US 12,409,145 B2
Granule, preparation containing the granule, production method of the granule, and production method of preparation containing the granule
Naoki Yoshihara, Osaka (JP); and Ryota Kimata, Osaka (JP)
Assigned to SAWAI PHARMACEUTICAL CO., LTD., Osaka (JP)
Filed by SAWAI PHARMACEUTICAL Co., Ltd., Osaka (JP)
Filed on Sep. 9, 2021, as Appl. No. 17/470,096.
Claims priority of provisional application 63/076,654, filed on Sep. 10, 2020.
Claims priority of application No. 2021-146436 (JP), filed on Sep. 8, 2021.
Prior Publication US 2022/0071913 A1, Mar. 10, 2022
Int. Cl. A61K 9/50 (2006.01); A61K 9/16 (2006.01); A61K 47/10 (2017.01); A61K 47/32 (2006.01)
CPC A61K 9/5073 (2013.01) [A61K 47/10 (2013.01); A61K 47/32 (2013.01)] 6 Claims
OG exemplary drawing
 
1. A granule comprising:
a core substance;
a melt component layer consisting of a first melt component, the melt component layer disposed on a surface of the core substance;
an active ingredient-containing layer containing a second melt component and an active ingredient, the active ingredient-containing layer disposed on a surface of the melt component layer;
a gelling substance-containing layer disposed on a surface where the second melt component and the active ingredient are disposed; and
a hydrophobic polymer-containing layer disposed on a surface of the gelling substance-containing layer,
wherein the core substance is composed of an adsorbent material selected from a group consisting of amberlite IRP-64, ion exchange resin, kaolin, calcium carmellose, hydrous silicon dioxide, magnesium silicate, light anhydrous silicic acid, light liquid paraffin, diatomaceous earth, synthetic aluminum silicate, aluminum oxide, aluminum hydroxide, absorbent cotton, magnesium carbonate, precipitated calcium carbonate, dextrin, silicon dioxide, composite aluminum silicate potassium grain, bentonite, polyethylene fiber, magnesium aluminate metasilicate, and medicinal charcoal,
the first melt component contained in the melt component layer is selected from a group consisting of glycerin monostearate, lauromacrogol, and stearic acid,
the second melt component in the active ingredient-containing layer is selected from a group consisting of stearic acid, glyceryl monostearate, carnauba wax, hydrogenated oil, lauromacrogol, palmitic acid, cetyl alcohol, aminoalkyl methacrylate copolymer E, ammonioalkyl methacrylate copolymer, dried methacrylic acid copolymer, hypromellose acetate succinate ester, polyvinylpyrrolidone, and polyvinyl acetal diethyl aminoacetate and, wherein the gelling substance-containing layer includes a gelling substance having a viscosity of 10 mPa/s or more in a 2% aqueous solution.