Granulated composite, rapid release tablet and method for producing same

Patent metadata

Field	Value
Publication number	US-11723872-B2
Application number	US-201916601270-A
Country	US
Kind code	B2
Filing date	Oct 14, 2019
Priority date	Nov 15, 2013
Publication date	Aug 15, 2023
Grant date	Aug 15, 2023

Abstract

Provided is a rapid release tablet excellent in binding capability and disintegrability and also excellent in storage stability and the like. More specifically, provided are a granulated composite comprising low-substituted hydroxypropyl cellulose having a degree of hydroxypropoxy substitution of from 5 to 16% by weight and D-mannitol, wherein the D-mannitol contains 0.9% by weight or less of D-sorbitol; a rapid release tablet comprising the granulated composite and a drug; and a method for producing a granulated composite comprising the steps of: mixing low-substituted hydroxypropyl cellulose having a degree of hydroxypropoxy substitution of from 5 to 16% by weight, first D-mannitol, and water to obtain an aqueous dispersion, and granulating while adding the aqueous dispersion to second D-mannitol, wherein the first D-mannitol and the second D-mannitol contain 0.9% by weight or less of D-sorbitol in total.

First claim

The invention claimed is:

1. A rapid release tablet, comprising a drug and a granulated composite comprising low-substituted hydroxypropyl cellulose having a degree of hydroxypropoxy substitution of from 5 to 16% by weight, a first D-mannitol and a second D-mannitol,
wherein the granulated composite is not a physical mixture but has a modified surface by granulating while spraying a surface of the second D-mannitol with a homogenous mixture of the low-substituted hydroxypropyl cellulose and the first D-mannitol, an interior of the second D-mannitol not being surface-modified, and
wherein the first D-mannitol and the second D-mannitol contain 0.81% by weight or less of D-sorbitol, and disintegration time of the tablet in an oral cavity is less than 30 seconds.

2. The rapid release tablet according to claim 1 , wherein the homogenous mixture further comprises polyvinyl alcohol.

3. The rapid release tablet according to claim 1 , wherein the first D-mannitol is present in the granulated composite in an amount of 5% to 50% by weight with respect to the total amount of D-mannitol.

Assignees

• Shinetsu Chemical Co

Inventors

• Hirama Yasuyuki
• Maruyama Naosuke

Classifications

• A61K9/2054 Primary

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

• A61K9/1623

  Sugars or sugar alcohols, e.g. lactose; Derivatives thereof; Homeopathic globules · CPC title

• A61K9/1635

  obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyvinyl pyrrolidone, poly(meth)acrylates · CPC title

• A61K9/1652

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