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Microcrystal and medicinal preparation containing the same

A crystallization and fine technology, applied in the direction of medical preparations containing active ingredients, pharmaceutical formulas, drug combinations, etc., can solve the problems of low stability, low solubility and oral absorbability, dissolution, absorbability, and stability Stable performance and other issues

Inactive Publication Date: 2006-10-11
KYOWA HAKKO KIRIN CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The crystals of Compound (I) obtained by the method described in the cited documents above are tabular crystals with an average particle diameter of 100 to several hundreds of μm, and have low solubility in water and low oral absorbability.
In addition, the crystal of Compound (I) does not have stable performance in terms of dissolution, absorption, and stability in the preparation process. Although it has been confirmed that the absorption can be improved by solubilization, it still has low stability. The problem

Method used

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  • Microcrystal and medicinal preparation containing the same
  • Microcrystal and medicinal preparation containing the same
  • Microcrystal and medicinal preparation containing the same

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0037] The crystals of the unpulverized compound (I) obtained by the method described in JP-A-2002-53580 were crushed at a crushing pressure of 0.4 MPa and a supply rate of 1 g / min using a jet mill (A-0jetto / Seishin Enterprises). Under the conditions, crushing was carried out. The average particle diameter of the compound (I) before and after pulverization was measured with a laser scattering type particle size distribution analyzer (LDSA-1300A / Tohnichi COMPUTER-APRIKE-SIONS). In addition, the crystallinity of compound (I) before and after pulverization was measured with a powder X-ray diffractometer (PW3050 / PANalytical). The results are shown in Table 1.

[0038] before crushing

Embodiment 2

[0040] Unpulverized crystals of Compound (I) obtained by the method described in JP-A-2002-53580 were ice-cooled, and then pulverized with a jet mill at a pulverization pressure of 0.6 MPa and a supply rate of 2 kg / hour. The average particle diameter of the compound (I) before and after pulverization was measured with a laser scattering type particle size distribution analyzer (Mastersizer 2000 / Marvel Instruments). In addition, the crystallinity of compound (I) before and after pulverization was measured with a powder X-ray diffractometer (PW3050 / PANalytical). The results are shown in Table 2.

[0041] before crushing

Embodiment 3

[0043] 0.8 g of the jet-milled compound (I) obtained in Example 2 and 3.2 g of hydroxypropylmethylcellulose were mixed in a vinyl bag to obtain a mixture of compound (I) and hydroxypropylmethylcellulose.

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Abstract

The present invention provides microcrystals of (S)-(+)-3,3,3-trifluoro-2-hydroxy-2-methyl-N-(5,5,10-trioxo-4,10-dihydrothieno[3,2-c][1]benzothiepin-9-yl) propaneamide represented by the following formula which has an average particle size of 80 mum or less, a pharmaceutical formulation comprising the microcrystals, and the like.

Description

technical field [0001] The present invention relates to a kind of (s)-(+)-3,3,3-trifluoro-2-hydroxyl-2-methyl-N-(5,5,10-trioxy-4,10-dihydrothiophene A crystal of [3,2-c][1]benzothiapin-9-yl)propaneamide [hereinafter referred to as compound (I)] and a pharmaceutical preparation containing the crystal. Background technique [0002] Compound (I) has a therapeutic effect on various diseases and symptoms such as frequent urination, urinary incontinence, and overactive bladder, and its crystallization and synthesis methods are known. In addition, examples of its usage form are also known (for example, refer to WO98 / 46587, WO02 / 78710, WO02 / 78711, WO02 / 78712, JP-A-2002-53580). The crystals of Compound (I) obtained by the methods described in the cited documents above are tabular crystals with an average particle diameter of 100 to several hundreds of μm, and have low solubility in water and low oral absorbability. In addition, the crystal of compound (I) does not have stable perf...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D495/04A61K31/381A61P13/02
CPCC07D495/04A61P13/00A61P13/02A61P13/10A61P7/12
Inventor 井泽直人佐藤纪惠八木信宏大内和枝成田正一青木登
Owner KYOWA HAKKO KIRIN CO LTD
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