Enoxolone derivative, preparation method and uses

A technology of glycyrrhetinic acid and glycyrrhetinic acid salt, which is applied in the direction of medical formula, drug combination, drug delivery, etc., 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 Effects of vasospasm, resolution of solubility, and improvement of safety

Active Publication Date: 2006-04-26
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] Embodiment 1: the preparation of glycyrrhetinic acid arginine

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

[0033] Arginine Glycyrrhetinate exhibits the following physicochemical properties:

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

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

[0036] Elemental analysis % calculated value (found 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] UV lambda max nm: 258

[0039] IR(KBr, v max...

Embodiment 2

[0041] Embodiment 2: the preparation of glycyrrhetinic acid arginine

[0042] Add glycyrrhetinic acid 2.35g (0.005mol), L-arginine 0.87g (0.005mol), 85% ethanol (V / V) 440mL successively in reaction bottle, stir reaction 2 hours, evaporate to dryness under reduced pressure, in 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 the reference substance for content determination, and the product content was 99.6%.

Embodiment 3

[0043] Embodiment 3: Preparation of Glycyrrhetinic Acid-Arginine Injection

[0044] Glycyrrhetinic acid arginine salt (prepared according to Example 1) 5g

[0045] Propylene glycol 150g

[0046] Sodium citrate 10g

[0047] Add water for injection to 1000ml

[0048] 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 pack into ampoules Medium, 1ml each, sterilized at 115°C (for 30 minutes, ready to use.

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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 present invention relates to a glycyrrhetinic acid derivative and its preparation method, use and preparation. Background technique [0002] Licorice (Glycyrrhiza uralensis Fisch.), a leguminous plant, grows in temperate and subtropical regions, and is mainly produced in western my country. As a commonly used Chinese herbal medicine, it was first recorded in "Shen Nong's Herbal Classic" in the Han Dynasty. The theory of traditional Chinese medicine believes that: licorice is flat in nature and sweet in taste, and has the effects of harmonizing urgency, nourishing the lungs, detoxifying, relieving cough, dredging the meridians, and benefiting qi and blood. It is widely used in traditional Chinese medicine prescriptions. old". In 1932, Ruzicka determined the chemical structure of glycyrrhizic acid, the active ingredient of licorice, which opened the prelude to the study of licorice with modern medicine. Since then, a large number of studies have sh...

Claims

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Application Information

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