US 11,786,526 B2
Pharmaceutical composition comprising rosuvastatin and ezetimibe and a preparation method thereof
Alena Prokopova, Prague (CZ); Jaroslava Svobodova, Krenice (CZ); Ondrej Dammer, Hostivice (CZ); and Petr Mikes, Prague (CZ)
Assigned to SANOFI, Paris (FR)
Appl. No. 16/330,268
Filed by SANOFI, Paris (FR)
PCT Filed Aug. 31, 2017, PCT No. PCT/CZ2017/050037
§ 371(c)(1), (2) Date Mar. 4, 2019,
PCT Pub. No. WO2018/041282, PCT Pub. Date Mar. 8, 2018.
Claims priority of application No. PV 2016-539 (CZ), filed on Sep. 5, 2016.
Prior Publication US 2020/0009136 A1, Jan. 9, 2020
Int. Cl. A61K 31/505 (2006.01); A61K 9/20 (2006.01); A61K 9/24 (2006.01); A61K 9/28 (2006.01); A61K 31/397 (2006.01)
CPC A61K 31/505 (2013.01) [A61K 9/209 (2013.01); A61K 9/2018 (2013.01); A61K 9/2813 (2013.01); A61K 31/397 (2013.01)] 15 Claims
OG exemplary drawing
 
1. A two-layer oral tablet comprising:
(a) rosuvastatin or its pharmaceutically acceptable salts, esters, hydrates or solvates;
(b) ezetimibe or its pharmaceutically acceptable salts, esters, hydrates or solvates;
wherein the tablet comprises one ezetimibe layer and one rosuvastatin layer;
wherein said ezetimibe layer comprises a granulate and an extragranulate phase;
wherein the granulate comprises ezetimibe or its pharmaceutically acceptable salts, esters, hydrates or solvates;
wherein the extragranulate phase comprises stearic acid or its acceptable salts as a glidant at a concentration of 0.15 to 0.5% by weight, including the limit values, relative to the weight of the ezetimibe layer, and at least one further pharmaceutically acceptable excipient comprising a filler, a binder, or a disintegrant; and
wherein said rosuvastatin layer consists of rosuvastatin or its pharmaceutically acceptable salt, ester, hydrate or solvate, and at least one pharmaceutically acceptable excipient, wherein said pharmaceutically acceptable excipient(s) are non-basic, and
wherein the rosuvastatin layer does not contain a basic excipient.