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Puerarin novel derivatives as well as preparation method and application thereof

A crystal form and drug technology, which is applied in the field of new puerarin derivatives and their preparation, can solve the problems of no new drug or clinical trials of puerarin derivatives, no major breakthroughs, etc., and achieve obvious anti-hypoxic activity , excellent effect

Active Publication Date: 2020-02-21
SICHUAN ACAD OF CHINESE MEDICINE SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, no major breakthroughs have been made, and no new drugs or clinical trials of puerarin derivatives have been reported.

Method used

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  • Puerarin novel derivatives as well as preparation method and application thereof
  • Puerarin novel derivatives as well as preparation method and application thereof
  • Puerarin novel derivatives as well as preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0052] The preparation of embodiment 1 compound of the present invention

[0053] ① chemical reaction

[0054] Puerarin 50g, add 20 times of 75% V / V ethanol to a 2L round bottom flask, heat to reflux in a water bath, then add 1-10% W / V NaOH or KOH or NaOH 2 CO 3 50ml of aqueous solution, react for 5-60min, take out the reaction solution, adjust the pH value to 6-7 with hydrochloric acid, and set aside.

[0055] ② Desalination

[0056] Method 1: Recover the solvent from the stock solution in step ① under reduced pressure at 60°C, concentrate in a water bath with an evaporating dish to form an extract, and dry under reduced pressure at 60°C to obtain a brown-yellow dry powder. Use 500ml of absolute ethanol to ultrasonically dissolve 5 times, filter through a G3 vertically fused glass sand funnel, combine the filtrates, recover the solvent, and dry under reduced pressure at 60°C to obtain a brownish-yellow dry powder for future use.

[0057] Method 2: Recover the solvent from...

Embodiment 2

[0064] Embodiment 2 prepares the injection of compound of the present invention

[0065] Taking the preparation of 1000ml injection of the compound of the present invention as an example, the raw and auxiliary materials used are as follows:

[0066]

[0067] The preparation process of the conventional injection is adopted, the pH is adjusted to 4-6 with 1% hydrochloric acid, and each 2ml contains 50mg of the compound of the present invention. This product is a colorless clear liquid.

Embodiment 3

[0068] Embodiment 3 prepares the tablet of compound of the present invention

[0069] Taking the preparation of 1000 tablets of the compound of the present invention as an example, the raw and auxiliary materials used are as follows:

[0070] Compound of the present invention 25g

[0071] Starch 160g

[0072] Magnesium Stearate 15g

[0073] It is made by a conventional tablet preparation process, each tablet weighs 0.2 g, and each tablet contains 25 mg of the compound of the present invention.

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Abstract

The invention provides compounds, or a salt or crystalline form of the compounds. A structure of the compounds is represented by a formula I shown in the specification. The compounds provided by the invention are novel-structural puerarin derivatives and are easily soluble in water, wherein the solubility of the compounds in the water is 100 times that of puerarin; and the compounds have obvious anti-hypoxia activity and effect better than that of the puerarin, can be clinically and widely used for preparing medicines for preventing and / or treating cardiovascular and cerebrovascular diseases and diseases such as diabetes, hypertension, cerebral infarction, viral myocarditis and glaucoma.

Description

technical field [0001] The invention belongs to the field of medicine preparation, and in particular relates to a novel puerarin derivative and its preparation method and application. Background technique: [0002] Puerarin is an isoflavone glycoside compound extracted from the dried root of the leguminous plant Puerarialobata (Willd.) Ohwi, the chemical name is 8-β-D-glucopyranose-4', 7-Dihydroxyisoflavone, the chemical structure is: [0003] [0004] Puerarin is a white to slightly yellow crystalline powder, which is soluble in methanol, slightly soluble in ethanol, and slightly soluble in water. [0005] Puerarin has a wide range of pharmacological activities. Pharmacological studies have shown that it has β-adrenergic receptor blocking effect, can reduce vascular resistance, expand coronary artery, improve myocardial contractility, reduce myocardial oxygen consumption, reduce acute myocardial infarction area, and protect myocardial ischemia-reperfusion injury effec...

Claims

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Application Information

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IPC IPC(8): C07D309/10A61K31/351A61P3/10A61P9/00A61P9/12A61P27/06A61P9/10
CPCC07D309/10A61P3/10A61P9/00A61P9/12A61P27/06A61P9/10
Inventor 袁崇均陈帅罗森王笳
Owner SICHUAN ACAD OF CHINESE MEDICINE SCI