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Quercetin-lysine coamorphous substance

An amorphous and lysine technology, applied in the field of medicine, can solve the problems of limited clinical application and low absorption bioavailability

Active Publication Date: 2016-12-14
SHENZHEN NYCRIST TECH CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, because quercetin is almost insoluble in water, the bioavailability of oral absorption is low, which greatly limits the clinical application.

Method used

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  • Quercetin-lysine coamorphous substance

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0056] Embodiment 1: Preparation method of quercetin-lysine co-amorphous substance

[0057] Lysine and quercetin anhydrate were weighed at a molar ratio of 1:0.5, placed in a high-speed ball mill at room temperature (45% RH) at a grinding frequency of 20 Hz, and dried for 20 minutes.

Embodiment 2

[0058] Embodiment 2: Preparation method of quercetin-lysine co-amorphous substance

[0059] Lysine and quercetin anhydrate were weighed at a molar ratio of 1:1, placed in a high-speed ball mill at room temperature (45% RH) at a grinding frequency of 25 Hz, and dried for 30 minutes.

Embodiment 3

[0060] Embodiment 3: Preparation method of quercetin-lysine co-amorphous substance

[0061] Lysine and quercetin anhydrate were weighed at a molar ratio of 1:1.2, placed in a high-speed ball mill at room temperature (45% RH) at a grinding frequency of 30 Hz, and dried for 60 minutes.

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Abstract

The invention relates to a quercetin-lysine coamorphous substance. The quercetin-lysine coamorphous substance is prepared in the mode that lysine and quercetin anhydrate are combined in the molar ratio of 1:(0.5-1.2); an X-ray powder diffraction spectrum which is obtained through Cu-Kalpha radiation and expressed with an angle 2theta does not have sharp diffraction peaks; the glass transition temperature is 130.42 DEG C. The powder X-ray diffraction and differential scanning spectrum of the quercetin-lysine coamorphous substance is different from the powder X-ray diffraction and differential scanning spectrum of the quercetin and the powder X-ray diffraction and differential scanning spectrum of the lysine, and therefore the solid state is a coamorphous state completely different from the coamorphous state of the quercetin and the coamorphous state of the lysine.

Description

[technical field] [0001] The invention relates to the technical field of medicine, in particular to a quercetin-lysine co-amorphous substance and a preparation method thereof. [Background technique] [0002] Quercetin (Quercetin anhydrate), also known as quercetin and quercetin, is a polyhydroxy flavonoid compound, and its chemical name is 3,3'4',5,7-pentahydroxyflavone. It is widely distributed in nature, commonly found in vegetables and fruits, and currently known to exist in more than 100 species of plants. Its range of pharmacological effects is also very wide. It has positive effects on anti-virus, anti-cancer, lowering blood sugar and blood pressure, regulating immunity and protecting cardiovascular system. It also has a positive effect on antidepressant. In terms of physical properties, quercetin is a yellow needle-like crystal, soluble in ethanol, methanol, ethyl acetate, glacial acetic acid, etc., insoluble in petroleum ether, benzene, ether, chloroform, and almos...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D311/30
CPCC07D311/30
Inventor 田芳
Owner SHENZHEN NYCRIST TECH CO LTD