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Pharmaceutical composition for modified release

a technology of pharmaceutical composition and modified release, which is applied in the direction of drug composition, biocide, metabolic disorder, etc., can solve the problems of unexpected variation in the data of drugcokinetic data according to the presence or absence of food intake, and achieve the reduction of cmax caused by food intake, significant relief of cmax, and reduction of changes

Inactive Publication Date: 2010-06-10
ASTELLAS PHARMA INC
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Benefits of technology

[0036]Further, a pharmaceutical composition for modified release in which AUC is not reduced can be provided.
[0037]With respect to a conventional formulation, Cmax in the fed state was decreased by 33% in comparison with that in a fasted state. By contrast, with respect to the pharmaceutical composition for modified release of the present invention, Cmax in the fed state was 58% in comparison with that in a fasted state, and this result showed that reduction of Cmax caused by food intake could be significantly alleviated by forming its formulation into the pharmaceutical formulation for modified release.

Problems solved by technology

A clinical trial of (R)-2-(2-aminothiazol-4-yl)-4′-[2-[(2-hydroxy-2-phenylethyl)amino]ethyl]acetic acid anilide in the form of conventional formulations revealed disadvantages, for example, that pharmacokinetic data unexpectedly varied according to the presence or absence of the intake of food (not published).

Method used

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  • Pharmaceutical composition for modified release
  • Pharmaceutical composition for modified release

Examples

Experimental program
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Effect test

example 1

[0104]In a mortar, 10 g of compound A hydrochloride, 2.5 g of polyethylene oxide (Dow chemical; product name: WSR-N-60K; The same compound was used in the following Examples.), and 7.5 g of polyethylene glycol (Sanyo Chemical Industries, Ltd.; PEG 6000; The same compound was used in the following Examples.) were mixed well. The mixture was formed into tablets using Autograph (Shimadzu; The same apparatus was used in the following Examples.) to obtain a pharmaceutical composition for modified release of the present invention having a tablet weight of 400 mg.

example 2

[0105]In a mortar, 10 g of compound A hydrochloride, 3.5 g of polyethylene oxide, and 6.5 g of polyethylene glycol were mixed well, and the mixture was formed into tablets using Autograph to obtain a pharmaceutical composition for modified release of the present invention having a tablet weight of 400 mg.

example 3

[0106]In a mortar, 10 g of compound A hydrochloride, 6.25 g of polyethylene oxide, and 5 g of polyethylene glycol were mixed well, and the mixture was formed into tablets using Autograph to obtain a pharmaceutical composition for modified release of the present invention having a tablet weight of 425 mg.

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Abstract

A pharmaceutical composition for modified release, comprising (1) (R)-2-(2-aminothiazol-4-yl)-4′-[2-[(2-hydroxy-2-phenylethyl)amino]ethyl]acetic acid anilide, or a pharmaceutically acceptable salt thereof, (2) at least one additive which ensures penetration of water into the pharmaceutical composition and which has a solubility such that the volume of water required for dissolving 1 g of the additive is 5 mL or less, and (3) a hydrogel-forming polymer having an average molecular weight of approximately 100,000 or more, or a viscosity of 12 mPa·s or more at a 5% aqueous solution at 25° C. is disclosed.

Description

TECHNICAL FIELD[0001]The present invention relates to a pharmaceutical composition for modified release capable of reducing food effects, which are observed in conventional tablets, by combining an active ingredient with specific ingredients to control a releasing rate of the active ingredient.[0002]More particularly, the present invention relates to a pharmaceutical composition comprising (R)-2-(2-aminothiazol-4-yl)-4′-[2-[(2-hydroxy-2-phenylethyl)amino]ethyl]acetic acid anilide or a pharmaceutically acceptable salt thereof, an additive which ensures penetration of water into the pharmaceutical composition, and a polymer which forms a hydrogel, in which the changes in AUC and Cmax caused by the intake of food can be decreased by controlling a releasing rate of the active ingredient.BACKGROUND ART[0003](R)-2-(2-aminothiazol-4-yl)-4′-[2-[(2-hydroxy-2-phenylethyl)amino]ethyl]acetic acid anilide dihydrochloride has been created by Astellas Pharma Inc., and it has been reported that thi...

Claims

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Application Information

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IPC IPC(8): A61K31/426A61P3/08
CPCA61K9/2031A61K31/426A61K9/2866A61K9/2853A61P13/08A61P13/10A61P3/04A61P3/06A61P3/08A61P3/10A61K47/32A61K47/34A61K47/38A61K9/06A61K9/2009A61K9/2013A61K9/2054A61K9/2095
Inventor TAKAISHI, YUUKITAKAHASHI, YUTAKANISHIZATO, TAKASHIMURAYAMA, DAISUKEMURAYAMA, EMIKONAKAMURA, SOICHIROSAKO, KAZUHIRO
Owner ASTELLAS PHARMA INC
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