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Dasatinib tablet

A technology of nylon tablets and organic solvents, applied in the field of pharmaceutical preparations, can solve problems such as adverse reactions, shortened time to maintain drug efficacy, unqualified dissolution rate, etc., and achieve the effect of simple process, low cost, and consistent quality

Active Publication Date: 2012-05-02
SHANGHAI ACEBRIGHT PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

For dasatinib, the saturation solubility of the anhydrous substance in water is larger than that of the monohydrate substance (anhydrous substance 3.25mg / ml; monohydrate substance 1.02mg / ml), which may easily lead to dissolution of tablets prepared from the anhydrous substance If the rate is too fast, adverse reactions caused by sudden release of the drug will occur, the time to maintain the drug effect will be shortened, and problems such as unqualified dissolution rate will easily occur.
Therefore, what existing dasatinib tablet all adopted is dasatinib monohydrate as raw material, how to adopt dasatinib anhydrous as raw material to prepare qualified dasatinib tablet, has not seen yet relevant reports

Method used

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Examples

Experimental program
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Effect test

Embodiment 1

[0035] Add 10 g of anhydrous dasatinib and 300 ml of absolute ethanol to a 500 ml four-necked flask equipped with a mechanical stirrer, a condenser and a thermometer to obtain a slurry; heat to reflux to 75 ° C to obtain a clear solution; then, slowly dissolve the solution Cool down to 60°C to obtain a suspension; then slowly cool down to room temperature for 10 hours, filter, and dry the obtained solid at 50°C to obtain 8.9g of a dry product. The particle size is: D (0.1) = 3 μm, D(0.5) = 20 μm, D(0.9) = 130 μm.

Embodiment 2

[0037] Add 20 g of anhydrous dasatinib and 700 ml of acetone to a 1000 ml four-neck flask equipped with a mechanical stirrer, a condenser and a thermometer to obtain a slurry; heat and reflux to 56 ° C to obtain a clear solution; then, slowly cool the solution to 48°C to obtain a suspension, then slowly cool down to room temperature for 5 hours, filter, and dry the obtained solid at 50°C to obtain 18.5g of a dry product. The particle size is: D(0.1)=4μm , D(0.5)=50 μm, D(0.9)=150 μm.

Embodiment 3

[0039] Add 10 g of anhydrous dasatinib and 300 ml of ethyl acetate into a 500 ml four-necked flask equipped with a mechanical stirrer, a condenser and a thermometer to obtain a slurry; heat to reflux to 78 ° C to obtain a clear solution; then, the solution is slowly Cool down to 65°C to obtain a suspension; then slowly cool down to room temperature for 15 hours, filter, and dry the obtained solid at 50°C to obtain 9.0 g of a dry product. The particle size is: D (0.1) = 3.5 μm, D(0.5) = 60 μm, D(0.9) = 100 μm.

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Abstract

The invention discloses a dasatinib tablet, which comprises dasatinib and pharmaceutically-acceptable medicinal auxiliary materials, and is characterized in that: the dasatinib is an anhydride of which the particle size D(0.1) is equal to 3.0-10 mum, D(0.5) is equal to 15-60 mum and D(0.9) is equal to 100-150 mum. A qualified dasatinib tablet is prepared by taking the dasatinib anhydride as a raw material, so that the problems of over-high dissolution rate of a tablet prepared from the anhydride, untoward reactions caused by initial burst release of a medicament, reduction in the acting time, easy occurrence of unqualified dissolution rate and the like, which are caused by relatively high water saturation solubility of the dasatinib anhydride, are solved, and the industrial batch production requirements of low cost, simple process and qualification on a dasatinib raw material and a preparation can be met.

Description

technical field [0001] The invention relates to a dasatinib tablet, which belongs to the technical field of pharmaceutical preparations. Background technique [0002] Dasatinib (Dasatinib / Sprycel), molecular formula C 22 h 26 ClN 7 o 2 S.H 2 O, molecular weight 506.02, used for all disease stages of chronic myelogenous leukemia (chronic phase, accelerated phase, lymphoid cell blast phase and myeloid blast phase) in adult patients. Among the approved drugs, Sprycel is the first oral chemotherapy drug capable of inhibiting multiple configurations of tyrosine protein kinase Abl. At nanomolar concentration, the drug can inhibit Bcr-Abl, SRC kinase family (SRC, LCK, YES, FYN), c-KIT, EPHA2 and PDGFR-B and other kinases. By inhibiting the action of the aforementioned kinases, Sprycel inhibits the proliferation of leukemia cells in the bone marrow of CML and Ph+ALL. It has the advantages of long-lasting curative effect and high safety, and has been approved for use in most ...

Claims

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Application Information

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IPC IPC(8): A61K9/20A61K31/506A61P35/02
Inventor 安晓霞张静张春雨马素伟
Owner SHANGHAI ACEBRIGHT PHARMA CO LTD
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