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Stable pharmaceutical composition comprising solifenacin, and method for preparing the same

一种索利那新、混合物的技术，应用在包括索利那新的稳定药物组合物及其制备领域，能够解决分解、湿法不稳定性等问题，达到无重量偏差、杰出含量均匀性的效果

Inactive Publication Date: 2015-08-05
CJ HEALTHCARE CORP
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] Meanwhile, although solifenacin or a pharmaceutically acceptable salt thereof in the raw material state may be stable, there is a problem with the drug that it is unstable due to various factors involved in the process of preparing it into the final product. break down over time
[0011] In addition, there are limitations in preventing the time-based decomposition of solifenacin by selecting and using specific binders for the wet granulation process due to the instability of the wet process

Method used

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  • Stable pharmaceutical composition comprising solifenacin, and method for preparing the same
  • Stable pharmaceutical composition comprising solifenacin, and method for preparing the same
  • Stable pharmaceutical composition comprising solifenacin, and method for preparing the same

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0046] Mill mixtures 1 and 2 were mixed in a 1 kg mixer (erweka AR402 / cubic mixer) at 200 rpm for 15 minutes, and the resulting mixture was lubricated and mixed with 7.5 g of magnesium stearate, filtered through a 30-mesh sieve, and then filtered using a single A tablet press (erweka AR401) forms round tablets. The respective component contents of the tablets thus obtained are shown in Table 1 below.

[0047] 【Table 1】

[0048] mixed purpose

[0049] Examples 2 to 7 and Comparative Example 1

Embodiment 2 to 7 and comparative Embodiment 1

[0051] Regarding the preparation of tablets with the compositions of Examples 2 to 7 and Comparative Example 1, and 16.65 g of solifenacin succinate, butylated hydroxytoluene (varies from 0.25 g to 0.5 g, depending on Example 2 to 7), 100.0 g of lactose hydrate and 50.0 g of microcrystalline cellulose were mixed by milling, and then filtered through a 30-mesh sieve (grinding and mixing-1). Subsequently, 100.0 g of microcrystalline cellulose and lactose hydrate (ranging from 212.35 g to 212.85 g, depending on Examples 2 to 7 and Comparative Example 1) were then filtered through a 30 mesh screen (Grind Mix-2).

[0052] Mill mixtures 1 and 2 were mixed in a 1 kg mixer (erweka AR402 / cubic mixer) at 200 rpm for 15 minutes, and the resulting mixture was lubricated and mixed with 7.5 g of magnesium stearate, filtered through a 30-mesh sieve, and then filtered using a single A tablet press (erweka AR401) forms round tablets. The core tablets thus completed are used for (yellow, opa...

Embodiment 8 to 12 and comparative Embodiment 2 and 3

[0058] 16.65 g of solifenacin succinate, 0.5 g of butylated hydroxytoluene, low-substituted hydroxypropyl cellulose (ranging from 0.0 g to 150.0 g, depending on each combination of Examples 8 to 11 and Comparative Example 2 ) and 95.0 g of isomalt were mixed by grinding and filtered through a 30-mesh sieve (Grind Mix-1).

[0059] Subsequently, 10.0 g of hydrophobic colloidal silicon dioxide and lactose hydrate (ranging from 207.35 g to 357.35 g, depending on Examples 8 to 11 and Comparative Example 2) were mixed and filtered through a 30-mesh sieve (Grind Mix-2 ).

[0060] Mill mixtures 1 and 2 were mixed in a 1 kg mixer (erweka AR402 / cubic mixer) at 200 rpm for 15 minutes, and the resulting mixture was lubricated and mixed with 7.5 g of magnesium stearate, filtered through a 30-mesh sieve, and then filtered using a single A tablet press (erweka AR401) forms round tablets. The core tablets thus completed are used for (yellow, opadry03B52293) coating. The respective compon...

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Abstract

The present invention relates to a solifenacin preparation containing solifenacin or a pharmaceutically acceptable salt thereof, an antioxidant, and a binder, which is manufactured via direct compression. Compared to the preparations manufactured via conventional wet granulation process, the preparation of the present invention can be manufactured by a simplified process such as direct compression, and has improved content uniformity, mixing degree, etc., even when the preparation is manufactured by high speed tableting.

Description

technical field [0001] The present invention relates to a stable formulation comprising solifenacin and a method for its preparation. Background technique [0002] Solifenacin is a compound represented by the following Chemical Formula 1, and is reported to have excellent selective antimuscarinic M3 receptor antagonism. [0003] [chemical formula 1] [0004] [0005] Meanwhile, although solifenacin or a pharmaceutically acceptable salt thereof in the raw material state may be stable, there is a problem with the drug that it is unstable due to various factors involved in the process of preparing it into the final product. break down over time. As a representative example, the amorphous form of solifenacin succinate is produced during wet granulation and is easily oxidized in a short time. Specifically, the main degradation product (oxidized form of solifenacin succinate) has been reported to be the main cause of the breakdown problem of the main drug. That is, it is di...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/20A61K9/28A61K31/49A61K47/08A61K47/38
CPCA61K31/439A61K9/2054A61K31/4725A61P11/00A61P11/02A61P11/06A61P13/00A61P13/02A61P13/10A61P43/00A61K9/20A61K47/38A61K9/2095A61K47/10
Inventor 徐英姬曹永大柳春善尹美永崔河龙韩成均
Owner CJ HEALTHCARE CORP
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