Oral formulations of kappa opioid receptor agonists
AssigneeCara Therapeutics, Inc.
InventorsBryan R. Wilson, Stephen J. O'Connor
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AssigneeCara Therapeutics, Inc.
InventorsBryan R. Wilson, Stephen J. O'Connor
Estimating the term…
The invention provides formulations for oral delivery of a therapeutic agent wherein the formulation comprises a kappa opioid receptor agonist and an absorption enhancer, the absorption enhancer includes a medium chain fatty acid or a salt of a medium chain fatty acid; and a medium chain fatty acid glyceride. The kappa opioid receptor agonist may be embedded in an oligosaccharide, such as trehalose. Also provided are capsules containing the oral formulations of the kappa opioid receptor agonists and the absorption enhancer of the invention and methods use of these formulations for the prophylaxis and treatment of variety of kappa opioid receptor-associated diseases and conditions such as pain, pruritus and inflammation; the method comprising administering to the mammal the formulation comprising the kappa opioid receptor agonist and an absorption enhancer.
A formulation from about 18% (w/w) to about 23% (w/w) CR845.HCl (D-Phe-D-Phe-D-Leu-D-Lys[ω(4-aminopyperidine-4carboxylic acid)].HCl), from about 60% (w/w) to about 77% (w/w) trehalose and a glyceride of one or more medium chain fatty acids selected from the group consisting of caproic acid, caprylic acid and capric acid;
A formulation for oral delivery of a kappa opioid receptor agonist, comprising CR845.HCl (D-Phe-D-Phe-D-Leu-D-Lys-[ω(4-aminopyperidine-4carboxylic acid)].HCl) and a glyceride of one or more medium chain fatty acids selected from the group consisting of caproic, caprylic and capric acids, wherein the CR845.HCl (D-Phe-D-Phe-D-Leu-D-Lys-[ω(4-aminopyperidine-4carboxylic acid)].HCl) is embedded in trehalose and exhibits a stability of greater than about 96% stored for at least a year at 25° C.
Dependencies are inferred from the claim text.