Olaparib-urea eutectic crystal and preparation method thereof

A technology of urea and solvent, which is applied in the field of medicinal chemistry, can solve the problems of limiting the oral absorption efficiency of drugs, low solubility, failure to obtain the co-crystal form A of olaparib and urea, etc., and achieves easy control of the crystallization process and heavy weight. The effect of good presentability and high apparent solubility

Active Publication Date: 2020-11-27
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 CN105753789B discloses a eutectic form A of olaparib and urea with a molar ratio of 1:1. However, the inventor of the present invention failed to obtain the olaparib described in the patent according to the preparation method in the example of patent 105753789B. Eutectic form A of pani with urea

Method used

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  • Olaparib-urea eutectic crystal and preparation method thereof
  • Olaparib-urea eutectic crystal and preparation method thereof
  • Olaparib-urea eutectic crystal and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0038] Weigh 1000 mg of olaparib and 276 mg of urea, add 15 mL of ethyl acetate to obtain a suspension, stir the suspension at room temperature for 1 h, filter, and dry the obtained white solid at 40 ° C to obtain olaparib and urea Eutectic solid sample in 84% yield.

Embodiment 2

[0040] Weigh 60 mg of olaparib and 16.5 mg of urea, add 1 mL of isopropyl acetate to obtain a suspension, stir the suspension at room temperature for 12 hours, filter, and dry the obtained white solid at 40°C to obtain olaparib Solid sample co-crystallized with urea.

Embodiment 3

[0042] Weigh 60 mg of olaparib and 16.5 mg of urea, add them to a ball mill jar, then add 20 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 solid sample of eutectic olaparib and urea.

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Abstract

The invention discloses an olaparib-urea eutectic crystal and a preparation method thereof. In the eutectic crystal, a molar ratio of olaparib to urea is 1: 2; in an X-ray powder diffraction pattern of the eutectic crystal, characteristic peaks occur when the value of 2theta is 6.4 + / - 0.2 degrees, 14.3 + / - 0.2 degrees, 15.0 + / - 0.2 degrees, 18.6 + / - 0.2 degrees, 19.2 + / - 0.2 degrees, 24.3 + / -0.2degrees and 24.8 + / -0.2 degrees. The preparation method of the eutectic crystal provided by the invention is simple in process, a crystallization process is easy to control, good in reproducibility and suitable for industrial production. Compared with olaparib free alkali, the eutectic crystal 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 urea 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-dihydro-4-oxo...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D237/32C07C275/02C07C273/16A61K31/502A61P35/00
CPCA61P35/00C07B2200/13C07C275/02C07D237/32
Inventor 陈嘉媚廖政郭肖杨吕文婷
Owner TIANJIN UNIVERSITY OF TECHNOLOGY
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