Olaparib amorphous compound, and preparation method thereof

A technology of amorphous substances and powders, applied in the direction of organic chemistry, can solve the problems of inability to guarantee drug dissolution stability, low bioavailability, unfavorable absorption, etc., achieve significant industrial application value, easy to achieve large-scale, and solvent residues Reduced effect

Active Publication Date: 2017-05-24
SHANGHAI BIOBOND PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

Existing studies have shown that: olaparib is a drug with low solubility and low bioavailability, and the existing crystal forms all have the disadvantages of poor solubility and unf...

Method used

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  • Olaparib amorphous compound, and preparation method thereof
  • Olaparib amorphous compound, and preparation method thereof
  • Olaparib amorphous compound, and preparation method thereof

Examples

Experimental program
Comparison scheme
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Embodiment 1

[0035] Embodiment 1: Preparation of Olaparib Amorphous Form

Embodiment 11

[0037] Under the protection of inert gas, directly heat the raw material of olaparib until it is completely melted; then transfer the molten material to a clean metal container whose temperature is room temperature or pre-cooled to lower than room temperature, so that the material can be rapidly cooled into a solid; The resulting solid was pulverized.

[0038] The obtained powder was taken for X-ray powder diffraction analysis and DSC analysis.

[0039] figure 1 For the XRD spectrum of the obtained powder, by figure 1 It can be seen that the obtained powder is amorphous olaparib, with a broad peak between 12.0 and 40.0 degrees in 2θ and a shoulder peak between 5.0 and 15.0 degrees in 2θ.

[0040] figure 2 For the DSC spectrum of the obtained powder, by figure 2 It can be seen that the obtained powder undergoes exothermic transformation at about 210.6°C.

Embodiment 12

[0042] Under the protection of an inert gas, directly heat the raw material of olaparib until it is completely melted; then pour the molten material into a stirred ice-water mixture to rapidly cool the material into shape; filter, collect the solid powder, and vacuum-dry at 55°C .

[0043] Through X-ray powder diffraction analysis and DSC analysis, the obtained powder is the described amorphous olaparib.

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Abstract

The invention discloses an olaparib amorphous compound, and a preparation method thereof. The x-ray powder diffraction pattern of the olaparib amorphous compound is represented by formula 1. The preparation method comprises following steps: olaparib raw material is heated directly under insert gas protection until complete fusion is realized; an obtained molten product is delivered into a clean metal container, or added into stirred ice-water mixture, or is cooled to room temperature in 2 to 3h directly so as to obtain the olaparib amorphous compound, wherein the temperature in the clean metal container is controlled to be room temperature, or the clean metal container is subjected to precooling until the temperature is lower than room temperature. The olaparib amorphous compound is high in solubility and stability; solvent residue amount is extremely low; the olaparib amorphous compound possesses significant importance in preparation, storage, and applications of subsequent preparations; the preparation method is simple; yield is high; quality is stable; production period is short; and large-scale production is convenient to realize.

Description

technical field [0001] The invention relates to an amorphous form of olaparib and a preparation method thereof, belonging to the technical field of medicinal chemistry. Background technique [0002] Olaparib (Olaparib), chemical name: 1-(cyclopropylformyl)-4-[5-[(3,4-dihydro-4-oxo-1-phthalazinyl)methyl]- 2-fluorobenzoyl] piperazine, its chemical structure is as shown in formula (I): [0003] [0004] The drug was created by the British biotechnology pharmaceutical company (KuDOS Pharmaceuticals), and continued to be developed after being acquired by the US company AstraZeneca, and has successively obtained priority review qualifications from the European Medicines Agency (EMA) and the US Food and Drug Administration (FDA) , which were approved for marketing in Europe and the United States on December 18, 2014 and December 19, 2014, respectively. Product name Lynparza TM , for the treatment of women with advanced ovarian cancer associated with a defect in the ovarian ca...

Claims

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Application Information

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IPC IPC(8): C07D237/32
CPCC07D237/32
Inventor 刘振德高河勇
Owner SHANGHAI BIOBOND PHARMA
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