Compositions for enhanced epithelial permeation of y2 receptor-binding peptides

Abstract

Pharmaceutical compositions comprising a PYY peptide, a cyclodextrin, and a compound selected from phosphatidylcholine or diglyceride, wherein the cyclodextrin and the compound selected from phosphatidylcholine or diglyceride are present in an amount sufficient to enhance epithelial permeation.

1 . A pharmaceutical composition comprising a PYY peptide, a cyclodextrin, and a compound selected from phosphatidylcholine or diglyceride, wherein the cyclodextrin and the compound selected from phosphatidylcholine or diglyceride are present in an amount sufficient to enhance epithelial permeation.  
   
   
       2 . The pharmaceutical composition of  claim 1 , wherein the PYY peptide is PYY (3-36).  
   
   
       3 . The pharmaceutical composition of  claim 1 , wherein the phosphatidylcholine is L-α-phosphatidylcholine didecanoyl (DDPC).  
   
   
       4 . The pharmaceutical composition of  claim 1 , wherein the cyclodextrin is selected from the group consisting of hydroxypropyl-α-cyclodextrin, sulfobutylether-β-cyclodextrin, and methyl-β-cyclodextrin.  
   
   
       5 . The pharmaceutical composition of  claim 1 , wherein the cyclodextrin is methyl-β-cyclodextrin.  
   
   
       6 . The pharmaceutical composition of  claim 1 , wherein the composition is an aqueous composition having a pH of from about 3 to about 6.  
   
   
       7 . The pharmaceutical composition of  claim 13 , wherein the pH is 5.0±0.5.  
   
   
       8 . The pharmaceutical composition of  claim 1 , further comprising a polyol.  
   
   
       9 . The pharmaceutical composition of  claim 8 , wherein the polyol is selected from the group consisting of sucrose, mannitol, sorbitol, lactose, L-arabinose, D-erythrose, D-ribose, D-xylose, D-mannose, trehalose, D-galactose, lactulose, cellobiose, gentibiose, glycerin and polyethylene glycol.  
   
   
       10 . The pharmaceutical composition of  claim 8 , wherein the polyol is sorbitol.  
   
   
       11 . The pharmaceutical composition of  claim 8 , further comprising a chelating agent.  
   
   
       12 . The pharmaceutical composition of  claim 11 , wherein the chelating agent is ethylene diamine tetraacetic acid (EDTA) or ethylene glycol tetraacetic acid (EGTA).  
   
   
       13 . The pharmaceutical composition of  claim 11 , wherein the chelating agent is ethylene diamine tetraacetic acid (EDTA).