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Palmatine hydrochloride-aspirin supramolecular compound

A supramolecular compound, palmatine hydrochloride technology, applied in the field of drug crystallization, can solve the problem that there is no public report on the preparation method and application of palmatine hydrochloride and aspirin supramolecular compound, and achieves green and efficient preparation method and crystal structure. Clear, physicochemically stable effects

Active Publication Date: 2022-05-13
MINJIANG UNIV +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] At present, there is no public report on supramolecular compound of palmatine hydrochloride and aspirin and its preparation method and application

Method used

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  • Palmatine hydrochloride-aspirin supramolecular compound
  • Palmatine hydrochloride-aspirin supramolecular compound
  • Palmatine hydrochloride-aspirin supramolecular compound

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0026] Put 0.5 mmol of palmatine hydrochloride hydrate and 0.5 mmol of aspirin into 50 mL of absolute ethanol, heat and stir to obtain a clear mixed solution; dry the mixed solution at room temperature to obtain palmatine hydrochloride-aspirin supramolecular compound .

[0027] The palmatine hydrochloride-aspirin supramolecular compound prepared in this embodiment is characterized by single crystal X-ray diffraction, and the result shows that the structural unit of the supramolecular compound comprises palmatine hydrochloride molecule, aspirin molecule and water molecule, three The molar ratio between them is 1:1:1; the supramolecular compound belongs to the triclinic crystal system, the P-1 space group, and the unit cell parameters are: a =7.8368(7) Å, b = 11.5369(6) Å, c = 16.4916(8) Å, α = 76.151(4) º , β = 83.683(5) º , gamma = 73.338(6) º , V = 1385.54(17) Å 3 , Z = 2, D c = 1.405 g / cm 3 , the molecular formula is [C 21 h 22 ClNO 4 ]·[C 9 h 8 o 4 ] ...

Embodiment 2

[0031] Put 1 mmol of palmatine hydrochloride hydrate, 1 mmol of aspirin and 5 mL of absolute ethanol into a glass bottle with a lid and mix them, put them into a magnetic rotor and seal them, and stir magnetically at room temperature to form a suspension, and keep it for 24 hours. The resulting precipitate was filtered, washed with a small amount of absolute ethanol, and dried to obtain the palmatine hydrochloride-aspirin supramolecular compound.

[0032] image 3 It is the powder X-ray diffraction pattern of the palmatine hydrochloride-aspirin supramolecular compound prepared in the present embodiment. Depend on image 3 Know, the palmatine hydrochloride-aspirin supramolecular compound that the present embodiment makes is identical with embodiment 1 θ The peaks appear at different angles, indicating that the two have the same crystal structure.

[0033] Figure 4 It is the dynamic water vapor adsorption diagram of palmatine hydrochloride hydrate and the palmatine hydroch...

Embodiment 3

[0036] Put 1 mmol of palmatine hydrochloride hydrate, 1 mmol of aspirin and 5 mL of deionized water into a glass bottle with a lid and mix them, put them into a magnetic rotor and seal them, and stir magnetically at room temperature to form a suspension, and keep it for 24 hours. The resulting precipitate was filtered, washed with a small amount of deionized water, and dried to obtain the palmatine hydrochloride-aspirin supramolecular compound.

[0037] X-ray powder diffraction characterization result shows, the palmatine hydrochloride-aspirin supramolecular compound that the present embodiment makes is identical with embodiment 1. θ The peaks appear at different angles, indicating that the two have the same crystal structure.

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Abstract

The invention discloses a palmatine hydrochloride-aspirin supramolecular compound as well as a preparation method and application thereof, and belongs to the technical field of medicine crystallization. The structural unit of the pharmaceutical co-crystal comprises palmatine hydrochloride molecules, aspirin molecules and water molecules, the molar ratio of the palmatine hydrochloride molecules to the aspirin molecules to the water molecules is 1: 1: 1, and the molecular formula of the pharmaceutical co-crystal is [C21H22ClNO3]. [C9H8O4]. H2O. The palmatine hydrochloride-aspirin supramolecular compound is prepared by mixing a palmatine hydrochloride hydrate and aspirin in a solvent according to a molar ratio of 1: 1 and carrying out spray drying, evaporation or suspension stirring and other processes, the preparation method is green and efficient, and the supramolecular compound is high in light stability, wet stability and thermal stability and weak in hygroscopicity, and can be used for preparing the palmatine hydrochloride-aspirin supramolecular compound. The compound has good human colorectal cancer cell inhibition activity, and can be used as an active component for preparing a pharmaceutical composition or a health care product for treating or preventing colorectal cancer.

Description

technical field [0001] The invention belongs to the technical field of medicine crystallization, and in particular relates to a palmatine hydrochloride-aspirin supramolecular compound, a preparation method thereof, and an application of a pharmaceutical composition or a health care product using the palmatine hydrochloride as an active ingredient. Background technique [0002] Palmatine hydrochloride (Palmatine chloride), also known as palmatine hydrochloride, palmatine hydrochloride, has the effect of clearing away heat and detoxifying, clinically used to treat gynecological inflammation, bacillary dysentery, enteritis, respiratory tract and urinary tract infection, surgical infection and ocular conjunctivitis etc. In addition, palmatine hydrochloride also shows good anti-cancer, hypoglycemic, anti-Alzheimer's disease and other pharmaceutical activities. Studies have shown that palmatine hydrochloride combined with photodynamic therapy is effective for breast cancer (Photo...

Claims

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Application Information

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IPC IPC(8): C07D455/03C07C69/157C07C67/52A61K31/4745A61K31/616A61P29/00A61P31/04A61P31/10A61P9/00A61P7/02A61P35/00A61P19/02
CPCC07D455/03C07C69/157A61K31/4745A61K31/616A61P29/00A61P31/04A61P31/10A61P9/00A61P7/02A61P35/00A61P19/02A61K2300/00Y02A50/30
Inventor 张燕杰娄本勇张晨刘磊张梅黄雅丽李延广向恒
Owner MINJIANG UNIV
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