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Anti-lung cancer pharmaceutical composition, its application, pill case and package

An anti-lung cancer drug and composition technology, applied in the field of biomedicine, can solve problems that need further research and have not yet seen anti-lung cancer treatment

Inactive Publication Date: 2014-07-23
FUDAN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

As follow-up studies have found, the amiloride also has inhibitory effects on other targets, including Na that regulates the pH value of tumor cells. + -H + Exchange body 1 (Na + -H + exchanger1, NHE1), and the urokinase-type plasminogen activator (uPA) that mediates tumor migration, invasion and metastasis, so it has a certain anti-tumor effect; but the role of its anti-tumor effect in vitro The effective concentration is in the range of several millimoles, which is a concentration that is difficult to achieve in vivo. Therefore, whether amiloride has anti-tumor application prospects in vivo and the in-depth mechanism elucidation still needs further study
[0006] So far, there has been no report on the drug combination of amiloride hydrochloride and EGFR TKI applied to the treatment of lung cancer

Method used

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  • Anti-lung cancer pharmaceutical composition, its application, pill case and package
  • Anti-lung cancer pharmaceutical composition, its application, pill case and package
  • Anti-lung cancer pharmaceutical composition, its application, pill case and package

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0036] Example 1 MTT method to detect the cytotoxic effect of amiloride hydrochloride combined with erlotinib and gefitinib on human non-small cell lung cancer Calu-6

[0037] Experimental Materials:

[0038] Human non-small cell lung cancer cell calu-6 (Shanghai Cell Bank, Chinese Academy of Sciences) was stored at 37°C, 5% CO 2 Under normal conditions, the medium was RPMI-1640 (Gibco) containing 10% fetal bovine serum (Hyclone). The standard product of amiloride hydrochloride was purchased from China National Institute for the Control of Pharmaceutical and Biological Products, and the mother solution 50mM was prepared by DMSO. Erlotinib hydrochloride and gefitinib raw materials are provided by Xuanhong Pharmaceutical (Jinan), and the mother solution is prepared with 10mM DMSO. MTT was purchased from Sigma (USA). experimental method:

[0039] 1. Digest the well-differentiated cells with trypsin, suspend them in conventional medium, and adjust the cell density to 5×10 4 c...

Embodiment 2

[0046] Example 2 MTT method to detect the cytotoxic effect of amiloride hydrochloride combined with erlotinib and gefitinib on human non-small cell lung cancer HCC-827, NCI-H292 and H1975

[0047] Experimental Materials:

[0048] Human non-small cell lung cancer cells HCC-827, NCI-H292, H1975 (Shanghai Cell Bank, Chinese Academy of Sciences) were stored at 37°C, 5% CO 2 Under normal conditions, the medium was RPMI-1640 (Gibco) containing 10% fetal bovine serum (Hyclone). The standard product of amiloride hydrochloride was purchased from China National Institute for the Control of Pharmaceutical and Biological Products, and the mother solution 50mM was prepared by DMSO. Erlotinib hydrochloride and gefitinib raw materials are provided by Xuanhong Pharmaceutical (Jinan), and the mother solution is prepared with 10mM DMSO. MTT was purchased from Sigma (USA).

[0049] experimental method:

[0050] 1. Digest the well-differentiated cells with trypsin, suspend them in conventiona...

Embodiment 3

[0055] Example 3 Long-term growth inhibition test of amiloride hydrochloride sensitization to erlotinib hydrochloride and gefitinib

[0056] Experimental Materials:

[0057] Giemsa stain was purchased from Sigma-Aldrich (071M4343); other materials were the same as in Example 1.

[0058] experimental method:

[0059] 1. Digest the well-differentiated cells with trypsin, suspend them in conventional medium, and adjust the cell density to 1×10 3 cells / ml. 600 μl / well was inoculated in a 6-well culture plate (1.9 mL medium was placed in the culture plate in advance), and cultivated overnight in an incubator.

[0060] 2. After 72 hours, the drug-containing medium was replaced, so that the final concentration of amiloride hydrochloride in the single drug group was 100 μM, the final concentrations of erlotinib hydrochloride and gefitinib were 10 μM, and the combined drug group contained the same final concentrations of the above two. concentration of the drug. The blank control ...

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Abstract

The invention belongs to the technical field of biology medicine, and relates to an anti-lung cancer pharmaceutical composition, an application, a pill case and a package, the pharmaceutical composition, the pill case and the package contain amiloride with therapeutically effective amount and an epidermal growth factor tyrosine kinase inhibitor EGFR-TKI with therapeutically effective amount which are can be taken as a combined preparation and used in a simultaneous, separating or orderly mode, and also comprises erlotinib and gefitinib but not limited; wherein the mol ratio of amiloride to EGFR-TKI is 500: 1-1: 50. When the pharmaceutical composition, the pill case and the package are used for treating tumor, the drug efficiency which is better than that of EGFR-TKI with individual usage can be obtained, and has curative effect for EGFR-TKI drug resistant tumor due to K-ras mutation.

Description

technical field [0001] The invention belongs to the technical field of biomedicine, and in particular relates to a pharmaceutical composition for anti-lung cancer and its application, a medicine box and a package. Background technique [0002] Malignant tumors are one of the most important diseases that endanger human health. Among them, lung cancer has replaced liver cancer as the malignant tumor with the highest incidence in my country; according to statistics, 522,000 people were diagnosed with lung cancer in 2008 alone, and more than 85% of them were difficult to treat. Non-small-cell lung cancer (NSCLC). Compared with small cell lung cancer, the NSCLC is not sensitive to chemotherapy, so how to improve the effect of postoperative chemotherapy for NSCLC is the key to prolonging the survival of patients, and it is also an important task for Chinese medical researchers. [0003] It is currently known that the epidermal growth factor receptor (Epidermal Growth Factor Recept...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K45/00A61P35/00A61K31/4965
Inventor 郑媛婷蔡卫民李涛邵腾飞周宁杨慧莹
Owner FUDAN UNIV
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