Method for producing solid dispersion containing hardly soluble polyphenol

Patent metadata

Field	Value
Publication number	US-10894058-B2
Application number	US-201515506939-A
Country	US
Kind code	B2
Filing date	Aug 19, 2015
Priority date	Aug 29, 2014
Publication date	Jan 19, 2021
Grant date	Jan 19, 2021

Abstract

Provided is a method of producing a solid dispersion that can improve solubility of a hardly soluble polyphenol in water. Specifically, provided is a method of producing a solid dispersion containing an amorphous hardly soluble polyphenol, the method including the steps of: mixing (A) a hardly soluble polyphenol, (B) at least one selected from the group consisting of a plant-derived polysaccharide, a seaweed-derived polysaccharide, and a microorganism-derived polysaccharide, a plant-derived polypeptide, and a microorganism-derived polypeptide, and (C) at least one selected from the group consisting of a monosaccharide and a disaccharide, followed by melting of the mixture by heating; and solidifying the molten product by cooling.

First claim

The invention claimed is:

1. A method of producing a solid dispersion containing an amorphous hardly soluble polyphenol, comprising the steps of:
mixing (A) a polyphenol having a solubility in water at 25° C. of 5 g/L or less, wherein said polyphenol is ellagic acid, (B) pectin, and (C) at least one selected from the group consisting of maltose, fructose, and glucose,
wherein the content of the component (A) in the mixture is from 5 mass % to 75 mass %, the content of the component (B) in the mixture is from 5 mass % to 80 mass %, and the content of the component (C) in the mixture is from 5 mass % to 85 mass %, and a mass ratio of the component (A) to a total of the component (B) and the component (C), [(A)/{(B)+(C)}], is from 0.17 to 0.47,
followed by
melting of the mixture by heating at a temperature of from 75° C. to 250° C.; and
solidifying the molten product by cooling to provide said solid dispersion.

2. The method of producing a solid dispersion according to claim 1 , wherein a mass ratio of the component (C) to the component (A), [(C)/(A)], in mixing of the component (A), the component (B), and the component (C) is from 0.2 to 19.

3. The method of producing a solid dispersion according to claim 1 , wherein a mass ratio of the component (C) to the component (B), [(C)/(B)], in mixing of the component (A), the component (B), and the component (C) is from 0.05 to 100.

4. The method of producing a solid dispersion according to claim 1 , wherein the step of mixing the component (A), the component (B), and the component (C), followed by melting of the mixture by heating, is carried out using an extruding machine including a screw.

5. The method of producing a solid dispersion according to claim 1 , wherein the component (B) pectin has an esterification rate of 50% or more.

Assignees

• Kao Corp

Inventors

• Umehara Masahiro
• Uda Akihiro
• Abe Tetsuya
• Yamada Yasushi

Classifications

• A61K8/73 Primary

  Polysaccharides · CPC title

• B01F23/811

  Heating the mixture · CPC title

• A61K9/146

  with organic macromolecular compounds · CPC title

• A61K8/498

  having 6-membered rings or their condensed derivatives, e.g. coumarin · CPC title

• A61K8/60

  Sugars; Derivatives thereof · CPC title