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Crystalline form I of Olaparib and preparation method therefor

A crystal form, powder diffraction pattern technology, applied in the direction of medical preparations, pharmaceutical formulations, organic active ingredients containing active ingredients, etc., can solve the difference in clinical efficacy, solubility and stability, affecting drug absorption and bioavailability. and other problems, to achieve the effect of non-toxic solvent, environmental protection and simple process

Inactive Publication Date: 2016-03-30
CRYSTAL PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] Different crystal forms of solid chemical drugs can cause different solubility and stability, which will affect the absorption and bioavailability of drugs, and will lead to differences in clinical efficacy

Method used

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  • Crystalline form I of Olaparib and preparation method therefor
  • Crystalline form I of Olaparib and preparation method therefor
  • Crystalline form I of Olaparib and preparation method therefor

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0047] The preparation method of olaparib crystal form I:

[0048] Dissolve 10.0 mg of olaparib free base in 1.0 mL of pure water, stir at room temperature for 7 days, filter with suction, dry, and collect the solid. After testing, the crystal form prepared in this example is crystal form I.

[0049] Table 1 shows the X-ray powder diffraction data of the crystal forms obtained in this example. Its XRPD pattern is as follows figure 1 , and its DSC graph is shown in figure 2 , and its TGA figure is shown in image 3 .

[0050] Table 1

[0051] 2theta

[0052] 30.41

Embodiment 2

[0054] The preparation method of olaparib crystal form I:

[0055] Add 10.0 mg of olaparib crystal form A in patent CN101528714B to 0.5 mL of pure water, then add 1.0 mg of crystal form I seed crystals, stir at room temperature for 72 hours, filter with suction, wash with pure water, and dry. The solid was collected, and it was detected that the crystalline form prepared in this example was crystalline form I.

[0056] Table 2 shows the X-ray powder diffraction data of Form I obtained in this example.

[0057] Table 2

[0058] 2theta

[0059] 26.13

Embodiment 3

[0061] Stability comparative test of olaparib crystal form I and crystal form A in patent CN101528714B:

[0062] Take 10.0 mg of the crystal form A in patent CN101528714B and 1.0 mg of the crystal form I prepared in Example 1 in a vial, add 0.5 mL of pure water to make a suspension. After stirring at room temperature for 72 hours, the XRPD of the test sample showed that the crystal form A in the patent CN101528714B had been completely transformed into the crystal form I in the present invention, and the results are shown in Table 3.

[0063] table 3

[0064]

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PUM

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Abstract

The present invention relates to a crystalline form I of Olaparib and a preparation method therefor. The present invention particularly provides a crystalline form I. The crystalline form I is characterized in that the X-ray powder diffraction pattern of the crystalline form I has characteristic peaks when the 2 theta value is 6.4 degrees + / - 0.2 degree, 12.7 degrees + / - 0.2 degree and 15.1 degrees + / - 0.2 degree. The crystalline form I provided by the present invention is better in stability, and has important values for optimization and development of the drug in the future.

Description

technical field [0001] The invention relates to the field of chemistry and medicine, in particular to the crystal form I of olaparib and a preparation method thereof. Background technique [0002] Olapani was first developed by the British biotechnology company KuDOS (Kudos) Pharmaceutical Co., Ltd. After being acquired by AstraZeneca, it continued to develop a drug for the treatment of ovarian cancer. On December 19, 2014, Olaparib was approved by the FDA for marketing in the United States. It is the first targeted drug approved by the FDA for ovarian cancer patients with BRCA mutations, and is suitable for patients who have previously undergone chemotherapy. It has been demonstrated in preclinical models that olaparib is a first-in-class oral poly ADP ribose polymerase (PARP) inhibitor that exploits defects in the DNA repair pathway to preferentially kill cancer cells. [0003] The chemical name of olaparib is 4-[3-(4-cyclopropanecarbonyl-piperazine-1-carbonyl)-4-fluoro-b...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D237/32A61K31/502A61P35/00
CPCC07D237/32
Inventor 陈敏华张炎锋刘凯邹坡张晓宇
Owner CRYSTAL PHARMA CO LTD
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