US 12,453,701 B2
Solid composition containing amorphous, poorly water-soluble material, and method for producing same
Tomohiro Nakao, Osaka (JP); and Yuki Imai, Osaka (JP)
Assigned to SAN-EI GEN F.F.I., INC., Osaka (JP)
Appl. No. 17/638,538
Filed by SAN-EI GEN F.F.I., INC., Toyonaka (JP)
PCT Filed Aug. 28, 2020, PCT No. PCT/JP2020/032765
§ 371(c)(1), (2) Date Feb. 25, 2022,
PCT Pub. No. WO2021/040027, PCT Pub. Date Mar. 4, 2021.
Claims priority of application No. 2019-159126 (JP), filed on Aug. 30, 2019; and application No. 2020-022821 (JP), filed on Feb. 13, 2020.
Prior Publication US 2023/0040337 A1, Feb. 9, 2023
Int. Cl. A61K 9/16 (2006.01); A23L 33/105 (2016.01); A61K 8/02 (2006.01); A61K 8/35 (2006.01); A61K 31/12 (2006.01)
CPC A61K 9/1652 (2013.01) [A23L 33/105 (2016.08); A61K 8/0245 (2013.01); A61K 8/35 (2013.01); A61K 9/1682 (2013.01); A61K 31/12 (2013.01)] 4 Claims
 
1. A method for producing a solid composition, comprising heating and kneading:
a crystalline curcumin (1b);
a hydroxypropylmethyl cellulose (2); and
one or more polysaccharides (3) selected from the group consisting of gum arabic, hydroxypropyl cellulose, ghatti gum, processed starch, locust bean gum, guar gum, alginic acid or a salt thereof, carrageenan, pectin, xanthan gum, pullulan, microcrystalline cellulose, fermented cellulose, methyl cellulose, carboxymethyl cellulose, dextrin, cyclodextrin, soybean polysaccharide, agar, tamarind seed gum, guar gum decomposition product, karaya gum, tara gum, welan gum, and gellan gum,
without using as a component any surfactant other than the components (1b), (2), and (3),
by using a kneader,
wherein the solid composition comprises:
an amorphous curcumin (1a);
the hydroxypropylmethyl cellulose (2); and
the polysaccharide (3) that is one or more types selected from the group consisting of gum arabic, hydroxypropyl cellulose, ghatti gum, processed starch, locust bean gum, guar gum, alginic acid or a salt thereof, carrageenan, pectin, xanthan gum, pullulan, microcrystalline cellulose, fermented cellulose, methyl cellulose, carboxymethyl cellulose, dextrin, cyclodextrin, soybean polysaccharide, agar, tamarind seed gum, guar gum decomposition product, karaya gum, tara gum, welan gum, and gellan gum,
wherein an XRD analysis value of the solid composition is 4.0% or less,
provided that the XRD analysis value is a numerical value calculated according to the formula: {(S2)/((S1)+(S2))}×100 (%) when an area of a halo peak in the range of 20=5 to 60° is represented by (S1) and an area of a sharp peak derived from a poorly water-soluble material in a crystalline state (1b) in a portion exceeding the halo peak is represented by (S2) in a chart obtained when the solid composition is analyzed with a powder X-ray diffractometer.