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Pharmaceutical composition for treating disease in oral cavity comprising rebamipide

A technology of rebamipide and composition, which is applied in the field of pharmaceutical composition containing rebamipide for the treatment of oral diseases, can solve the problem of not including viscosity enhancer, low concentration of rebamipide, rebamipide low level problem

Inactive Publication Date: 2013-12-04
OTSUKA PHARM CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, in the above-mentioned liquid formulations, the concentration of rebamipide is very low, namely 300 mg / 300 mL or 600 mg / 300 mL (ie, 1 mg / mL or 2 mg / mL), and each mouthwash is about 50 mL, and the rebamipide used in it is the larger granule contained in the commercially available tablets
Additionally, thanks to ALKOX ? (Polyethylene oxide) is an industrial additive and its use as a pharmaceutical additive is problematic
[0006] Patent Reference 4 discloses a formulation example (rebamipide 0.2 mg / mL) as a spray formulation for the treatment of stomatitis by mixing 100 mg rebamipide, 2 g Inagel ? (F-13) and 5 g ALKOX ? (E-30), prepared by adding parabens and ethanol, and adjusting the volume to 500 mL, but the concentration of rebamipide was very low, and the particle size of rebamipide was not studied in this reference
[0007] In addition, Patent Reference 5 discloses a suspension of rebamipide fine particles obtained by mixing at least one compound selected from water-soluble polymers and surfactants, an acidic aqueous solution, and an aqueous solution containing a water-soluble salt of rebamipide prepared with improved clarity, but this patent reference only discloses ophthalmic compositions, which do not include viscosity enhancers

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0139] 20 g of carboxymethylcellulose sodium (CMCNa) (7L2P, Ashland) was dissolved in approximately 400 g of purified water. 28.4 g of concentrated hydrochloric acid was added thereto, and further purified water was added to prepare 550 g of sodium carboxymethylcellulose (7L2P)-hydrochloric acid aqueous solution. Separately, 17.6 g of sodium hydroxide was added to about 2600 g of purified water to prepare an aqueous sodium hydroxide solution. 81.6 g of rebamipide (Otsuka Pharmaceutical Co., Ltd.) was dissolved in an aqueous sodium hydroxide solution while heating the solution, and then purified water was added thereto to adjust the total weight to 2940 g. From the prepared sodium hydroxide-rebamipide solution, 1470 g was taken out for the next step.

[0140] To a disperser (ROBOMIX) cooled in an ice bath ? , PRIMIX Corporation) was gradually added to the aqueous solution of sodium carboxymethylcellulose-hydrochloric acid stirred at 5500 rpm, and the above-mentioned sodium hy...

Embodiment 2

[0155] 40 g of hydroxypropylmethylcellulose (HPMC) (TC-5E, Shin-Etsu Chemical Co., Ltd.) was dissolved in about 400 g of purified water. 28.4 g of concentrated hydrochloric acid was added thereto, and purified water was further added to prepare 550 g of HPMC(TC-5E)-hydrochloric acid aqueous solution. Separately, 17.6 g of sodium hydroxide was added to about 2600 g of purified water to prepare an aqueous sodium hydroxide solution. 81.6 g of rebamipide (Otsuka Pharmaceutical Co., Ltd.) was dissolved in an aqueous sodium hydroxide solution while heating the solution, and then purified water was added thereto to adjust the total weight to 2940 g. From the prepared sodium hydroxide-rebamipide solution, 1470 g was taken out for the next step.

[0156] To a disperser (ROBOMIX) cooled in an ice bath ? , PRIMIX Corporation) was gradually added to the aqueous solution of HPMC (TC-5E)-hydrochloric acid stirred at 5500 rpm, and the above-mentioned sodium hydroxide-rebamipide solution wh...

Embodiment 3

[0170] 40 g of polyvinylpyrrolidone K25 (PVPK25) (BASF) was dissolved in about 400 g of purified water. 28.4 g of concentrated hydrochloric acid was added thereto, and purified water was further added to prepare 550 g of PVPK25-hydrochloric acid aqueous solution. Separately, 17.6 g of sodium hydroxide was added to about 2600 g of purified water to prepare an aqueous sodium hydroxide solution. 81.6 g of rebamipide (Otsuka Pharmaceutical Co., Ltd.) was dissolved in an aqueous sodium hydroxide solution while heating the solution, and then purified water was added thereto to adjust the total weight to 2940 g. From the prepared sodium hydroxide-rebamipide solution, 1470 g was taken out for the next step.

[0171] To a disperser (ROBOMIX) cooled in an ice bath ? , PRIMIX Corporation) was gradually added to the aqueous solution of PVPK25-hydrochloric acid stirred at 5500 rpm with the above-mentioned sodium hydroxide-rebamipide solution whose temperature was maintained at about 50°C...

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Abstract

The present invention is directed to a pharmaceutical composition comprising rebamipide having a mean particle size of less than 500 nm, a dispersing agent, and a viscosity enhancing agent wherein the viscosity enhancing agent has no aggregative action for the rebamipide particles, which is used as a gargle or a liquid preparation for swish and swallow comprising rebamipide for preventing and / or treating stomatitis caused by radiotherapy.

Description

technical field [0001] The present invention relates to a pharmaceutical composition suitable for treating diseases of the oral cavity or pharynx, especially oral mucosal disorders, which comprises rebamipide [chemical name: 2-(4-chlorobenzamido) as an active ingredient )-3-(2-oxo-1,2-dihydroquinolin-4-yl)propionic acid], the average particle diameter of which is less than 500 nm (preferably the average particle diameter is less than 300 nm); the preparation method of the composition ; and its uses. Background technique [0002] It is known that rebamipide or a salt thereof as an active ingredient in the pharmaceutical composition of the present invention can be used as a drug for treating gastritis / gastric ulcer. In addition, it is also disclosed that rebamipide is useful for the treatment of dry eye, that is, xerophthalmia (Patent Reference 1), and a pharmaceutical composition containing rebamipide as a salivary secretion stimulating agent is also known (Patent Reference ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/00A61K31/4704
CPCA61K9/006A61K47/38A61K31/4704A61K9/10A61K47/32A61P1/00A61P1/02A61P1/04A61P29/00A61K9/08
Inventor 松田贵邦佐古信朋中岛贵子樱井一志
Owner OTSUKA PHARM CO LTD
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