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

Patent metadata

Field	Value
Publication number	US-10314786-B2
Application number	US-201715722592-A
Country	US
Kind code	B2
Filing date	Oct 2, 2017
Priority date	Oct 7, 2016
Publication date	Jun 11, 2019
Grant date	Jun 11, 2019

Abstract

Provided is a hydroxyalkyl alkyl cellulose exhibiting good flowability and high compressibility. More specifically, there are provided a hydroxyalkyl alkyl cellulose having a volume-based average particle size, determined by dry laser diffractometry, of more than 100 μm and not more than 150 μm; and after dividing all particles into fine particles, spherical particles and fibrous particles by a dynamic image analysis, a volume fraction of the fibrous particles relative to all of the particles of more than 40% and not more than 50%, 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 having a volume-based average particle size, determined by dry laser diffractometry, of more than 100 μm and not more than 150 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 relative to all of the particles of more than 40% and not more than 50%, 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, and
the fibrous particles have a length of fiber of 40 μm or more and are particles other than the spherical particles consisting 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.

2. The hydroxyalkyl alkyl cellulose according to claim 1 , having, after dividing the fibrous particles into long and short fibrous particles, a ratio of a volume fraction of the short fibrous particles relative to all of the particles to a volume fraction of the long fibrous particles relative to all of the particles of 0.35 to 0.55;
wherein
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 40μm 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.

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

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

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

6. The solid preparation according to claim 5 , wherein the solid preparation is a sustained-release preparation.

7. 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 size, determined by a sieving analysis, of 2 to 10 mm and a water content of 5% by weight or less;
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 .

8. The method for producing a hydroxyalkyl alkyl cellulose according to claim 7 , wherein the second wet hydroxyalkyl alkyl cellulose has a water content of 40 to 60% by weight.

9. A method for producing a tablet, comprising:
each step in the method for producing a hydroxyalkyl alkyl cellulose according to claim 7 ; 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

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

Classifications

• A61K47/38

  Cellulose; Derivatives thereof · CPC title

• A61K9/146

  with organic macromolecular compounds · CPC title

• C08L1/32

  Cellulose ether-esters · CPC title

• A61K9/2054 Primary

  Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose · CPC title

• C08B11/20

  Post-etherification treatments of chemical or physical type, {e.g. mixed etherification in two steps}, including purification · CPC title