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
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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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