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Enoxolone derivative, preparation method and uses

A technology of glycyrrhetinic acid and medicines, applied in the field of glycyrrhetinic acid derivatives, preparation and application, which can solve the problems of limiting the clinical application of glycyrrhetinic acid, the inability to prepare injections, and vascular irritation, so as to reduce irritation and vasospasm , Solve the solubility and improve the effect of safety

Active Publication Date: 2011-10-26
SHANDONG LUYE PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] Although the sodium salt or potassium salt of glycyrrhetinic acid reported in the literature can improve its solubility, there is still sodium retention and vascular irritation, which cannot be prepared into injections, which greatly limits the clinical application of glycyrrhetinic acid

Method used

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  • Enoxolone derivative, preparation method and uses
  • Enoxolone derivative, preparation method and uses
  • Enoxolone derivative, preparation method and uses

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0031] Example 1: Preparation of glycyrrhetinic acid arginine

[0032] Add 2.35 g (0.005 mol) of glycyrrhetinic acid, 0.87 g (0.005 mol) of L-arginine, and 440 mL of 90% ethanol (V / V) to the reaction flask, stir and react for 2 hours, and evaporate the solvent under reduced pressure. Add 20 mL of ethyl acetate to the residue, grind to obtain a pale yellow precipitate, filter, and dry under reduced pressure to obtain 3.0 g of a pale yellow solid with a yield of 93%. Glycyrrhetinic acid was used as a reference substance for content determination, and the product content was 99.7%.

[0033] Glycyrrhetinic acid arginine shows the following physical and chemical properties:

[0034] Properties: light yellow powder mp: 183~186℃.

[0035] ESI-MS m / z: 644([M-H] + ).

[0036] Elemental analysis% calculated value (actual value): C 67.05 (67.48), H9.38 (9.27), N8.69 (8.81).

[0037] Molecular formula: (C 36 H 60 N 4 O 4 )

[0038] UVλ max nm: 258IR (KBr, v max , Cm -1 ): 3172(-NH 2 , -OH), 1647 ...

Embodiment 2

[0040] Example 2: Preparation of Glycyrrhetinic Acid Arginine

[0041] Add 2.35 g (0.005 mol) of glycyrrhetinic acid, 0.87 g (0.005 mol) of L-arginine, and 440 mL of 85% ethanol (V / V) to the reaction flask, stir and react for 2 hours, and evaporate the solvent under reduced pressure. Add 20 mL of ethyl acetate to the residue, grind to obtain a light yellow precipitate, filter, and dry under reduced pressure to obtain 3.1 g of a light yellow solid with a yield of 96%. Glycyrrhetinic acid was used as a reference substance for content determination, and the product content was 99.6%.

Embodiment 3

[0042] Example 3: Preparation of Glycyrrhetinic Acid Arginine Injection

[0043] Glycyrrhetinic acid arginine salt (prepared according to Example 1) 5g

[0044] Propylene glycol 150g

[0045] Sodium citrate 10g

[0046] Add water for injection to 1000ml

[0047] Weigh the prescription amount of glycyrrhetinic acid arginine salt, dissolve it in propylene glycol under heating, add sodium citrate and water for injection, adjust the pH to 9.0 with 5% NaOH, add 0.1% activated carbon and stir for 30 minutes, filter, and dispense into ampoules Medium, 1ml per tube, sterilize at 115°C for 30 minutes, it is ready.

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Abstract

The present invention provides one new kind of glycyrrhetic acid derivative with high water solubility, high absorption, no irritation to blood vessel and capacity of being prepared into injection, and its preparation process, medicinal composition and preparation. The glycyrrhetic acid derivative has excellent treating effect on acute and chronic hepatitis, bacterial hepatitis, viral hepatitis, cerebral ischemia / re-perfusion damage, brain injury and myocardial ischemia / re-perfusion damage.

Description

Technical field [0001] The invention relates to a glycyrrhetinic acid derivative and its preparation method, application and preparation. Background technique [0002] Licorice (Glycyrrhiza uralensis Fisch.) is a legume plant that grows in temperate and subtropical regions. It is mainly produced in western my country. It was first published as a common Chinese herbal medicine in the "Shen Nong's Materia Medica" in the Han Dynasty. According to the theory of traditional Chinese medicine, licorice is calm in nature and sweet in taste. It has the functions of relieving urges, moisturizing the lungs, detoxifying, relieving cough, regulating the meridians, and promoting qi and blood. It is widely used in traditional Chinese medicine prescriptions. Ancient Chinese medical scholars referred to it as old". In 1932, Ruzicka determined the chemical structure of glycyrrhizic acid, the active ingredient of licorice, and opened the prelude to the study of licorice with modern medicine. Sinc...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07C63/00A61K31/56A61K9/19A61K9/20A61K9/48A61K9/08A61K9/10A61P1/16A61P31/04A61P31/12A61P9/10
Inventor 王超云刘生生许卉
Owner SHANDONG LUYE PHARMA CO LTD