Solid pharmaceutical composition

Patent metadata

Field	Value
Publication number	US-9603804-B2
Application number	US-201414786394-A
Country	US
Kind code	B2
Filing date	Apr 24, 2014
Priority date	Apr 25, 2013
Publication date	Mar 28, 2017
Grant date	Mar 28, 2017

Abstract

[Problem] To provide a solid pharmaceutical composition which contains a compound represented by general formula (1) or a salt thereof and suppresses decomposition of said compound or salt thereof, and a production method of said solid pharmaceutical composition.
[Solution] This solid pharmaceutical composition contains a compound represented by general formula (1) or a salt thereof, a cellulosic excipient, and an acidic substance of pH 4.0 or less.

First claim

The invention claimed is:

1. A solid pharmaceutical composition comprising:
7-[3S,4S)-3-{(cyclopropylamino)methyl}-4-fluoropyrolidin-1-yl]-6-fluoro-1-(2-fluoroethyl)-8-methoxy-4-oxo-1,4-dihydroquinoline-3-carboxylic acid hydrochloride;
a cellulosic excipient; and
an acidic substance having a pH of 4.0 or lower,
wherein the acidic substance is at least one compound selected from the group consisting of glutamic acid hydrochloride, tartaric acid, citric acid, malic acid, fumaric acid, monobasic sodium citrate, glutamic acid, aspartic acid, and alginic acid.

2. The solid pharmaceutical composition according to claim 1 , wherein the acidic substance has a solubility in water at 20° C. of 30% or less.

3. The solid pharmaceutical composition according to claim 1 , wherein the acidic substance has a pH of 2.2 or higher and 4.0 or lower.

4. The solid pharmaceutical composition according to claim 1 , wherein the acidic substance is at least one compound selected from the group consisting of fumaric acid, monobasic sodium citrate, glutamic acid, aspartic acid, and alginic acid.

5. The solid pharmaceutical composition according to claim 1 , wherein the cellulosic excipient is crystalline cellulose.

6. The solid pharmaceutical composition according to claim 1 , which is obtained by mixing the 7-[(3S,4S)-3-{(cyclopropylamino)methyl}-4-fluoropyrolidin-1-yl]-6-fluoro-1-(2-fluoroethyl)-8-methoxy-4-oxo-1,4-dihydroquinoline-3-carboxylic acid hydrochloride, the cellulosic excipient, and the acidic substance to obtain a mixture,
wherein the acidic substance is at least one compound selected from the group consisting of glutamic acid hydrochloride, tartaric acid, citric acid, malic acid, fumaric acid, monobasic sodium citrate, glutamic acid, aspartic acid, and alginic acid, and
granulating the mixture through a dry granulation method.

7. A method of producing a solid pharmaceutical composition, comprising:
mixing 7-[(3S,4S)-3-{(cyclopropylamino)methyl}-4-fluoropyrolidin-1-yl]-6-fluoro-1-(2-fluoroethyl)-8-methoxy-4-oxo-1,4-dihydroquinoline-3-carboxylic acid hydrochloride, a cellulosic excipient, and an acidic substance having a pH of 4.0 or lower to obtain a mixture,
wherein the acidic substance is at least one compound selected from the group consisting of glutamic acid hydrochloride, tartaric acid, citric acid, malic acid, fumaric acid, monobasic sodium citrate, glutamic acid, aspartic acid, and alginic acid; and
granulating the mixture through a dry granulation method.

Assignees

• Kyorin Seiyaku Kk

Inventors

• Uchida Hiroshi
• Hanada Masataka

Classifications

• A61P31/04

  Antibacterial agents · CPC title

• A61K31/4709

  Non-condensed quinolines and containing further heterocyclic rings · CPC title

• A61K9/2013

  Organic compounds, e.g. phospholipids, fats · CPC title

• A61K9/2095

  Tabletting processes · CPC title

• A61K9/2054 Primary

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