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Olaparib and maleic acid cocrystal and preparation method thereof

A technology of maleic acid and solvents, which is applied in the field of medicinal chemistry, can solve the problems of low solubility, failure to obtain the co-crystal form A of olaparib and urea, and limit the oral absorption efficiency of drugs, and achieve good reproducibility , The crystallization process is easy to control, and the effect of improving oral absorption efficiency

Active Publication Date: 2020-09-22
TIANJIN UNIVERSITY OF TECHNOLOGY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Olaparib is currently listed as crystal form A, which has low solubility, which limits the oral absorption efficiency of the drug
Patent CN 105753789B discloses the eutectic crystal form A of olaparib and urea, but the inventor of the present invention repeated the preparation method of the example of patent 105753789B, and failed to obtain the cocrystal of olaparib and urea described in the patent Form A

Method used

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  • Olaparib and maleic acid cocrystal and preparation method thereof
  • Olaparib and maleic acid cocrystal and preparation method thereof
  • Olaparib and maleic acid cocrystal and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0038] Weigh 900 mg of olaparib and 240 mg of maleic acid, add 15 mL of n-heptane and 250 μL of ethanol to obtain a suspension, stir the suspension at room temperature for 3 h, filter, and dry the obtained white solid at 40 ° C to obtain Olaparib A solid sample of the co-crystal of lapani and maleic acid with a yield of 93.0%.

Embodiment 2

[0040] Weigh 60 mg of olaparib and 16 mg of maleic acid, add 1 mL of anisole and 10 μL of ethanol to obtain a suspension, stir the suspension at room temperature for 12 h, filter, and dry the obtained white solid at 40 ° C to obtain Olaparib Solid sample of the co-crystal of lapani and maleic acid.

Embodiment 3

[0042] Weigh 60 mg of olaparib and 16 mg of maleic acid, add them to a ball mill jar, then add 10 μL of ethanol, grind at a frequency of 20 Hz for 30 min, and dry the resulting white solid at 40 ° C to obtain a cocrystal of olaparib and maleic acid. solid sample.

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Abstract

The invention discloses an olaparib and maleic acid cocrystal and a preparation method thereof. The molar ratio of olaparib to maleic acid in the cocrystal is 1:1, and an X-ray powder diffraction pattern of the cocrystal has characteristic peaks when the 2theta values are 5.1+ / -0.2 degrees, 9.8+ / -0.2 degrees, 13.7+ / -0.2 degrees, 16.0+ / -0.2 degrees, 17.7+ / -0.2 degrees and 20.0+ / -0.2 degrees. The cocrystal preparation method provided by the invention is simple in process, easy to control the crystallization process, good in reproducibility and suitable for industrial production. Compared with olaparib free alkali, the cocrystal has higher apparent solubility, and is beneficial to improving the oral absorption efficiency of olaparib.

Description

technical field [0001] The invention relates to the technical field of medicinal chemistry, in particular to a co-crystal of olaparib and maleic acid and a preparation method thereof. Background technique [0002] Pharmaceutical active ingredients usually exist in crystalline forms, such as polymorphs, hydrates, solvates, salts, and co-crystals. For the same pharmaceutical active ingredient, different crystalline forms have different physical and chemical properties. Therefore, obtaining a suitable crystalline form of a drug is of great importance in the pharmaceutical industry. The drug exists in the form of co-crystal, which can improve the stability, solubility and processability of the active ingredient of the drug, which has significant advantages. Therefore, pharmaceutical co-crystals are an effective means to improve the physicochemical properties of pharmaceutical active ingredients. [0003] The chemical name of Olaparib is 1-(cyclopropylformyl)-4-[5-[(3,4-dihydr...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D237/32A61K31/502C07C57/145C07C51/43A61P35/00
CPCA61P35/00C07B2200/13C07C57/145C07D237/32
Inventor 陈嘉媚吕文婷戴霞林
Owner TIANJIN UNIVERSITY OF TECHNOLOGY
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