, cancer cachexia, psoriasis, hypotension and panic attacks.