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Abiraterone acetate crystal form and preparation method thereof

A technology of abiraterone acetate and crystal form, applied to a new crystal form of the prostate cancer treatment drug abiraterone acetate and its preparation, the pharmaceutical composition of the new crystal form, the application field in the treatment of prostate cancer, can solve the problem of Unable to inhibit androgen and other problems, to achieve good stability and activity, good preparation adaptability, suitable for long-term storage effect

Inactive Publication Date: 2012-01-18
CHONGQING PHARMA RES INST
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  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0007] Androgens can promote the growth of prostate cancer cells. At present, castration therapy, including drugs and surgery, is generally the first choice for patients with advanced prostate cancer to reduce the production of androgens in the testes, but this treatment cannot inhibit the production of androgens in other parts of the body

Method used

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  • Abiraterone acetate crystal form and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0069] Preparation of Abiraterone Acetate Form E

[0070] In a 100ml reaction bottle, add 10g of abiraterone acetate and 50ml of acetonitrile, heat up to reflux to dissolve completely, cool to below 10°C to crystallize at a stirring speed of 140~150 rpm, filter, and depressurize the obtained solid Dry to obtain the crystal form E of abiraterone acetate. The measured X-ray powder diffraction pattern is shown in figure 1 , the measured values ​​are as follows (take peaks whose relative intensity is greater than or equal to 7%),

[0071] d value 2θ value Relative Strength(%) 15.12 5.8° 31 9.28 9.5° 7 7.31 12.1° 48 7.01 12.6° 7 5.95 14.9° 66 5.84 15.2° 62 5.54 16.0° 50 5.13 17.3° 17 4.81 18.4° 100 4.66 19.0° 65 4.48 19.8° 21 4.07 21.8° 46 3.95 22.5° 30 3.85 23.1° 40 3.78 23.5° 10 3.65 24.4° 10 3.50 25.5° 14 3.42 26.0° 7 3.31 26.9° 8 3.23 27.6° 23 ...

Embodiment 2

[0073] Preparation of Abiraterone Acetate Form E

[0074] In a 500ml reaction bottle, add 5g of abiraterone acetate and 80ml of methanol, dissolve the product completely at 30~35°C, add 160ml of water at a stirring speed of 50~60 rpm, crystallize, filter, and obtain a solid Dry under reduced pressure to obtain the crystal form E of abiraterone acetate.

[0075]

Embodiment 3

[0077] Preparation of Abiraterone Acetate Form E

[0078] In a 100ml reaction bottle, add 10g of abiraterone acetate and 50ml of ethanol, heat up to reflux to dissolve the product completely, cool to below 0°C to crystallize at a stirring speed of 190~250 rpm, and filter to obtain abiraterone acetate Dragonglass Form E.

[0079]

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Abstract

The invention relates to a new crystal form of a medicament, namely abiraterone acetate for treating prostatic cancer and a preparation method thereof, a pharmaceutical composition containing the new crystal form, and application of the new crystal form in preparing medicines for treating prostatic cancer.

Description

[0001] technical field [0002] The present invention relates to the fields of organic chemistry and pharmacy, in particular to a new crystal form of abiraterone acetate, a drug for treating prostate cancer, and a preparation method thereof, as well as a pharmaceutical composition of the new crystal form and its application in the treatment of prostate cancer . Background technique [0003] Abiraterone acetate, chemical name: (3β)-17-(3-pyridyl)-androst-5,16-dien-3-ol acetate, the structure is shown in formula I, [0004] . [0005] [0006] Abiraterone acetate can be converted into abiraterone in the body. Abiraterone is a cytochrome oxidase P450 (CYP450)c17 inhibitor, which reduces androgen levels by inhibiting the key enzyme in androgen synthesis-CYP450c17, so , Abiraterone not only inhibits the androgen produced by the testes but also other parts of the body such as the adrenal gland. [0007] Androgens can promote the growth of prostate cancer cells. At present, c...

Claims

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Application Information

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IPC IPC(8): C07J43/00A61K31/58A61P35/00
Inventor 刑乃果石瑞那郑德平邓杰罗杰叶文润
Owner CHONGQING PHARMA RES INST
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