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Stable particular pharmaceutical composition of solifenacin or salt thereof

A technology of solifenacin and composition, applied in the field of stable granular pharmaceutical composition of solifenacin or its salt

Inactive Publication Date: 2008-03-12
ASTELLAS PHARMA INC
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0012]On the other hand, Solifenacin and its salts are known to have very high solubility to various solvents and have very strong bitter taste and astringent properties

Method used

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  • Stable particular pharmaceutical composition of solifenacin or salt thereof
  • Stable particular pharmaceutical composition of solifenacin or salt thereof
  • Stable particular pharmaceutical composition of solifenacin or salt thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0091] A substance obtained by coating solifenacin succinate on crystalline cellulose core particles using HPC-SL as a binder

[0092] 10 parts of solifenacin succinate, 3.4 parts of hydroxypropyl cellulose (trade name HPC-SL, manufactured by Nippon Soda Co., Ltd., hereinafter referred to as HPC) are added in the mixed solution of 26.6 parts of water and 26.6 parts of methanol, and stirred (MGM-66, manufactured by SHIBATA) was stirred and dissolved to prepare a drug solution. Next, 60 parts of crystalline cellulose (trade name Celphere, manufactured by Asahi Kasei) was added to a fluidized bed granulator (FLO-1, manufactured by Gratto Co., Ltd.). 3 / min, adhesive liquid spray speed 4.0g / min, spray air pressure 3.0kg / cm 2 Under the conditions, the aforementioned drug solution is sprayed on the Celphere to obtain the granular composition of the present invention.

Embodiment 2

[0094] The granular composition obtained in Example 1 was humidified at 25° C. and 75% RH for 12 hours, further dried at 30° C. and 40% RH for 3 hours, and crystallized to obtain the granular composition of the present invention.

Embodiment 3

[0096] Using PEG6000 as a binder, the material obtained by coating solifenacin succinate on crystalline cellulose core particles

[0097] Add 10 parts of solifenacin succinate and 3.4 parts of polyethylene glycol (trade name Macrogol 6000, manufactured by Sanyo Chemical Industry) to a mixed solution of 26.6 parts of water and 26.6 parts of methanol, and use a stirrer (MGM-66, manufactured by SHIBATA) Stir to dissolve and prepare a drug solution. Next, 60 parts of Celphere (manufactured by Asahi Kasei) was added to a fluidized bed granulator (FLO-1, manufactured by Gratto Co., Ltd.) 3 / min, adhesive liquid spray speed 10g / min, spray air pressure 3.0kg / cm 2 Under the conditions, the aforementioned drug solution is sprayed on the Celphere to obtain the granular composition of the present invention.

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Abstract

The present invention relates to a granule of solifenacin or its salt that is suitable for coating when clinically providing solifenacin or its salt preparation, is spherical, and can inhibit decomposition over time pharmaceutical composition. More specifically, the present invention relates to a granular pharmaceutical composition obtained when solifenacin or its salt is formulated with a binder whose Tg or mp value is less than 174°C. Moreover, a more stable granular composition of solifenacin or a salt thereof can be provided by performing a crystallization-promoting treatment after manufacturing the granular pharmaceutical composition.

Description

technical field [0001] The present invention relates to a stable granular pharmaceutical composition formed by using solifenacin or its salt and a specific binder and a manufacturing method thereof, an orally disintegrating tablet containing the granular pharmaceutical composition, and the granular medicine Method of stabilizing the composition. Background technique [0002] Solifenacin is shown in the following structural formula (I): [0003] [chemical formula 1] [0004] [0005] Structural formula (I) [0006] It is chemically known as 1-phenyl-1,2,3,4-tetrahydro-2-isoquinolinecarboxylic acid (1R,3'R)-quinuclidinyl ester. [0007] It has been reported that a series of quinucidine derivatives including solifenacin or its salts have no effect on muscarine M 3 Receptors have excellent selective antagonism and are useful in urinary disorders (e.g. neurogenic urinary frequency, neurogenic bladder, nocturia, unstable bladder, bladder contractures an...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/4725A61K9/14A61K47/26A61K47/32A61K47/34A61K47/36A61K47/38
CPCA61K9/1676A61K31/4725A61K9/0056A61P11/00A61P11/06A61P13/00A61P13/06A61K9/16A61K31/439A61K47/26A61K47/38
Inventor 梅岛启之大井宏志斋藤胜实武谷佑子
Owner ASTELLAS PHARMA INC
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