Resveratrol-temozolomide eutectic crystal and preparation method and application thereof

A technology of resveratrol and temozolomide, which is applied in the field of drug co-crystals, can solve the problems of limiting the residence time of temozolomide, reducing the efficacy of prodrugs, affecting the therapeutic effect, etc., so as to improve the bioavailability of drugs, save the dosage of drugs, and improve the solubility. Effect

Pending Publication Date: 2020-07-17
GUANGXI UNIV OF CHINESE MEDICINE
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Because of its rapid oral elimination and short half-life, it may limit the residence time of temozolomide at the surgical site, thereby affecting the therapeutic effect
In addition, temozolomide also has stability problems. During storage, its color changes from white to light brown / pink, indicating that temozolomide is degraded to AIC, which reduces the efficacy of the prodrug

Method used

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  • Resveratrol-temozolomide eutectic crystal and preparation method and application thereof
  • Resveratrol-temozolomide eutectic crystal and preparation method and application thereof
  • Resveratrol-temozolomide eutectic crystal and preparation method and application thereof

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Experimental program
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Effect test

Embodiment 1

[0036] The resveratrol-temozolomide co-crystal uses resveratrol as an active pharmaceutical ingredient, and combines with another drug temozolomide through weak hydrogen bonds to form a resveratrol-temozolomide drug co-crystal, which is crystallized in a monoclinic Crystal system, space group P2 1 / c, axis length Shaft angle α=90.00°, β=95.9755(1)°, γ=90.00°, Concretely has the following chemical structural formula:

[0037]

[0038] A preparation method of resveratrol-temozolomide co-crystal, comprising the following steps:

[0039] (1) Put resveratrol and temozolomide in a 10mL vial at a molar ratio of 1:1, add 6mL of methanol, stir at room temperature for 24 hours, filter, and dry to obtain resveratrol-temozolomide cocrystal powder;

[0040] (2) Transfer the filtrate obtained by filtration to a beaker, let it stand for volatilization, and precipitate orange crystals.

Embodiment 2

[0042] A kind of resveratrol-temozolomide co-crystal preparation method, comprises the following steps:

[0043] (1) Put resveratrol and temozolomide in a grinding tank according to a certain molar ratio, add 1-2 drops of methanol dropwise; grind for 45 minutes at a speed of 1200r / min to obtain resveratrol-temozolomide co-crystal powder.

[0044] The drug active ingredient (API) selected in the present invention is resveratrol, and another drug temozolomide is prepared to obtain a drug co-crystal with a novel structure. Its eutectic structure is briefly described as follows:

[0045] The resveratrol-temozolomide co-crystal of the present invention is composed of resveratrol and temozolomide crystallized in a crystal lattice at a ratio of 1:1. Among them, resveratrol and temozolomide form hydrogen bonds through O-H...O interaction, and there is π-π stacking between molecules. The space group of the drug cocrystal is monoclinic, space group P2 1 / c, axis length Shaft angl...

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Abstract

The invention aims to provide a resveratrol-temozolomide eutectic crystal, which can improve the solubility of a medicine, improve the stability and improve the bioavailability, and also provides a preparation method and application of the resveratrol-temozolomide eutectic crystal. The invention relates to the resveratrol-temozolomide eutectic crystal. Resveratrol is used as an active pharmaceutical ingredient and is combined with another drug temozolomide through hydrogen bond weak action to form a resveratrol-temozolomide drug-drug co-crystal, the resveratrol-temozolomide drug-drug co-crystal is crystallized in a monoclinic system, the space group is P21 / c, the axial long axis angle alpha is 90.00 degrees, beta is 95.9755 (1) degrees and gamma is 90.00 degrees.

Description

technical field [0001] The invention belongs to the field of drug co-crystals, in particular to a resveratrol-temozolomide drug co-crystal. Background technique [0002] Resveratrol (Resveratrol), chemical name: 3,5,4'-trihydroxystilbene, its chemical structure is as follows: [0003] [0004] Resveratrol is a natural non-flavonoid polyphenolic compound, mainly derived from grapes, peanuts, mulberries, etc. However, due to its low water solubility, poor stability, low bioavailability, instability under light, heat and oxidant conditions, it is easily oxidatively degraded, which limits its application to a certain extent. Therefore, improving the solubility and other properties of resveratrol and then improving the bioavailability has become an urgent problem to be solved. Temozolomide (Temozolomide) has the following chemical structural formula: [0005] [0006] Temozolomide (Temozolomide) is a small molecule, fat-soluble alkylating agent, and it has a certain effec...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D487/04C07C39/215C07C37/84
CPCC07D487/04C07C39/215C07C37/84C07B2200/13
Inventor 陈清林宁马晓琴刘水丽
Owner GUANGXI UNIV OF CHINESE MEDICINE
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