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Pharmaceutical composition of osimertinib, and applications thereof

A composition and drug technology, applied in the field of medicine, can solve the problems of high toxicity and side effects of epidermal growth factor receptor tyrosine kinase inhibitors, and achieve the effects of low drug resistance, few side effects and high curative effect

Inactive Publication Date: 2020-04-24
CHIA TAI TIANQING PHARMA GRP CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0014] The purpose of the present invention is to solve the problems of epidermal growth factor receptor tyrosine kinase inhibitors (EGFR-TKIs) drug resistance and large toxic and side effects in the treatment of non-small cell lung cancer (NSCLC), and provide a method for targeted therapy of lung cancer The pharmaceutical composition provided by the invention has better water solubility, low drug resistance, high curative effect, and few side effects

Method used

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  • Pharmaceutical composition of osimertinib, and applications thereof
  • Pharmaceutical composition of osimertinib, and applications thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0032] Embodiment 1 dosage form preparation

[0033] According to the ratio of quercetin copper: osimertinib 500:1, 300:1, 200:1, 50:1, 5:1, add pharmaceutically acceptable conventional excipients or auxiliary ingredients, and make it orally by conventional methods formulations for follow-up testing.

Embodiment 2

[0034] Example 2 Cell experiment

[0035] Cell proliferation assay was used to determine the effect of osimertinib, quercetin metal complex and pharmaceutical composition of the present invention on cancer cell line A549:

[0036] 1. Experimental materials

[0037] (1) Drugs

[0038] Osimertinib, copper quercetin and the pharmaceutical composition of the present invention are all self-made products.

[0039] All the above drugs were dissolved in DMSO, made into a 100 mmol / L storage solution, stored at -20°C, and used in subsequent examples.

[0040] (2) cells

[0041] Human lung adenocarcinoma cells A549 (expressing wild-type EGFR gene) were cultured in RPMI-1640 medium containing 10% fetal bovine serum, penicillin and streptomycin (final concentration 100 U·mL-1) at a constant temperature of 37°C for 5 %CO 2 In the incubator, the cells grow adherently in a single layer. In the experiment, the cells in the logarithmic growth phase in a good growth state were taken, digest...

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Abstract

A purpose of the invention is to solve the problems of drug resistance, high toxic and side effects and the like of epidermal growth factor receptor tyrosine kinase inhibitors (EGFR-TKIs) in non-smallcell lung cancer (NSCLC) treatment and provide a pharmaceutical composition for targeted therapy of lung cancer, wherein the active ingredients of the pharmaceutical composition are quercetin metal coordination compound and osimertinib or a pharmaceutically acceptable salt thereof, and the quercetin metal coordination compound is selected from quercetin copper, quercetin manganese and quercetin zinc. The pharmaceutical composition provided by the invention has good water solubility, low drug resistance, high curative effect and few side effects.

Description

technical field [0001] The invention belongs to the field of medicine, and in particular relates to a pharmaceutical composition containing a quercetin metal complex and osimertinib and an application thereof. Background technique [0002] Lung cancer is one of the most common malignant tumors in the world. Lung cancer-related deaths account for more than 20% of cancer-related deaths worldwide. According to statistics in 2015, about 610,000 patients died of the disease in China every year, accounting for 22% of all cancer-related deaths. It has become the first cause of death of malignant tumors in urban population in my country. [0003] Non-small cell lung cancer (NSCLC) accounts for about 80-85% of all lung cancers, including squamous cell carcinoma (squamous cell carcinoma), adenocarcinoma, and large cell carcinoma. About 75% of patients are diagnosed with locally advanced or metastatic disease. The 5-year survival rate is very low. Chemotherapy is routine treatment f...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/555A61K31/506A61P35/00
CPCA61K31/506A61K31/555A61P35/00A61K2300/00
Inventor 王春雷叶红春
Owner CHIA TAI TIANQING PHARMA GRP CO LTD
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