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

A technology of polymorphs and dasatinib, applied in the field of polymorphs of dasatinib, preparation methods of polymorphs and pharmaceutical compositions thereof, can solve problems such as reduction

Active Publication Date: 2011-06-08
NANJING CAVENDISH BIO ENG TECH +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0010] 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 medicinal composition thereof
  • Dasatinib polymorphic substance as well as preparation method and medicinal composition thereof
  • Dasatinib polymorphic substance as well as preparation method and medicinal composition thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0095] Add 16 g of Dasatinib and 160 ml of purified water into the reaction flask, heat up to reflux with stirring, cultivate the crystals for 3 hours, and then naturally lower to room temperature and filter with suction. The filter cake is rinsed with an appropriate amount of water and drained. The filter cake was dried under reduced pressure (-0.095MPa) at about 50°C, and dried with phosphorus pentoxide. 15.4 g of white solid was obtained. Yield: 96.3%.

[0096]

Embodiment 2

[0098] Add 10 g of Dasatinib and 90 ml of purified water into the reaction flask, heat up to reflux with stirring, cultivate the crystals for 4 hours, reduce to room temperature, and filter with suction. The filter cake is rinsed with an appropriate amount of water and drained. The filter cake was dried under reduced pressure (-0.095MPa) at about 50°C, and dried with phosphorus pentoxide. 9.8 g of white solid was obtained. Yield: 98.0%.

[0099]

Embodiment 3

[0101] The prescription and preparation process of Dasatinib capsules:

[0102] The polymorph III of dasatinib was prepared into a capsule preparation containing 50 mg with several excipients according to the following method.

[0103]

[0104] The manufacturing method of capsules containing dasatinib polymorph III is to add the first four of the above excipients and dasatinib polymorph III with water to prepare a soft material, and the soft material is made into a wet material. After the granules are dried, the dried granules are uniformly mixed with magnesium stearate and then filled into the capsule shell to obtain dasatinib capsules.

[0105] Dissolution curve:

[0106] Capsule formula 1

[0107] time

[0108] See the dissolution profile of capsule formula 1 Figure 5 .

[0109] Capsule formula 2

[0110] time

[0111] See the dissolution profile of capsule formula 2 Image 6 .

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Abstract

The invention discloses a dasatinib polymorphic substance. In addition, the invention also discloses a preparation method and a medicinal composition of the dasatinib polymorphic substance. The dasatinib polymorphic substance provided by the invention has the advantages of good physicochemical property and good stability, is more suitable for industrial scale preparation, and the like.

Description

Technical field [0001] The present invention relates to a polymorph of a pharmaceutical compound, more specifically, to a polymorph of dasatinib. In addition, the present invention also relates to a preparation method of the polymorph and a pharmaceutical composition thereof. Background technique [0002] Dasatinib, trade name SPRYCEL TM , Is an oral tyrosine kinase inhibitor developed by BMS, used in adult chronic myeloid leukemia (CML), and can also be used to treat 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- Pyrimidyl]amino]-5-thiazolecarboxamide, the chemical structure is as follows: [0003] [0004] Bristol-Myers Squibb Company recorded and disclosed five crystalline forms of dasatinib in the Chinese patent application-application number CN200580011916.6 (publication date is June 13, 2007) The preparation method of the corresponding cry...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D417/12A61K31/506A61P37/06A61P19/04A61P29/00A61P25/00A61P1/00A61P17/06A61P35/02A61P35/00A61P37/08A61P11/06A61P9/10A61P11/00
Inventor 严荣杨浩许永翔
Owner NANJING CAVENDISH BIO ENG TECH
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