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Dasatinib polymorphic substance as well as preparation method and pharmaceutical composition thereof

A polymorph, dasatinib technology, which can be used in drug combinations, antitumor drugs, pharmaceutical formulations, etc., and can solve the problems of inability to reduce, unfavorable for industrial-scale preparation, and difficult to dissolve.

Inactive Publication Date: 2011-11-23
NANJING CAVENDISH BIO ENG TECH +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0011] Since dasatinib is almost insoluble in water or organic solvents such as methanol, ethanol, propanol, isopropanol, butanol, and pentanol, even if it is dissolved under heating, it needs to use a large amount of solvent that is more than 100 times larger, and the dissolution is very difficult. It is not conducive to industrial scale preparation; in addition, the method taught by the application document CN200580011916.6 cannot effectively reduce the related substances in the product in the crystal form preparation process to improve the quality of the product

Method used

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  • Dasatinib polymorphic substance as well as preparation method and pharmaceutical composition thereof
  • Dasatinib polymorphic substance as well as preparation method and pharmaceutical composition thereof
  • Dasatinib polymorphic substance as well as preparation method and pharmaceutical composition thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0162] Preparation of polymorph I:

[0163] A. Add 10g of dasatinib and 40ml of dimethyl sulfoxide into the reaction bottle, and heat up to 60-70°C under stirring. After the crystals were precipitated, the temperature was lowered to 0° C. to grow the crystals for 10 minutes. Suction filtration, the filter cake was rinsed with water and then with a mixture of water and acetone (1:1) and drained. The filter cake is dried under reduced pressure (-0.095MPa) at about 50°C, and is assisted with phosphorus pentoxide. 7.7 g of white solid were obtained. Yield: 77%.

[0164]

[0165] B. Add 10g of dasatinib and 40ml of dimethyl sulfoxide in the reaction flask, and slowly heat up to 60-70°C under stirring. After dissolving, add 160ml of ethanol:water (1:1) mixed solution under heat preservation, and stir After the crystals were precipitated, the temperature was lowered to 0° C. to grow the crystals for 10 minutes. Suction filtration, and the filter cake was rinsed with a mixture...

Embodiment 2

[0168] Preparation of polymorph II:

[0169] A. Add 10g of dasatinib and 40ml of dimethylformamide into the reaction bottle, heat up to 60-70°C and dissolve under stirring; place the above-mentioned dimethylformamide solution of dasatinib in a closed system environment of acetone In, the volume of acetone is 300ml. Allow acetone to evaporate into the dasatinib in dimethylformamide solution at room temperature to reflux temperature. After several hours or even several days, piled crystals are precipitated in the solution and then left to stand for several hours or even several days. Suction filtration, filter cake rinse with acetone. The filter cake is dried under reduced pressure at about 50°C (-0.095MPa), and is assisted with phosphorus pentoxide. 6.1 g of white solid were obtained. Yield: 61%.

[0170]

[0171] B. Add 10g of dasatinib and 40ml of dimethyl sulfoxide into the reaction bottle, and dissolve it under stirring at 60-70°C; In the system environment, the vo...

Embodiment 3

[0174] The prescription and preparation process of dasatinib capsules:

[0175] The above-mentioned dasatinib polymorph I, II, or the mixture of I and II in any ratio is prepared into a solid preparation containing 50 mg by using several excipients according to the following method.

[0176]

[0177]

[0178] The manufacture method of the capsule containing dasatinib polymorph I, II or the mixture of the above two polymorphs in any ratio is to combine the first four of the above-mentioned excipients with the dasatinib polymorph Compound I, II or the mixture of any proportion of the above two polymorphs are mixed evenly, and a soft material is obtained by adding an appropriate amount of water. The soft material is made into wet granules and then dried. After the dried granules are mixed with magnesium stearate evenly Fill the capsule shell to obtain dasatinib capsules.

[0179] Dissolution profile:

[0180] Capsule Formula 1

[0181] time

[0182] For the di...

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Abstract

The invention discloses a dasatinib polymorphic substance. In addition, the invention also discloses a preparation method and a pharmaceutical composition of the dasatinib polymorphic substance. The dasatinib polymorphic substance disclosed by the invention has the advantages of excellent physical and chemical properties, good stability and the like, and is more suitable for industrial preparation.

Description

[0001] This application is a divisional application of the application number 201019026056.3 and the invention name "dasatinib polymorph and its preparation method and pharmaceutical composition" submitted on February 8, 2010. technical field [0002] The present invention relates to a polymorphic form of a pharmaceutical compound, more specifically, to a polymorphic form of dasatinib. In addition, the present invention also relates to a preparation method of the polymorphic form and a pharmaceutical composition thereof. Background technique [0003] Dasatinib, trade name SPRYCEL TM , is an oral tyrosine kinase inhibitor developed by BMS, which is used for adult chronic myelogenous leukemia (CML), and can also be used for the treatment of Philadelphia chromosome-positive acute lymphoblastic leukemia and other diseases. Its chemical name is N-(2-chloro-6-methylphenyl)-2-[[6-[4-(2-hydroxyethyl)-1-piperazinyl]-2-methyl-4- Pyrimidinyl]amino]-5-thiazolecarboxamide, the chemical ...

Claims

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Application Information

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IPC IPC(8): C07D417/12A61K31/506A61P35/02
Inventor 严荣杨浩许永翔
Owner NANJING CAVENDISH BIO ENG TECH
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