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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

Active Publication Date: 2021-06-11
CHINA PHARM UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] Aiming at the problems existing in the prior art, the present invention improves the solubility and the dissolution rate of the BCSIV drug abiraterone acetate by adopting nanocrystal technology, and prepares it into freeze-dried powder or tablet, thereby increasing its absorption and solving its relatively low bioavailability. It also reduces the cost of drugs and provides experimental basic data for the further development of nanocrystal preparations of other poorly soluble drugs

Method used

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  • Abiraterone acetate nanocrystal as well as preparation and preparation method thereof
  • Abiraterone acetate nanocrystal as well as preparation and preparation method thereof
  • Abiraterone acetate nanocrystal as well as preparation and preparation method thereof

Examples

Experimental program
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Effect test

Embodiment 1

[0029] Embodiment 1 screens the kind of stabilizer

[0030] Preparation method: First, weigh the abiraterone acetate raw material and stabilizer at a ratio of 5:1, add appropriate amount of water, and ultrasonically mix the solution evenly, then perform high-speed shearing on the solution, remove the initial suspension of the lower layer, add zirconia grinding beads and A stir bar was used to obtain nanocrystals of abiraterone acetate after media grinding. The obtained nanocrystals were mixed uniformly with a lyoprotectant (sucrose and mannitol in a weight ratio of 1:1, and the total dosage was 10% w / v), and then vacuum-dried for 48 hours to obtain a lyophilized powder of abiraterone acetate nanocrystal preparation.

[0031] Sodium dodecyl sulfate (SDS), hydroxypropyl methylcellulose (HPMC), poloxamer 188 (P188), poloxamer 407 (P407), polyvinylpyrrolidone K30 (PVP K30) and spit Temperature 80 (Tween 80) six stabilizers. Through detection, it is found that the nanocrystal con...

Embodiment 2

[0032] The screening of the ratio of embodiment 2 medicines and stabilizer

[0033] Adjust the weight ratio of abiraterone acetate bulk drug and stabilizer (select poloxamer 407 or poloxamer 188), and other preparation methods are the same as in Example 1.

[0034] Screened abiraterone acetate bulk drug: three weight ratios of stabilizer P407=3:1, 4:1, 5:1, and abiraterone acetate bulk drug: stabilizer P188=3:1, 4:1, 5:1 three weight ratios, it is found that different stabilizers are prepared according to the ratio of 5:1, the particle size of the preparation is smaller and the stability is the best.

Embodiment 3

[0035] Embodiment 3 is to the screening of each stabilizer ratio of compound stabilizer

[0036] According to the screening of stabilizers in Example 1, two stabilizers, Poloxamer 407 and Poloxamer 188, were considered for compounding. A total of four ratios of P407:P188=7:1, 1:1, 3:5, and 1:3 were screened, and it was found that the formulation of 7:1 had a smaller particle size and the best stability. The preparation method is the same as in Example 1.

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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.

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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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/19A61K31/58A61K47/10A61K47/26A61K9/20A61P35/00
CPCA61K9/19A61K31/58A61K47/10A61K47/26A61K9/2095A61K9/2054A61P35/00
Inventor 沈雁涂家生李钰奇唐宝强何东升
Owner CHINA PHARM UNIV
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