US 11,684,674 B2
Oral formulations of kappa opioid receptor agonists
Bryan R. Wilson, Brewster, NY (US); and Stephen J. O'Connor, Guilford, CT (US)
Assigned to Cara Therapeutics, Inc., Stamford, CT (US)
Filed by Cara Therapeutics, Inc., Stamford, CT (US)
Filed on Apr. 28, 2021, as Appl. No. 17/242,678.
Application 17/242,678 is a continuation of application No. 16/570,333, filed on Sep. 13, 2019, granted, now 11,033,629.
Claims priority of provisional application 62/731,802, filed on Sep. 14, 2018.
Prior Publication US 2021/0346505 A1, Nov. 11, 2021
This patent is subject to a terminal disclaimer.
Int. Cl. A61K 38/07 (2006.01); A61K 47/54 (2017.01); A61K 31/40 (2006.01); A61K 31/485 (2006.01); A61K 47/14 (2017.01); A61K 9/48 (2006.01); A61K 47/18 (2017.01); A61K 9/107 (2006.01); A61K 38/08 (2019.01); A61K 47/64 (2017.01); A61K 47/26 (2006.01)
CPC A61K 47/545 (2017.08) [A61K 9/107 (2013.01); A61K 9/4891 (2013.01); A61K 31/40 (2013.01); A61K 31/485 (2013.01); A61K 38/07 (2013.01); A61K 38/08 (2013.01); A61K 47/14 (2013.01); A61K 47/183 (2013.01); A61K 47/186 (2013.01); A61K 47/26 (2013.01); A61K 47/64 (2017.08)] 20 Claims
 
1. 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; wherein the CR845.HCl exhibits a bioavailability of greater than 10%.