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Flavonoid new chemical entity, composition and use

A technology of flavonoid compounds and compositions, which is applied in the field of medicine, can solve the problems of unpublished literature reports, etc., and achieve the effects of improving hygroscopicity, improving operability, and good sliding properties

Pending Publication Date: 2016-08-10
刘力
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Currently published literature only reports hesperidin [molecular formula: C 28 h 34 o 15， Molecular weight: 610.56, CAS: 520-26-3], [Reference 1, Zhu Rongli, et al., Research on the extraction process of hesperidin from orange peel, Food and Fermentation Industry, Issue 6, 2012, pp. 57-60; literature 2. He Lina, Ye Hua, Guo Fangqiu, Research on Hesperidin Analytical Methods, Guangzhou Chemical Industry, 2012, 40(14):126-128; Document 3, Qian Junzhen and Wang Bochu, Research Progress on the Pharmacological Effects of Hesperidin, Natural Product Research and Development, CSCD 2010 Issue 1 - Page, 5 pages in total; Literature 4, Zhang Dongsong, Gao Huiyuan, Wu Lijun, Research Progress on the Pharmacological Activity of Hesperidin, Chinese Modern Traditional Chinese Medicine, 2006, 8(7):25-27; Literature 5, Xiong Li, Li Jun, Wang Wen, et al, Therapeutic Effects and Partial Mechanisms of Hesperidin on Collagen Arthritis in Rats, Journal of Anhui Medical University, 2011, 46(10):1013-1017; Literature 6, Li Wei, Liu Juan , Liu Gan, Li Jun, The protective effect and mechanism of hesperidin on mice with acute chemical liver injury, Journal of Anhui Medical University, 2010,45(3):346-350;] Public literature also reports that hesperidin is used for Preparation of flavonoid derivatives such as methyl hesperidin and diosmin; but so far, there is no published bibliography at home and abroad for the hesperidin crystalline hydrate of the present invention [C 28 h 34 o 15 · n H 2 O, wherein n=0.75, 1.0] and its preparation method and use

Method used

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  • Flavonoid new chemical entity, composition and use

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0075]Example 1 Preparation of Hesperidin 0.75 Hydrate In a stainless steel bucket, add 2kg of dry orange peel fine powder, add 12 times the amount of water, 1 times the amount of ethanol to soak, and use ultrasonic waves with a frequency between 25kHz-50kHz to assist extraction After 30 minutes, add enough saturated lime water, stir, control the pH of the solution=11.5-12, and soak for 2 hours under stirring, filter and separate the solid matter, and obtain the first part of the filter residue and the first part of the filtrate; the obtained first part of the filtrate Use 3M hydrochloric acid solution to adjust the pH to 4-6, place it to allow the precipitate to be fully separated; the obtained first part of the filter residue is then soaked in 6 times the amount of water and 0.1 times the amount of ethanol and assisted by ultrasonic extraction with a frequency between 25kHz and 50kHz for 30 Minutes, add saturated lime water, stir, control pH = about 11.5, soak in this way for...

Embodiment 2

[0076] Example 2 Preparation of hesperidin monohydrate In a stainless steel bucket, add 3 kg of dry orange peel fine powder, add 12 times the amount of water to soak for 1 hour, add enough saturated lime water, stir, and control the pH of the solution=11.5- 12 or so, soak for 2 hours under stirring, filter and separate the solid matter, and obtain the first part of the filter residue and the first part of the filtrate; the obtained first part of the filtrate is adjusted to pH 4-6 with 3M hydrochloric acid solution, and placed to allow the precipitation to be fully analyzed. Obtain the precipitate of the first part of the filtrate; the obtained first part of the filter residue is then soaked with 10 times the amount of water, add saturated lime water, stir, control the pH=11.5, soak in this way for 2 hours, filter, discard the filter residue, and obtain the second part of the precipitate Adjust the pH of the filtrate to 4.5 with 3M hydrochloric acid solution, and place it to all...

Embodiment 3

[0077]Example 3 Preparation of hesperidin 0.75 hydrate In a stainless steel bucket, add 2.2kg of dry orange peel fine powder, add 8 times the amount of ethanol, 3 times the amount of water, soak for 3 hours and use the frequency between 25kHz-50kHz Ultrasonic-assisted extraction for 30 minutes, filtering, the filtrate of the first part and the filter residue of the first part, the filter residue was soaked in 12 times the amount of water for 1 hour, added saturated lime water, stirred, and the pH of the solution was controlled to be around 11.0-12, and stirred Soak under water for 2 hours, filter and separate the solid matter to obtain the second part of the filter residue and the second part of the filtrate; adjust the pH of the obtained first part of the filtrate and the second part of the filtrate to 4-6 with 2M hydrochloric acid solution, and place it to precipitate Sufficiently separate out, filter with suction, wash the solid with ethanol for 3 times, fully rinse with ace...

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Abstract

The invention provides a flavonoid new chemical entity, which has little moisture absorption and good storage stability, and is applicable to preparation of food or health food or drugs for reduction of capillary fragility, treatment or prevention of chronic venous insufficiency, hemorrhoid, scurvy, venous lower limb ulcer, premenstrual syndrome, diabetics' microangiopathy and secondary upper limb lymphedema, cardiovascular diseases, blood glucose and lipid regulation, antisepsis and inflammation reduction, virus resisting, cancer resisting, immunity adjustment, radiation protection, liver protection, rheumatoid arthritis or arthritis resisting, ulcer resisting, phlegm eliminating, asthma relieving, black spots, freckles, free radical resistance, and oxidation resistance.

Description

technical field [0001] The present invention relates to the technical field of medicine, and specifically provides flavonoid derivatives, a new compound entity and composition of vitamin medicine-hesperidin, as well as its preparation and application. Background technique [0002] Polymorphic forms of chemical drugs play an important role in drug research. In the field of pharmacology, the research work on drug crystal forms and drug hydrates or drug solvates has been listed in the research scope of the National Twelfth Five-Year Major New Drug Innovation Science and Technology Major Project. Solvents of compounds, including hydrates, have been prepared and used in medicines for a long time, such as the antineoplastic drug cyclophosphamide recorded in the 36th edition of the US Pharmacopoeia, the 8.1th edition of the European Pharmacopoeia, and the 2010 edition of the Chinese Pharmacopoeia in a solid form at room temperature. It exists in the form of hydrate, and the compou...

Claims

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Application Information

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IPC IPC(8): C07H17/07C07H1/08A61K31/7048A61P9/14A61P31/04A61P7/10A61P19/02A61P17/02A61P3/10A61P9/00A61P3/06A61P9/12A61P29/00A61P31/12A61P35/00A61P37/02A61P1/16A61P1/04A61P11/06A61P11/10A61P39/06A61P17/18A61P17/16A61P17/00A23L1/30
Inventor 刘力
Owner 刘力
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