US 12,076,373 B2
Formulations for oral administration of active agents
Gregory Burshtein, Modiin (IL); Ariel Rothner, Jerusalem (IL); Phillip M. Schwartz, Jerusalem (IL); and Hillel Galitzer, Yad Binyamin (IL)
Assigned to Entera Bio Ltd., Jerusalem (IL)
Filed by Entera Bio Ltd., Jerusalem (IL)
Filed on Dec. 23, 2019, as Appl. No. 16/724,400.
Application 16/724,400 is a continuation of application No. 15/549,436, granted, now 10,583,177, previously published as PCT/IL2016/050155, filed on Feb. 9, 2016.
Claims priority of provisional application 62/113,638, filed on Feb. 9, 2015.
Claims priority of provisional application 62/113,625, filed on Feb. 9, 2015.
Claims priority of provisional application 62/113,604, filed on Feb. 9, 2015.
Claims priority of provisional application 62/113,600, filed on Feb. 9, 2015.
Claims priority of provisional application 62/113,673, filed on Feb. 9, 2015.
Claims priority of provisional application 62/113,619, filed on Feb. 9, 2015.
Claims priority of provisional application 62/113,629, filed on Feb. 9, 2015.
Prior Publication US 2020/0138913 A1, May 7, 2020
This patent is subject to a terminal disclaimer.
Int. Cl. A61K 38/29 (2006.01); A61K 9/00 (2006.01); A61K 9/20 (2006.01); A61K 9/28 (2006.01); A61K 31/05 (2006.01); A61K 31/166 (2006.01); A61K 31/19 (2006.01); A61K 31/195 (2006.01); A61K 31/20 (2006.01); A61K 38/22 (2006.01); A61K 38/55 (2006.01); A61K 47/12 (2006.01); A61P 5/18 (2006.01); A61P 19/10 (2006.01); A61K 45/06 (2006.01)
CPC A61K 38/29 (2013.01) [A61K 9/0053 (2013.01); A61K 9/20 (2013.01); A61K 9/2009 (2013.01); A61K 9/2013 (2013.01); A61K 9/2054 (2013.01); A61K 9/2086 (2013.01); A61K 9/28 (2013.01); A61K 9/2886 (2013.01); A61K 31/05 (2013.01); A61K 31/166 (2013.01); A61K 31/19 (2013.01); A61K 31/20 (2013.01); A61K 38/22 (2013.01); A61K 38/55 (2013.01); A61K 47/12 (2013.01); A61P 5/18 (2018.01); A61P 19/10 (2018.01); A61K 45/06 (2013.01); A61K 2300/00 (2013.01)] 18 Claims
OG exemplary drawing
 
1. A pharmaceutical composition for oral administration of a therapeutic active agent, the composition comprising a therapeutically active agent, SNAC (sodium 8-N-(2-hydroxybenzoyl)aminocaprylate), and at least one antacid compound in a total amount of at least 0.002 molar equivalent of base, wherein said at least one antacid compound is selected from the group consisting of sodium carbonate, sodium bicarbonate, sodium gluconate, sodium citrate, sodium hydroxide, potassium carbonate, potassium bicarbonate, potassium gluconate, potassium citrate, potassium hydroxide, magnesium carbonate, magnesium gluconate, magnesium citrate, magnesium hydroxide, magnesium oxide, aluminum carbonate, aluminum gluconate, aluminum citrate, and aluminum hydroxide,
the pharmaceutical composition being formulated as a solid unit dosage form which is soluble in gastric fluid.
 
12. A pharmaceutical composition unit dosage form for oral administration of a therapeutically active agent, the unit dosage form comprising:
a core comprising the therapeutically active agent and SNAC (sodium 8-N-(2-hydroxybenzoyl)aminocaprylate); and
an external layer comprising at least one protective agent selected from the group consisting of an antacid compound in a total amount of at least 0.002 molar equivalent of base and a protease inhibitor,
wherein said at least one antacid compound is selected from the group consisting of sodium carbonate, sodium bicarbonate, sodium gluconate, sodium citrate, sodium hydroxide, potassium carbonate, potassium bicarbonate, potassium gluconate, potassium citrate, potassium hydroxide, magnesium carbonate, magnesium gluconate, magnesium citrate, magnesium hydroxide, magnesium oxide, aluminum carbonate, aluminum gluconate, aluminum citrate, and aluminum hydroxide,
wherein the unit dosage form does not comprise an enteric coating.