	US 12,290,601 B2
	Pharmaceutical composition comprising axitinib
Manuel Gago Guillan, Sant Boi de Llobregat (ES); Rohit Kumar, Sant Boi de Llobregat (ES); and Lisardo Alvarez Fernandez, Sant Boi de Llobregat (ES)
Assigned to Synthon B.V., Nijmegen (NL)
Appl. No. 17/609,545
Filed by Synthon B.V., Nijmegen (NL)
PCT Filed May 8, 2020, PCT No. PCT/EP2020/062840 § 371(c)(1), (2) Date Nov. 8, 2021, PCT Pub. No. WO2020/225413, PCT Pub. Date Nov. 12, 2020.
Claims priority of application No. 19173671 (EP), filed on May 9, 2019.
Prior Publication US 2022/0226246 A1, Jul. 21, 2022
Int. Cl. A61K 9/20 (2006.01); A61K 9/28 (2006.01); A61K 31/4439 (2006.01); A61P 35/00 (2006.01)

CPC A61K 9/20 (2013.01) [A61K 9/2009 (2013.01); A61K 9/2018 (2013.01); A61K 9/2027 (2013.01); A61K 9/2054 (2013.01); A61K 9/2059 (2013.01); A61K 9/28 (2013.01); A61K 31/4439 (2013.01); A61P 35/00 (2018.01)]

8 Claims

1. An immediate release tablet composition comprising axitinib form IV characterized by an XRPD pattern comprising the peaks at about 8.9, 12.0, 14.6, 15.2, 15.7, 17.8, 19.1, 20.6, 21.6, 23.2, 24.2, 24.9, 26.1 and 27.5±0.1 degrees 2θ, when measured with Cu Kα1 radiation and one or more pharmaceutically acceptable excipients, said tablet comprises an intragranular phase and an extragranular phase, wherein said intragranular phase consists essentially of:

0.5-5% axitinib Form IV

25-35% w/w of lactose, and

20-30% w/w of microcrystalline cellulose; and

said extragranular phase comprises:

30-50% w/w of one or more binders,

0.1-10% w/w of one or more disintegrants, and

0.1-10% w/w of one or more lubricants,

all relative to the total tablet weight without coating; and

wherein the composition exhibits a dissolution rate between 40% and 70% in 30 minutes when tested in 900 ml 0.01 N hydrochloric acid pH 2.0 at 37° C., 75 rpm in a USP apparatus II.