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Application of silibinin or its salt in the preparation of drugs that enhance the curative effect of alk-tki and delay its drug resistance

A technology of silibinin and curative effect, which is applied in the field of medical application to achieve the effects of enhancing curative effect, delaying ALK-TKI drug resistance, and improving stability

Active Publication Date: 2018-05-08
THE THIRD AFFILIATED HOSPITAL OF THIRD MILITARY MEDICAL UNIV OF PLA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, there is no literature reporting the use of silibinin or its salts in the preparation of drugs that enhance the efficacy of ALK-TKIs and delay their drug resistance.

Method used

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  • Application of silibinin or its salt in the preparation of drugs that enhance the curative effect of alk-tki and delay its drug resistance
  • Application of silibinin or its salt in the preparation of drugs that enhance the curative effect of alk-tki and delay its drug resistance
  • Application of silibinin or its salt in the preparation of drugs that enhance the curative effect of alk-tki and delay its drug resistance

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0030] Embodiment 1 A kind of silybin sustained-release tablet

[0031]

[0032] a. Add silibinin or its salt to octylphenol polyoxyethylene ether and propylene glycol alginate, and grind to uniformity to obtain silibinin or its salt grind; the microcrystalline cellulose is Add water at a ratio of 1:3 to obtain an aqueous solution; mix silibinin or its salt grind and aqueous solution evenly, and emulsify at high speed to obtain silybin or its salt colostrum; silybin or its salt The salted colostrum is emulsified in a high-pressure homogenizer to obtain silibinin or its salt emulsion; the silibinin or its salt emulsion is spray-dried to obtain silybin or silibinin with a particle size range of 15-25 μm its salt microcapsules;

[0033] b. mixing silibinin or its salt microcapsules with carboxymethylcellulose sodium evenly to obtain mixed powder;

[0034] c. Dissolve 3 / 4 of octyldodecanol in absolute ethanol, add mixed powder, mix evenly, and make soft material;

[0035] d. P...

Embodiment 2

[0036] Embodiment 2 A kind of silybin meglumine sustained-release tablet

[0037]

[0038] Prepare according to the method of Example 1.

experiment example 1

[0039] Experimental example 1 in vitro experiment

[0040] 1. The purpose of the experiment: whether silybin can increase the sensitivity of ALK-TKI cell lines and their drug-resistant strains to ALK-TKI;

[0041] 2. Experimental method: MTT method was used to calculate the activity of lung cancer cells;

[0042] 3. Experimental steps:

[0043] (1) For ALK-TKI sensitive strain H2228 cells, EGFR-TKI sensitive strain H1650 cells, ALK-TKI resistant strain H2228-CR cells, EGFR-TKI resistant strain H1650-M3 cells, EGFR-TKI sensitive strain PC-9 Cells and EGFR-TKI resistant strain PC-9GR cells were respectively amplified, and the logarithmic phase of human lung cancer cell lines were collected, the cells were digested with trypsin, and the cell suspension was centrifuged to sediment the cells; the cells were resuspended in the medium, count;

[0044] (2) Dilute the cell density to 2×10 after counting 4 / mL, add 100 μL of cell suspension to each well of a flat-bottomed 96-well pl...

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Abstract

The present invention relates to a new application of silibinin or its salt, in particular to the application of silibinin or its salt in the preparation of drugs that enhance the curative effect of ALK-TKI and delay its drug resistance; silibinin can significantly reduce Invasion of drug-resistant cells: The average number of cells that made the ALK-TKI-resistant strain H2228-CR invasive ranged from 238 to 86; in addition, silibinin combined with crizotinib could significantly attenuate the growth of transplanted tumors; Silibinin can significantly enhance the efficacy of crizotinib.

Description

technical field [0001] The invention belongs to the field of medical applications, and particularly relates to the application of silibinin or its salts in the preparation of drugs for enhancing the curative effect of ALK-TKI and delaying its drug resistance. Background technique [0002] Lung cancer is currently the main cause of human death due to cancer, and its morbidity and mortality have been increasing in recent years. Non-small cell lung cancer (Non SmaLL CeLL Lung Cancer, NSCLC) accounts for 80%-85% of all lung cancer cases. At present, the individualized treatment of NSCLC has attracted much attention. Studies have shown that echinoderm microtubule-associated protein-like 4 / anaplastic lymphoma kinase (EML4 / ALK) plays a very important role in the occurrence and development of NSCLC. ALK fusion gene-positive patients account for 3%-7% of all NSCLC patients. For advanced NSCLC patients with positive EML4 / ALK fusion gene, the molecular targeted drug for lung cancer,...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/506A61K31/4545A61K31/357A61K9/26A61K47/10A61P1/16A61P11/00A61P35/00
Inventor 何勇李力
Owner THE THIRD AFFILIATED HOSPITAL OF THIRD MILITARY MEDICAL UNIV OF PLA
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