US 11,938,130 B2
Stable pharmaceutical composition for oral administration
Masakazu Miyazaki, Tokyo (JP); Ryohei Ishiba, Tokyo (JP); Yuki Takaishi, Tokyo (JP); and Fumiaki Uejo, Tokyo (JP)
Assigned to ASTELLAS PHARMA INC., Tokyo (JP)
Filed by ASTELLAS PHARMA INC., Tokyo (JP)
Filed on May 12, 2023, as Appl. No. 18/316,357.
Application 18/316,357 is a continuation of application No. 18/085,842, filed on Dec. 21, 2022.
Application 18/085,842 is a continuation of application No. 17/000,763, filed on Aug. 24, 2020, abandoned.
Application 17/000,763 is a continuation of application No. 15/741,377, granted, now 10,786,500, issued on Sep. 29, 2020, previously published as PCT/JP2016/069615, filed on Jul. 1, 2016.
Claims priority of application No. 2015-134817 (JP), filed on Jul. 3, 2015.
Prior Publication US 2023/0301992 A1, Sep. 28, 2023
This patent is subject to a terminal disclaimer.
Int. Cl. A61K 31/497 (2006.01); A61K 9/20 (2006.01); A61K 47/10 (2017.01); A61K 47/26 (2006.01)
CPC A61K 31/497 (2013.01) [A61K 9/20 (2013.01); A61K 9/2095 (2013.01); A61K 47/10 (2013.01); A61K 47/26 (2013.01)] 7 Claims
 
1. A pharmaceutical composition for oral administration comprising:
6-ethyl-3-({3-methoxy-4-[4-(4-methylpiperazin-1-yl)piperidin-1-yl]phenyl}amino)-5-(tetrahydro-2H-pyran-4-ylamino)pyrazine-2-carboxamide hemifumarate and at least one pharmaceutical additive selected from the group consisting of lactose, D-mannitol, anhydrous dibasic calcium phosphate, talc, calcium stearate, magnesium stearate, microcrystalline cellulose, hydroxypropyl cellulose, hypromellose, corn starch, low-substituted hydroxypropyl cellulose, and croscarmellose sodium,
wherein a proportion of crystals of 6-ethyl-3-({3-methoxy-4-[4-(4-methylpiperazin-1-yl)piperidin-1-yl]phenyl}amino)-5-(tetrahydro-2H-pyran-4-ylamino)pyrazine-2-carboxamide hemifumarate is 62% or more with respect to a total amount of 6-ethyl-3-({3-methoxy-4-[4-(4-methylpiperazin-1-yl)piperidin-1-yl]phenyl}amino)-5-(tetrahydro-2H-pyran-4-ylamino)pyrazine-2-carboxamide hemifumarate in the pharmaceutical composition.