Abiraterone acetate nanocrystal as well as preparation and preparation method thereof

A technology of abiraterone acetate and nanocrystals, which is applied in the directions of non-active ingredient medical preparations, medical preparations containing active ingredients, and pill delivery, etc., can solve the problems of increased absorption and low bioavailability, and achieve increased absorption. , The effect of reducing drug cost, improving solubility and dissolution rate
CN112933053AActive Publication Date: 2021-06-11CHINA PHARM UNIV
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Patent Information

Authority / Receiving Office
CN · China
Patent Type
Applications(China)
Current Assignee / Owner
CHINA PHARM UNIV
Publication Date
2021-06-11

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Abstract

The invention belongs to the field of pharmaceutical preparations, and provides an abiraterone acetate nanocrystal as well as a preparation and a preparation method thereof. The preparation process of the abiraterone acetate nanocrystal comprises the following steps of: weighing an abiraterone acetate raw material medicine and a stabilizer in proportion; adding a proper amount of water, carrying out ultrasonic mixing uniformly; carrying out high-speed shearing on a solution; taking a lower-layer primary suspension; adding zirconium oxide grinding beads and stirrers, and carrying out medium grinding to obtain the abiraterone acetate nanocrystal. A freeze-drying protective agent can be added into the abiraterone acetate nanocrystal, and vacuum drying is carried out to obtain the abiraterone acetate nanocrystal freeze-dried powder. According to the abiraterone acetate nanocrystal as well as the preparation and preparation method thereof of the present invention, the solubility and the dissolution rate of the BCSIV drug abiraterone acetate are improved by using the nanocrystal technology; and the BCSIV drug abiraterone acetate can be prepared into the freeze-dried powder or tablets, such that the absorption of the BCSIV drug abiraterone acetate is increased, the problem of low bioavailability of the BCSIV drug abiraterone acetate is solved,and the drug cost is reduced.
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Description

technical field

[0001] The invention relates to the field of pharmaceutical preparations, in particular to a nanocrystal of abiraterone acetate, a preparation and a preparation method thereof. Background technique

[0002] Abiraterone acetate is a 3-acetyl analog of abiraterone, a prodrug of abiraterone, an orally effective CPY17 inhibitor that can comprehensively block androgen synthesis in testicular, adrenal, and prostate cancer cells , can cut off the fuel supply of tumor androgen, so as to kill prostate cancer cells. The drug was first approved by the US FDA on April 28, 2011, for the treatment of castration-resistant metastatic prostate cancer (mCRPC) in combination with prednisone or prednisolone.

[0003] Abiraterone acetate is a lipophilic compound belonging to the BCSIV class of drugs. Due to its low solubility and low permeability properties, it affects the absorption in the body and reduces the bioavailability. Therefore, it is necessary to take appropriate me...

Claims

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