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Eutectic crystal of temozolomide and baicalein as well as preparation method for eutectic crystal

A technology of temozolomide and baicalein, applied in the field of chemical medicine, to achieve the effect of improving oral half-life, simple preparation method, and improving stability

Active Publication Date: 2018-10-09
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 baicalein

Method used

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  • Eutectic crystal of temozolomide and baicalein as well as preparation method for eutectic crystal
  • Eutectic crystal of temozolomide and baicalein as well as preparation method for eutectic crystal
  • Eutectic crystal of temozolomide and baicalein as well as preparation method for eutectic crystal

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0044] Weigh 1.94 g of temozolomide and 2.70 g of baicalein, add them into 150 mL of methanol to obtain a suspension, stir the suspension at room temperature for 21 h, filter, and dry the obtained yellow solid to obtain a solid sample of temozolomide-baicalein cocrystal.

Embodiment 2

[0046] Weigh 19.48 mg of temozolomide and 27.12 mg of baicalein, add 2 mL of distilled water to obtain a suspension, stir the suspension at room temperature for 24 hours, centrifuge to remove the yellow solid in the lower layer, and dry to obtain a solid sample of temozolomide-baicalein cocrystal.

Embodiment 3

[0048] Weigh 19.84 mg of temozolomide and 27.95 mg of baicalein, add 1 mL of methanol and 1 mL of distilled water in a mixed solvent to obtain a suspension, stir the suspension at room temperature for 4 hours, filter, and dry the obtained yellow solid to obtain temozolomide-baicalein co- Crystalline solid samples.

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Abstract

The invention relates to eutectic crystal of temozolomide and baicalein as well as a preparation method for the eutectic crystal. Specifically, an X-ray powder diffraction pattern of the eutectic crystal has characteristic peaks with 2 theta value being 7.7 + / -0.2 degree, 8.6+ / -0.2 degree, and 12.7+ / -0.2 degree. The eutectic crystal provided by the invention has obvious advantages in stability, solubility, pharmacokinetic properties and the like of two pharmaceutical ingredients in comparison with existing temozolomide and baicalein bulk drugs, has an important value in developing drug combination of two drugs.

Description

technical field [0001] The invention relates to the field of chemical medicine, in particular to a co-crystal of temozolomide and baicalein and a preparation method thereof. Background technique [0002] Temozolomide (TMZ) is an alkylating agent antitumor drug containing an imidazole tetrazine ring, and its chemical name is 3,4-dihydro-3-methyl-4-oxoimidazole[5,1-d] And 1,2,3,5-tetrazine-8-carboxamide, its chemical structure is: [0003] [0004] Temozolomide is a prodrug and has no activity itself. It is converted into the active compound MITC (5-(3-methyltriazen-1-yl) imidazole-4-amide) by non-enzymatic pathway at physiological pH level, the latter It is further hydrolyzed into AIC (5-amino-imidazol-4-amide) and methyl diazonium ions, and then methyl diazonium ions act on the O6 and N7 sites on guanine to methylate DNA, making it impossible to combine with thymus Pyrimidine pairing produces cytotoxicity and exerts antitumor activity. The drug can pass through the blo...

Claims

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Application Information

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IPC IPC(8): C07D487/04C07D311/30A61P35/00A61P35/02A61K31/352A61K31/4188
CPCA61P35/00A61P35/02C07B2200/13C07D311/30C07D487/04
Inventor 李金美陈嘉媚鲁统部
Owner TIANJIN UNIVERSITY OF TECHNOLOGY
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