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Temozolomide and hesperetin cocrystal and preparation method thereof

A technology of temozolomide and hesperetin, which is applied in the field of medicinal chemistry and achieves the effects of good reproducibility, broad application prospects and simple process

Pending 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

At present, there is no relevant report on the co-crystal of the two active ingredients of temozolomide and hesperetin

Method used

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  • Temozolomide and hesperetin cocrystal and preparation method thereof
  • Temozolomide and hesperetin cocrystal and preparation method thereof
  • Temozolomide and hesperetin cocrystal and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0052] Weigh 1.94g temozolomide and 3.02g hesperetin, add 50mL of 80% ethanol to obtain a suspension, stir the suspension at room temperature for 1h, filter, and dry the obtained pale yellow solid at 40°C to obtain temozolomide and hesperetin Eutectic solid sample in 94% yield.

Embodiment 2

[0054] Weigh 19.4 mg temozolomide and 30.2 mg hesperetin, add 1 mL of acetone to obtain a suspension, stir the suspension at room temperature for 12 hours, filter, and dry the obtained pale yellow solid at 40°C to obtain temozolomide and hesperetin Eutectic solid samples.

Embodiment 3

[0056] Weigh 19.4 mg of temozolomide and 30.2 mg of hesperetin, 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 obtained pale yellow solid at 40 ° C to obtain a solid sample of temozolomide and hesperetin cocrystal.

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Abstract

The invention discloses a temozolomide and hesperetin cocrystal and a preparation method thereof. The molar ratio of temozolomide to hesperetin in the cocrystal is 1:1, and an X-ray powder diffractionpattern of the cocrystal has characteristic peaks when the 2theta values are 11.9+ / -0.2 degrees, 25.3+ / -0.2 degrees, 26.8+ / -0.2 degrees and 27.1+ / -0.2 degrees. The cocrystal preparation method provided by the invention is simple in process, the crystallization process is easy to control, the reproducibility is good, and the method is suitable for industrial production. The cocrystal can effectively improve the stability and tabletting property of temozolomide, improve the solubility of hesperetin and slow down the dissolution of temozolomide, and provides a research basis for treatment of cancer by combining temozolomide and hesperetin.

Description

technical field [0001] The invention relates to the technical field of medicinal chemistry, in particular to a co-crystal of temozolomide and hesperetin and a preparation method thereof. Background technique [0002] Drug co-crystallization refers to the combination of drug molecules and other physiologically acceptable acids, bases, salts and non-ionic compound molecules in the same crystal lattice through non-covalent bonds such as hydrogen bonds, π-π stacking effects, and van der Waals forces. crystals. On the premise of not destroying the covalent bonds of the drug, the formation of co-crystals can change the physicochemical properties of the drug, including stability, solubility, and tabletability. In addition, after the formation of co-crystals, the pharmacokinetic parameters of some drugs can also be changed, such as C max (peak plasma concentration), T max (peak time), t 1 / 2 (elimination half-life) and AUC (area under the plasma concentration-time curve) and so o...

Claims

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Application Information

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IPC IPC(8): C07D487/04A61K31/4188C07D311/32A61K31/352A61P35/00
CPCC07D487/04C07D311/32A61P35/00C07B2200/13
Inventor 陈嘉媚王洁戴霞林
Owner TIANJIN UNIVERSITY OF TECHNOLOGY
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