US 12,083,227 B2
Solid pharmaceutical formulations for treating endometriosis, uterine fibroids, polycystic ovary syndrome or adenomyosis
Yihong Qiu, North Chicago, IL (US); Yuchuan Gong, North Chicago, IL (US); Alexander Ruggles, Lake Forest, IL (US); Jared A. Baird, Grayslake, IL (US); Hui Zu, North Chicago, IL (US); Gregory A. McClelland, San Diego, CA (US); and Anna V. Stepanenko, Del Mar, CA (US)
Assigned to AbbVie Inc., North Chicago, IL (US); and Neurocrine Biosciences, Inc., San Diego, CA (US)
Filed by AbbVie Inc., North Chicago, IL (US); and Neurocrine Biosciences, Inc., San Diego, CA (US)
Filed on Aug. 20, 2018, as Appl. No. 16/105,440.
Claims priority of provisional application 62/547,410, filed on Aug. 18, 2017.
Claims priority of provisional application 62/660,104, filed on Apr. 19, 2018.
Prior Publication US 2019/0054027 A1, Feb. 21, 2019
This patent is subject to a terminal disclaimer.
Int. Cl. A61K 9/20 (2006.01); A61K 31/513 (2006.01); A61P 15/00 (2006.01)
CPC A61K 9/2031 (2013.01) [A61K 9/2009 (2013.01); A61K 9/2013 (2013.01); A61K 9/2027 (2013.01); A61K 31/513 (2013.01); A61P 15/00 (2018.01)] 46 Claims
 
1. A high drug load, stable tablet comprising sodium 4-((R)-2-[5-(2-fluoro-3-methoxy-phenyl)-3-(2-fluoro-6-trifluoromethyl-benzyl)-4-methyl-2,6-dioxo-3,6-dihydro-2H-pyrimidin-1-yl]-1-phenyl-ethylamino)butanoate (“elagolix sodium”);
wherein the high drug load, stable tablet comprises from about 50% to about 90% of elagolix sodium by weight of the tablet and from about 0.1% to about 20% of a pharmaceutically acceptable meltable binder by weight of the tablet, wherein about 310 mg elagolix sodium is present in the tablet and wherein the pharmaceutically acceptable meltable binder is selected from the group consisting of a polyethylene glycol (PEG), a cellulose derivative, a poloxamer, and combinations thereof; and
wherein the high drug load, stable tablet controls degradation of elagolix sodium to within pharmaceutically acceptable levels for at least 1 month when said tablet is stored at 40° C./75% relative humidity.