Polymorphs of abiraterone acetate and preparation method thereof

A technology of abiraterone acetate and abiraterone acetate, which is applied to the polymorphic form of abiraterone acetate and its preparation field, can solve the problem of different binding force of crystal particles, influence on drug dissolution rate, influence on drug fluidity and pressure. Issues such as tablet hardness, tablet weight variation, content uniformity, and physical stability
CN101768199AInactive Publication Date: 2010-07-07深圳万乐药业有限公司

Patent Information

Authority / Receiving Office
CN · China
Patent Type
Applications(China)
Current Assignee / Owner
深圳万乐药业有限公司
Publication Date
2010-07-07
Estimated Expiration
Not applicable · inactive patent

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Abstract

The invention discloses polymorphs A, B, C and D of abiraterone acetate. A preparation method of the polymorphs comprises the step of re-crystallizing the abiraterone acetate subjected to the separation and the purification of a chromatographic column in different solvents. Through stable investigation, four polymorphs have favorable stability and flowability, can be used as raw materials for storage and transportation and are suitably applied to antitumor medicinal preparations.
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Description

technical field

[0001] The invention relates to polymorphic forms of pharmaceutical compounds, in particular to polymorphic forms of abiraterone acetate and a preparation method thereof. Background technique

[0002] Abiraterone is an oral inhibitor of cytochrome oxidase P450 (CYP450) c17, which reduces androgen levels by inhibiting the key enzyme in androgen synthesis - CYP450c17, and has effects on androgen in the testis and other parts of the body Inhibition, for the treatment of advanced prostate cancer. Abiraterone acetate is the prodrug of Abiraterone, also known as Abiraterone-3-acetate, its structural formula is:

[0003]

[0004] The synthesis method of the compound is disclosed in WO-A-95 / 09178, but the crystal form of the compound is not involved, and there is no other document reporting the crystal form of abiraterone. It is known that the polymorphic form of a drug is of great significance to the physical and chemical properties of the drug, bioavailability...

Claims

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