Hydroxyalkyl alkyl cellulose, method for producing the same, and solid preparation

Patent metadata

Field	Value
Publication number	US-10550202-B2
Application number	US-201715722636-A
Country	US
Kind code	B2
Filing date	Oct 2, 2017
Priority date	Oct 7, 2016
Publication date	Feb 4, 2020
Grant date	Feb 4, 2020

Abstract

There is provided is a hydroxyalkyl alkyl cellulose exhibiting good flowability and high compressibility. More specifically, provided are a hydroxyalkyl alkyl cellulose having a volume-based average particle diameter, determined by dry laser diffractometry, of 50 to 100 μm, and having, on a basis of a dynamic image analysis to divide all particles into fine particles, spherical particles and fibrous particles, a volume fraction of the fibrous particles consisting of long and short fibrous particles relative to all of the particles of 45 to 70%, and a volume fraction of the fine particles relative to all of the particles of less than 2.0%; a solid preparation including the hydroxyalkyl alkyl cellulose; and others.

First claim

The invention claimed is:

1. A hydroxyalkyl alkyl cellulose comprising:
a volume-based average particle diameter, determined by dry laser diffractometry, of 50 to 100 μm, and having, on a basis of a dynamic image analysis to divide all particles into fine particles, spherical particles and fibrous particles, a volume fraction of the fibrous particles consisting of long and short fibrous particles relative to all of the particles of 45 to 70%, and a volume fraction of the fine particles relative to all of the particles of less than 2.0%, wherein
the fine particles have a length of fiber of less than 40 μm,
the spherical particles have a length of fiber of 40 μm or more and consist of first and second spherical particles, wherein the first spherical particles have an elongation, which is a ratio of a diameter of fiber to a length of fiber, of 0.5 or more, and the second spherical particles have an elongation of less than 0.5, an aspect ratio, which is a ratio of a maximal Feret diameter to a minimal Feret diameter, of 0.5 or more, and a circularity, which is a ratio of a perimeter (P EQPC ) of a circle that has the same area as a projection area to a perimeter (P real ) of a real particle, of 0.7 or more,
the long fibrous particles have a length of fiber of 200 μm or more and an elongation of less than 0.5, and consist of first and second long fibrous particles, wherein the first long fibrous particles have an aspect ratio of less than 0.5, and the second long fibrous particles have an aspect ratio of 0.5 or more and a circularity of less than 0.7, and
the short fibrous particles have a length of fiber of 40 μm or more and less than 200 μm and an elongation of less than 0.5, and consist of first and second short fibrous particles wherein the first short fibrous particle have an aspect ratio of less than 0.5, and the second short fibrous particle have an aspect ratio of 0.5 or more and a circularity of less than 0.7.

2. The hydroxyalkyl alkyl cellulose according to claim 1 , having a volume fraction of the short fibrous particles of 15 to 35%.

3. The hydroxyalkyl alkyl cellulose according to claim 1 , having a volume fraction ratio of the short fibrous particles to the long fibrous particles of 0.60 to 1.40.

4. The hydroxyalkyl alkyl cellulose according to claim 1 , having a specific surface area, determined by the BET method, of not less than 0.35 m 2 /g and less than 0.50 m 2 /g.

5. The hydroxyalkyl alkyl cellulose according to claim 1 , having such a viscosity that a 2% by weight aqueous solution of the hydroxyalkyl alkyl cellulose has a viscosity at 20° C. of 50 to 200,000 mPa·s.

6. The hydroxyalkyl alkyl cellulose according to claim 1 , wherein the hydroxyalkyl alkyl cellulose is hydroxypropyl methyl cellulose.

7. A solid preparation comprising the hydroxyalkyl alkyl cellulose of claim 1 .

8. The solid preparation according to claim 7 , wherein the solid preparation is a sustained-release preparation.

9. A method for producing a hydroxyalkyl alkyl cellulose, comprising the steps of:
bringing cellulose pulp into contact with an alkali metal hydroxide solution to obtain alkali cellulose;
reacting the alkali cellulose with an etherifying agent to obtain a hydroxyalkyl alkyl cellulose product;
washing and draining the hydroxyalkyl alkyl cellulose product to obtain a first wet hydroxyalkyl alkyl cellulose;
granulating the first wet hydroxyalkyl alkyl cellulose to obtain a granulated hydroxyalkyl alkyl cellulose;
drying the granulated hydroxyalkyl alkyl cellulose to obtain a dried hydroxyalkyl alkyl cellulose having an average particle diameter, determined by a sieving analysis, of 2 to 10 mm and a water content of 6 to 10% by weight;
mixing the dried hydroxyalkyl alkyl cellulose with water to obtain a second wet hydroxyalkyl alkyl cellulose; and
drying and pulverizing the second wet hydroxyalkyl alkyl cellulose to obtain a hydroxyalkyl alkyl cellulose of claim 1 .

10. The method for producing a hydroxyalkyl alkyl cellulose according to claim 9 , wherein the second wet hydroxyalkyl alkyl cellulose has a water content of more than 6% by weight and not more than 47% by weight, and a 2% by weight aqueous solution of the produced hydroxyalkyl alkyl cellulose has a viscosity at 20° C. of 50to 10,000 mPa·s.

11. The method for producing a hydroxyalkyl alkyl cellulose according to claim 9 , wherein the second wet hydroxyalkyl alkyl cellulose has a water content of more than 47% by weight and not more than 65% by weight, and a 2% by weight aqueous solution of the produced hydroxyalkyl alkyl cellulose has a viscosity at 20° C. of more than 10,000 mPa·s and not more than 200,000 mPa·s.

12. A method for producing a tablet, comprising:
each step in the method for producing a hydroxyalkyl alkyl cellulose according to claim 9 ; and a step of tableting the produced hydroxyalkyl alkyl cellulose by a dry direct tableting method or a dry granulation tableting method.

Assignees

• Shinetsu Chemical Co

Inventors

• Yokosawa Takuya
• Kitaguchi Taishi
• Hirama Yasuyuki
• Kitamura Akira

Classifications

• G01N2021/479

  Speckle · CPC title

• C08L1/32

  Cellulose ether-esters · CPC title

• C09D101/30

  Aryl ethers; Aralkyl ethers · CPC title

• A61K47/38

  Cellulose; Derivatives thereof · CPC title

• C08B3/08 Primary

  of monobasic organic acids with three or more carbon atoms, {e.g. propionate or butyrate} · CPC title