Application of desmethylene berberine acetate hydrochloride in the preparation of medicaments for preventing or treating drug-induced liver injury

A technology for desmethylene berberine and acute liver injury, applied in the preparation of drugs for the prevention or treatment of acute liver injury, in the field of desmethylene berberine acetate hydrochloride, to improve gastrointestinal absorption, Reduce oxidative stress and inflammatory effects, increase the effect of drug stability

Active Publication Date: 2022-07-05
南京线靶生物医药科技有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

So far, there are no records and reports about the application of desmethylene berberine acetate hydrochloride in the prevention and / or treatment of acute liver injury caused by acetaminophen in the prior art

Method used

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  • Application of desmethylene berberine acetate hydrochloride in the preparation of medicaments for preventing or treating drug-induced liver injury
  • Application of desmethylene berberine acetate hydrochloride in the preparation of medicaments for preventing or treating drug-induced liver injury
  • Application of desmethylene berberine acetate hydrochloride in the preparation of medicaments for preventing or treating drug-induced liver injury

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0052] Example 1. Preparation of desmethylene berberine acetate hydrochloride

[0053] Method: Weigh 1.2g DMB, put it into a 50mL round-bottomed flask, add 10mL acetic anhydride and mix well, then add 200μL concentrated sulfuric acid; stir and react at 70°C for 2h, pour the reaction solution into 10mL ice-cold purified water, and use plastic wrap. After sealing, place it in a 4°C refrigerator for 30 minutes, filter, and wash the filter cake with an appropriate amount of ice water, and the filter cake is the product after drying.

[0054] Result: Demethylene berberine acetate hydrochloride was obtained, and the product appeared as yellow powder.

Embodiment 2

[0055] Example 2. Purity analysis of desmethylene berberine acetate hydrochloride

[0056] Methods: The HPLC method was used for analysis. Demethylene berberine acetate hydrochloride was dissolved in acetonitrile, and filtered through a 0.22 μm microporous membrane to prepare a sample with a final concentration of 200 μg / ml. HPLC chromatograph: Agilent 1100 high performance liquid chromatograph. Chromatographic column: Agilent Eclipse XDB-C18 (4.6×150 mm, 5 μm). Mobile phase: A: 20 mM phosphate buffer, B: acetonitrile. HPLC gradient elution conditions: 0-13min, 20%B-55%B; 13-14min, 55%B; 14-15min, 20%B; 15-16min, 20%B. Detection wavelength: 349nm. Column temperature: 30 °C, flow rate: 1.0 ml / min, and injection volume of 1 μl.

[0057] Results: HPLC analysis results were as follows figure 1 As shown, the retention time of desmethylene berberine acetate hydrochloride is 6.520 min, and the purity is more than 99%, which meets the requirements of biological activity and pharm...

Embodiment 3

[0058] Example 3. Structural identification of desmethylene berberine acetate hydrochloride

[0059] Methods: The molecular structure was identified by infrared spectroscopy, mass spectrometry and nuclear magnetic resonance spectroscopy. The mass spectrometer is watersQ-TOF MicroTM, ionization mode: ESI(+), mass scanning range: m / z80-1000, capillary voltage: 2500v, cone voltage: 25v, ion source temperature: 100°C, atomization temperature: 200 ℃, cone gas flow rate: 50L / hr, atomizing gas flow rate: 400L / hr.

[0060] Results: The positive ion mass spectrometry analysis results of desmethylene berberine acetate hydrochloride were as follows figure 2 As shown, ESI-MS (m / z): molecular ion peak [M+H]+=408.1, which is consistent with the theoretical molecular weight of desmethylene berberine acetate hydrochloride.

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Abstract

The invention relates to the field of biomedicine, in particular to the application of desmethylene berberine acetate hydrochloride in the preparation of a drug for preventing or treating drug-induced liver injury. Compared with desmethylene berberine hydrochloride, desmethylene berberine acetate has increased stability, improved oral absorption and bioavailability, and has anti-inflammatory and antioxidant activities. In the process of acute liver injury caused by acetaminophen, it can prolong the survival time of patients and win precious treatment time for patients.

Description

Technical field: [0001] The invention relates to the field of biomedicine, in particular to the application of desmethylene berberine acetate hydrochloride in preparing a medicine for preventing or treating acute liver injury. Background technique: [0002] Drug-induced liver injury (DILI) is the liver injury caused by the hypersensitivity or reduced tolerance of the drug itself or its metabolites as well as the specific constitution. The pathogenic mechanisms of drug-induced liver injury are generally divided into two categories. One is that the degree of injury is dose-dependent and is directly caused by the drug and its intermediate metabolites on the liver. The other is the specificity of the body to the drug This kind of drug-induced liver injury is unpredictable and affected by genetic and other factors. Statistics show that the incidence of drug-induced liver injury in my country is higher than 20 / 100,000 people, with an average of 23.80 / 100,000 people. In the Unite...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/4375A61P1/16
CPCA61K31/4375A61P1/16
Inventor 张玉彬李青霞张淼
Owner 南京线靶生物医药科技有限公司
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