US 11,980,610 B2
Oral solid dosage form composition having improved disintegration and preparation method therefor
Sang Yeob Park, Daejeon (KR); Hye Jung Lim, Daejeon (KR); Jae Young Lee, Seongnam-si (KR); Min Hyo Seo, Yongin-si (KR); and Sa Won Lee, Seongnam-si (KR)
Assigned to SAMYANG HOLDINGS CORPORATION, Seoul (KR)
Appl. No. 16/760,302
Filed by SAMYANG HOLDINGS CORPORATION, Seoul (KR)
PCT Filed Oct. 30, 2018, PCT No. PCT/KR2018/013034
§ 371(c)(1), (2) Date Apr. 29, 2020,
PCT Pub. No. WO2019/088669, PCT Pub. Date May 9, 2019.
Claims priority of application No. 10-2017-0144139 (KR), filed on Oct. 31, 2017.
Prior Publication US 2020/0261426 A1, Aug. 20, 2020
Int. Cl. A61K 31/436 (2006.01); A61K 9/00 (2006.01); A61K 31/192 (2006.01); A61K 31/366 (2006.01); A61K 31/4025 (2006.01); A61K 31/415 (2006.01); A61K 31/4178 (2006.01); A61K 31/44 (2006.01); A61K 31/47 (2006.01); A61K 31/501 (2006.01); A61K 31/502 (2006.01); A61K 31/5025 (2006.01); A61K 31/506 (2006.01); A61K 47/32 (2006.01)
CPC A61K 31/436 (2013.01) [A61K 9/0053 (2013.01); A61K 31/192 (2013.01); A61K 31/366 (2013.01); A61K 31/4025 (2013.01); A61K 31/415 (2013.01); A61K 31/4178 (2013.01); A61K 31/44 (2013.01); A61K 31/47 (2013.01); A61K 31/501 (2013.01); A61K 31/502 (2013.01); A61K 31/5025 (2013.01); A61K 31/506 (2013.01); A61K 47/32 (2013.01)] 10 Claims
 
1. An oral solid formulation composition comprising
a mixture comprising an active ingredient and a water-soluble or gastric-soluble polymer as a solubilizing carrier, and a foaming component as a disintegration promoter,
wherein the foaming component comprises a foaming agent and does not comprise an acidifying agent;
the active ingredient is selected from the group consisting of sorafenib tosylate, lapatinib ditosylate, dasatinib anhydride, nilotinib hydrochloride monohydrate, cabozantinib malate, and ponatinib hydrochloride hydrate;
the water-soluble or gastric-soluble polymer is a mixture of hypromellose and Eudragit E in a weight ratio of 0.62-0.63:1;
the active ingredient is comprised in an amount of 35 to 45% by weight based on a total weight of the composition;
the water-soluble or gastric-soluble polymer is comprised in an amount of 23 to 28% by weight based on the total weight of the composition; and
the foaming agent is comprised in an amount of 25 to 35 parts by weight based on 100 parts by weight of the water-soluble or gastric-soluble polymer.