Low-substituted hydroxypropyl cellulose and solid preparation

Patent metadata

Field	Value
Publication number	US-10959959-B2
Application number	US-201715667307-A
Country	US
Kind code	B2
Filing date	Aug 2, 2017
Priority date	Aug 16, 2016
Publication date	Mar 30, 2021
Grant date	Mar 30, 2021

Abstract

Provided is low-substituted hydroxypropyl cellulose from which a granulation product having an adequate particle size can be obtained in a wet granulation method and a tablet having excellent compactibility and disintegrability can be obtained. More specifically, provided is low-substituted hydroxypropyl cellulose having a hydroxypropoxyl content of from 5 to 16% by weight and a water-soluble content of less than 2% by weight, wherein a weight ratio of water to the low-substituted hydroxypropyl cellulose giving a maximum torque is from 3 to 5 as determined while adding one part by weight of water per minute to one part by weight of the low-substituted hydroxypropyl cellulose under mixing with biaxial mixing blades. Also provided are a solid preparation including the low-substituted hydroxypropyl cellulose, and the like.

First claim

The invention claimed is:

1. Low-substituted hydroxypropyl cellulose having a hydroxypropoxyl content of from 5 to 16% by weight and a water-soluble content at 25° C. of less than 1.5% by weight, wherein a weight ratio of water to the low-substituted hydroxypropyl cellulose giving a maximum torque is from 3 to 5 as determined while adding one part by weight of water per minute to one part by weight of the low-substituted hydroxypropyl cellulose under mixing with biaxial mixing blades.

2. The low-substituted hydroxypropyl cellulose according to claim 1 , having an alkali viscosity at 20° C. of from 20 to 120 mPa·s, wherein the alkali viscosity means a viscosity of a 2% by weight solution of the low-substituted hydroxypropyl cellulose in a 10% by weight aqueous sodium hydroxide solution.

3. The low-substituted hydroxypropyl cellulose according to claim 1 , having a volume-average particle size of from 30 to 100 μm as measured by a dry laser diffraction method.

4. The low-substituted hydroxypropyl cellulose according to claim 1 , wherein a mixing blade on one axis of the biaxial mixing blades is rotated at 60 rpm with a peripheral velocity of 0.72 m/minute and a mixing blade on the other axis of the biaxial mixing blades is rotated at 30 rpm with a peripheral velocity of 0.36 m/minute.

5. A solid preparation, comprising the low-substituted hydroxypropyl cellulose of claim 1 .

6. The solid preparation according to claim 5 , having a dosage form of a tablet, granules, fine granules or a capsule.

7. A method for producing low-substituted hydroxypropyl cellulose of claim 1 , comprising the steps:
pulverizing starting low-substituted hydroxypropyl cellulose having a hydroxypropoxyl content of from 5 to 16% by weight into low-substituted hydroxypropyl cellulose powder having a volume-average particle size of from 30 to 100 μm as measured by a dry laser diffraction method; and
classifying the low-substituted hydroxypropyl cellulose powder to remove therefrom small particles having a volume-average particle size of less than 30 μm as measured by the dry laser diffraction method.

8. A method for producing a granulation product of the low-substituted hydroxypropyl cellulose, comprising the steps of:
blending the low-substituted hydroxypropyl cellulose of claim 1 , a drug, and water or a water-soluble binder solution to obtain a mixture; and
granulating the mixture.

Assignees

• Shinetsu Chemical Co

Inventors

• Hirama Yasuyuki
• Maruyama Naosuke

Classifications

• A61K9/1652 Primary

  Polysaccharides, e.g. alginate, cellulose derivatives; Cyclodextrin (homeopathic globules A61K9/1623) · CPC title

• A23V2002/00

  Food compositions, function of food ingredients or processes for food or foodstuffs · CPC title

• A61K47/38

  Cellulose; Derivatives thereof · CPC title

• C08L1/284

  with hydroxylated hydrocarbon radicals · CPC title

• A23V2200/21

  Binding agent · CPC title