Solid preparation containing alkyl cellulose and method for producing the same

Patent metadata

Field	Value
Publication number	US-10696751-B2
Application number	US-201715450151-A
Country	US
Kind code	B2
Filing date	Mar 6, 2017
Priority date	Mar 9, 2016
Publication date	Jun 30, 2020
Grant date	Jun 30, 2020

Abstract

Provided are a solid preparation comprising an alkyl cellulose which provides excellent moldability and disintegrability even in a small amount of the alkyl cellulose, and a production method therefor. Specifically, provided are a solid preparation having an alkyl cellulose having a specific surface area by BET method of 0.5 to 10.0 m2/g and a dissolution start temperature of 5 to 27° C.; and a method for producing a solid preparation having the steps of: mixing a cellulose pulp and a first alkali metal hydroxide solution with stirring to obtain alkali cellulose, reacting the alkali cellulose with an alkylating agent to obtain a first reaction mixture, mixing the first reaction mixture and a second alkali metal hydroxide solution with stirring and without further addition of any alkylating agent to obtain a second reaction mixture, and pulverizing an alkyl cellulose isolated from the second reaction mixture to obtain an alkyl cellulose.

First claim

The invention claimed is:

1. A solid preparation comprising:
an alkyl cellulose having a specific surface area determined by BET method of 0.5 to 10.0 m 2 /g and a dissolution start temperature of 5 to 27° C.

2. The solid preparation according to claim 1 , wherein a 2% by weight aqueous solution of the alkyl cellulose has a viscosity of 1 to 15 mPa·s at 20° C.

3. The solid preparation according to claim 1 , wherein the alkyl cellulose has a volume average particle size determined by dry laser diffractometry of 1 to 50 μm.

4. The solid preparation according to claim 2 , wherein the alkyl cellulose has a volume average particle size determined by dry laser diffractometry of 1 to 50 μm.

5. The solid preparation according to claim 1 , wherein the alkyl cellulose has a loose bulk density of 0.01 to 0.30 g/mL.

6. The solid preparation according to claim 1 , wherein the alkyl cellulose has a degree of substitution (DS) of alkyl group of 1.61 to 2.03.

7. The solid preparation according to claim 1 , wherein the alkyl cellulose is methyl cellulose.

8. The solid preparation according to claim 1 , wherein the alkyl cellulose comprised by the solid preparation is in an amount of more than 0% by weight but not more than 20% by weight.

9. A method for producing a solid preparation, comprising the steps of:
mixing a cellulose pulp and a first alkali metal hydroxide solution with stirring to obtain alkali cellulose;
reacting the alkali cellulose with an alkylating agent to obtain a first reaction mixture;
mixing the first reaction mixture and a second alkali metal hydroxide solution with stirring and without further addition of any alkylating agent to obtain a second reaction mixture;
isolating an alkyl cellulose from the second reaction mixture, wherein the isolated alkyl cellulose has a specific surface area determined by BET method of 0.5 to 10.0 m 2 /g and a dissolution start temperature of 5 to 27° C.;
pulverizing the alkyl cellulose to obtain a pulverized alkyl cellulose;
depolymerizing the pulverized alkyl cellulose to obtain a low-polymerization-degree alkyl cellulose;
pulverizing the low-polymerization-degree alkyl cellulose to obtain a pulverized low-polymerization-degree alkyl cellulose; and
subjecting a mixture or granule containing the pulverized low-polymerization-degree alkyl cellulose and a drug to dry direct tableting or dry granulation tableting;
wherein a ratio of a weight of a first alkali metal hydroxide in the first alkali metal hydroxide solution to a total weight of the first alkali metal hydroxide in the first alkali metal hydroxide solution and a second alkali metal hydroxide in the second alkali metal hydroxide solution is 50 to 86%.

Assignees

• Shinetsu Chemical Co

Inventors

• Yokosawa Takuya
• Maruyama Naosuke
• Kitamura Akira

Classifications

• A61K9/2095

  Tabletting processes · CPC title

• A61K9/2072

  characterised by shape, structure or size; Tablets with holes, special break lines or identification marks; Partially coated tablets; Disintegrating flat shaped forms (A61K9/0004, A61K9/0056, A61K9/0065 take precedence) · CPC title

• A61K9/2054 Primary

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

• C11D17/0073

  Tablets · CPC title

• C11D3/225

  etherified, e.g. CMC · CPC title