Co-crystal of abiraterone acetate and trans-aconitic acid, and preparation method, pharmaceutical composition and application thereof

A technology of abiraterone acetate and trans-aconitic acid is applied in the directions of drug combination, medical preparations with non-active ingredients, and medical preparations containing active ingredients, etc., to achieve high bioavailability, obvious improvement, and improved solubility Effect

Active Publication Date: 2021-08-03
SHANGHAI INST OF MATERIA MEDICA CHINESE ACAD OF SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0007] So far, US 10045998B2 has reported the co-activity of abiraterone acetate with adipic acid, citric acid, D, L-malic acid, maleic acid, methyl 4-hydroxybenzoate, saccharin, L-tartaric acid, vanillic acid. Crystals and salts, compared with abiraterone acetate itself, have a certain increase in solubility in acidic media, but no pharmacokinetic experiments have been conducted to prove that the existing co-crystals or salts have improved drug absorption

Method used

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  • Co-crystal of abiraterone acetate and trans-aconitic acid, and preparation method, pharmaceutical composition and application thereof
  • Co-crystal of abiraterone acetate and trans-aconitic acid, and preparation method, pharmaceutical composition and application thereof
  • Co-crystal of abiraterone acetate and trans-aconitic acid, and preparation method, pharmaceutical composition and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0053] Abiraterone acetate 0.1mmol and trans-aconitic acid 0.05mmol are added in 4 milliliters of ethanol according to stoichiometric ratio 2:1, after dissolving completely, slowly volatilize at room temperature again, obtain abiraterone acetate and trans-aconitic acid Co-crystal of head acid.

Embodiment 2

[0055] Add 0.1mmol of abiraterone acetate and 0.05mmol of trans aconitic acid into 4 milliliters of methanol according to the stoichiometric ratio of 2:1, after completely dissolving, volatilize slowly at 50 degrees Celsius to obtain abiraterone acetate and trans aconitic acid Co-crystal of aconitic acid.

Embodiment 3

[0057] Abiraterone acetate 0.1mmol and trans-aconitic acid 0.05mmol are added in 4 milliliters of acetone according to stoichiometric ratio 2:1, after dissolving completely, slowly volatilize under the condition of 50 degrees Celsius again, obtain abiraterone acetate and trans-aconitic acid Co-crystal of aconitic acid.

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Abstract

The invention relates to a co-crystal of abiraterone acetate and trans-aconitic acid, a preparation method thereof, a pharmaceutical composition and application of the co-crystal. An X-ray powder diffraction pattern of the eutectic crystal of abiraterone acetate and trans-aconitic acid has characteristic peaks when diffraction angles 2 theta are 6.7 degrees, 7.3 degrees, 7.6 degrees, 13.6 degrees, 14.0 degrees, 15.0 degrees, 17.1 degrees, 17.9 degrees, 18.5 degrees, 19.5 degrees and 24.9 degrees. Compared with abiraterone acetate in the prior art, the eutectic crystal of abiraterone acetate and trans-aconitic acid provided by the invention has the advantage that the drug solubility, dissolution performance, in-vivo drug absorption and the like are remarkably improved.

Description

technical field [0001] The invention relates to the technical fields of medicinal chemistry and crystallization technology, in particular to a co-crystal of abiraterone acetate and trans-aconitic acid, a preparation method thereof, a pharmaceutical composition and an application thereof. Background technique [0002] The chemical name of Abiraterone Acetate is: 17-(3-pyridiny)androsta-5,16-diene-3β-acetate ((3β)-17-(3-pyridiny)androsta-5 ,16-dien-3-ol acetate), its chemical structure is as follows: [0003] [0004] Abiraterone acetate can be converted into abiraterone in the body, and abiraterone is an androgen biosynthesis inhibitor that can inhibit 17α-hydroxylase / C17,20 lyase and reduce androgen in testicular, adrenal and prostate tumor tissues. Hormone production. However, due to its poor water solubility and poor oral absorption, abiraterone acetate greatly limits its clinical application. [0005] Pharmaceutical co-crystal refers to the formation of active pharm...

Claims

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Application Information

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IPC IPC(8): A61K9/14A61K31/58A61K47/12A61P13/08A61P35/00
CPCA61K31/58A61K9/145A61P13/08A61P35/00
Inventor 梅雪锋杨泽恩朱冰清戴文娟王建荣
Owner SHANGHAI INST OF MATERIA MEDICA CHINESE ACAD OF SCI
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