US 12,239,737 B2
Oral rapamycin nanoparticle preparations and use
Dana Vaughn, Seguin, TX (US); and Neal K. Vail, Castle Hills, TX (US)
Assigned to Rapamycin Holdings, Inc., San Antonio, TX (US)
Filed by Rapamycin Holdings, Inc., San Antonio, TX (US)
Filed on Aug. 2, 2021, as Appl. No. 17/391,495.
Application 17/391,495 is a continuation of application No. 16/527,398, filed on Jul. 31, 2019, granted, now 11,077,061.
Application 16/527,398 is a continuation of application No. 15/109,278, granted, now 10,391,059, issued on Aug. 27, 2019, previously published as PCT/US2014/073097, filed on Dec. 31, 2014.
Claims priority of provisional application 62/040,000, filed on Aug. 21, 2014.
Claims priority of provisional application 61/980,095, filed on Apr. 16, 2014.
Claims priority of provisional application 61/922,800, filed on Dec. 31, 2013.
Prior Publication US 2021/0386672 A1, Dec. 16, 2021
This patent is subject to a terminal disclaimer.
Int. Cl. A61K 9/14 (2006.01); A61K 9/00 (2006.01); A61K 31/436 (2006.01)
CPC A61K 9/146 (2013.01) [A61K 9/0053 (2013.01); A61K 9/141 (2013.01); A61K 31/436 (2013.01)] 17 Claims
 
1. A particulate pharmaceutical preparation, comprising:
a) an enteric coating material, having characteristics such that it remains intact until it reaches the near-neutral to basic conditions of targeted portions of the alimentary canal of a mammalian subject, and then dissolves;
b) a solid excipient matrix; and
c) nanoparticles dispersed within said solid excipient matrix, said nanoparticles comprising:
1) a micelle-inducing compound, said micelle-inducing compound comprising an amphipathic compound; and
2) a pharmaceutically active core comprising rapamycin or an analog of rapamycin;
d) said micelle-inducing compound naturally inducing formation of micelles, said micelles having properties that promote stability of said rapamycin or said analog of rapamycin when said nanoparticles are dispersed within said solid excipient matrix.