Method of preparing composite granule comprising low-substituted hydroxypropyl cellulose and rapid release preparation

Patent metadata

Field	Value
Publication number	US-10406107-B2
Application number	US-201313909516-A
Country	US
Kind code	B2
Filing date	Jun 4, 2013
Priority date	Jun 15, 2012
Publication date	Sep 10, 2019
Grant date	Sep 10, 2019

Abstract

Provided is a base material for dry direct tableting, the material being excellent in a binding property and disintegrability. More specifically, provided is a method of preparing a composite granule comprising at least a step of granulating a second sugar or sugar alcohol while adding thereto an aqueous dispersion comprising at least low-substituted hydroxypropyl cellulose having a degree of hydroxypropoxy substitution of 5 to 16% by weight, polyvinyl alcohol, a first sugar or sugar alcohol, and water.

First claim

The invention claimed is:

1. A method of preparing a composite granule for tableting, comprising at least a step of granulating a second sugar or sugar alcohol while spraying thereto an aqueous dispersion comprising at least low-substituted hydroxypropyl cellulose having a degree of hydroxypropoxy substitution of 5 to 16% by weight, polyvinyl alcohol, a first sugar or sugar alcohol, and water, wherein the aqueous dispersion coats a surface of the second sugar or sugar alcohol for surface-modification of the second sugar or sugar alcohol with the low-substituted hydroxypropyl cellulose and the polyvinyl alcohol, and wherein the composite granule is characterized by the absence of a drug except for the first sugar or sugar alcohol and the second sugar or sugar alcohol.

2. The method of preparing a composite granule according to claim 1 , wherein the first sugar or sugar alcohol and the second sugar or sugar alcohol may be the same or different and are each at least one selected from the group consisting of mannitol, trehalose, xylitol, erythritol, lactose and sucrose.

3. The method of preparing a composite granule according to claim 1 , wherein the low-substituted hydroxypropyl cellulose is comprised in an amount of 1 to 15 parts by weight based on 100 parts by weight of a total amount of the first sugar or sugar alcohol and the second sugar or sugar alcohol.

4. The method of preparing a composite granule according to claim 1 , wherein the polyvinyl alcohol is comprised in an amount of 0.05 to 0.4 parts by weight based on 100 parts by weight of a total amount of the first sugar or sugar alcohol and the second sugar or sugar alcohol.

5. A rapid release tablet comprising at least the composite granule prepared by the method as claimed in claim 1 and a drug, and being obtained by mixing the composite granule with the drug.

Assignees

• Shinetsu Chemical Co

Inventors

• Maruyama Naosuke
• Hirama Yasuyuki

Classifications

• A61K9/2018

  Sugars, or sugar alcohols, e.g. lactose, mannitol; Derivatives thereof, e.g. polysorbates · CPC title

• A61K47/38 Primary

  Cellulose; Derivatives thereof · CPC title

• A61K31/167

  having the nitrogen of a carboxamide group directly attached to the aromatic ring, e.g. lidocaine, paracetamol · CPC title

• A61K9/0056

  Mouth soluble or dispersible forms; Suckable, eatable, chewable coherent forms; Forms rapidly disintegrating in the mouth; Lozenges; Lollipops; Bite capsules; Baked products; Baits or other oral forms for animals · CPC title

• A61K31/375

  Ascorbic acid, i.e. vitamin C; Salts thereof · CPC title