US 11,052,048 B2
Esomeprazole-containing complex capsule and preparation method therefor
Taek Kwan Kwon, Suwon-si (KR); Seung Hun Chang, Anyang-si (KR); Ho Taek Im, Yongin-si (KR); Yong Il Kim, Suwon-si (KR); Jae Hyun Park, Suwon-si (KR); and Jong Soo Woo, Seoul (KR)
Assigned to HANMI PHARM. CO., LTD., Hwaseong-si (KR)
Appl. No. 16/345,456
Filed by HANMI PHARM. CO., LTD., Hwaseong-si (KR)
PCT Filed Oct. 19, 2017, PCT No. PCT/KR2017/011571
§ 371(c)(1), (2) Date Apr. 26, 2019,
PCT Pub. No. WO2018/080104, PCT Pub. Date May 3, 2018.
Claims priority of application No. 10-2016-0142156 (KR), filed on Oct. 28, 2016.
Prior Publication US 2019/0247316 A1, Aug. 15, 2019
Int. Cl. A61K 9/48 (2006.01); A61P 1/04 (2006.01); A61K 31/4439 (2006.01); A61K 9/50 (2006.01)
CPC A61K 9/4808 (2013.01) [A61K 9/48 (2013.01); A61K 9/4825 (2013.01); A61K 9/4833 (2013.01); A61K 9/4891 (2013.01); A61K 9/50 (2013.01); A61K 31/4439 (2013.01); A61P 1/04 (2018.01)] 11 Claims
 
1. A composite capsule comprising:
a first dissolving part comprising a core comprising, as an active ingredient, esomeprazole or a pharmaceutically acceptable salt thereof, an inner coating layer on the core, and a first enteric coating layer on the inner coating layer; and
a second dissolving part comprising a core comprising, as an active ingredient, esomeprazole or a pharmaceutically acceptable salt thereof, an inner coating layer on the core, and a second enteric coating layer on the inner coating layer,
wherein the first enteric coating layer comprises, as a coating base material, methacrylic acid copolymer LD in an amount of about 5% (w/w) to about 50% (w/w) of the core on which the inner coating layer is formed,
the second enteric coating layer comprises, as a coating base material, a mixture containing methacrylic acid copolymer S and methacrylic acid copolymer L at a ratio of about 1.5:1 (w/w) to about 3.5:1 (w/w) in an amount of about 15% (w/w) to about 40% (w/w) of the core on which the inner coating layer is formed,
wherein the cores of the first dissolving part and the second dissolving part are all mini-tablets,
wherein the inner coating layer is on the core and is contained in an amount of about 3% (w/w) to about 5% (w/w) of the core on which the inner coating layer is formed, and
wherein, in an artificial intestinal fluid having a pH of 6.7 to 6.9 and a temperature of 37±0.5° C., the active ingredient of the first dissolving part releases into the artificial intestinal fluid before the active ingredient of the second dissolving part releases.