US 11,986,554 B2
Orally disintegrating compositions
Sheera Moses-Heller, Atlit (IL)
Assigned to DEXCEL PHARMA TECHNOLOGIES LTD., Jerusalem (IL)
Filed by DEXCEL PHARMA TECHNOLOGIES LTD., Jerusalem (IL)
Filed on Jul. 30, 2021, as Appl. No. 17/389,612.
Application 17/389,612 is a continuation of application No. 15/238,109, filed on Aug. 16, 2016, granted, now 11,077,055.
Application 15/238,109 is a continuation of application No. PCT/IL2016/050425, filed on Apr. 21, 2016.
Claims priority of provisional application 62/154,250, filed on Apr. 29, 2015.
Prior Publication US 2021/0353535 A1, Nov. 18, 2021
This patent is subject to a terminal disclaimer.
Int. Cl. A61K 31/4439 (2006.01); A61K 9/00 (2006.01); A61K 9/16 (2006.01); A61K 9/20 (2006.01); A61K 9/28 (2006.01); A61K 9/50 (2006.01); A61K 31/4184 (2006.01)
CPC A61K 9/0056 (2013.01) [A61K 9/1623 (2013.01); A61K 9/1676 (2013.01); A61K 9/2072 (2013.01); A61K 9/2081 (2013.01); A61K 9/2086 (2013.01); A61K 9/28 (2013.01); A61K 9/2886 (2013.01); A61K 9/5026 (2013.01); A61K 9/5042 (2013.01); A61K 9/5047 (2013.01); A61K 9/5078 (2013.01); A61K 31/4184 (2013.01); A61K 31/4439 (2013.01)] 13 Claims
 
1. An orally disintegrating tablet comprising (i) enteric coated active cores comprising about 2 mg to about 50 mg of a proton pump inhibitor selected from the group consisting of lansoprazole, omeprazole, pantoprazole, leminoprazole, perprazole, rabeprazole, and a pharmaceutically acceptable salt thereof; and (ii) at least one pharmaceutically acceptable excipient comprising a disintegrant comprising cross-linked polyvinylpyrrolidone, the enteric coated active cores comprising:
(a) inert seeds comprising sugar spheres;
(b) a drug coating layer over the inert seeds, wherein the drug coating layer comprises the proton pump inhibitor and mannitol, wherein the drug coating layer further comprises at least one alkalizing agent selected from the group consisting of arginine, lysine, meglumine, a stearic acid salt, sodium hydroxide, potassium hydroxide, calcium carbonate, magnesium carbonate, and zinc carbonate, in an amount of about 1% to about 5% by weight of the total composition;
(c) a subcoating layer over the drug coating layer, wherein the subcoating layer comprises hydroxypropyl methylcellulose; and
(d) a single enteric coating layer in an amount of about 10% to about 25% by weight of the total composition over the subcoating layer, wherein the enteric coating layer comprises hydroxypropyl methylcellulose phthalate and cetyl alcohol,
wherein the enteric coated active cores together with the at least one pharmaceutically acceptable excipient comprising a disintegrant are compressed into the form of a tablet,
wherein the tablet substantially disintegrates in the oral cavity of a subject in need thereof within less than about 60 seconds after administration and provides a delayed release profile of the proton pump inhibitor, and
wherein in vitro drug release in 15 minutes at 0.1N HCl and 40% ethanol is less than about 20%.