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Molecularly compatible pharmaceutical composition of docetaxel and elemene and application thereof

A technology of docetaxel and elemene, which is applied in the direction of drug combinations, medical preparations containing active ingredients, antineoplastic drugs, etc., can solve the problems of performance improvement, small scope of application, and limited curative effect, and achieve easy tolerance drug, good antitumor activity, and long residence time

Active Publication Date: 2019-02-01
HANGZHOU NORMAL UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] It is disclosed in the prior art that both docetaxel and elemene have certain anticancer effects, but their curative effects on tumors alone are limited, and there are certain toxic and side effects, especially for drug-resistant tumors. Poor, so its scope of application is small, and its performance needs to be improved

Method used

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  • Molecularly compatible pharmaceutical composition of docetaxel and elemene and application thereof
  • Molecularly compatible pharmaceutical composition of docetaxel and elemene and application thereof
  • Molecularly compatible pharmaceutical composition of docetaxel and elemene and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0037] (1) Test preparation:

[0038] Cultivation of test cell lines

[0039] Take the frozen cells out of the liquid nitrogen tank for recovery, digest the cells, count them, dilute them with medium to form a suspension, and place them at 37°C, 5% CO 2 cultured in an incubator.

[0040] Preparation of drug mother solution

[0041]Take docetaxel bulk drug and elemene bulk drug respectively, dissolve them in DMSO, and then take appropriate volumes and dilute them with culture medium to form mixtures with different proportions.

[0042] (2) Test process

[0043] Cells were digested and counted to prepare tumor cell suspension MCF-7, MCF-7 / T (paclitaxel-resistant MCF-7 cells), A549, A549 / T (paclitaxel-resistant A549 cells), HCT-8, For HCT-8 / T (paclitaxel-resistant HCT-8 cells), MGC-803, PC-3, add 100 μl of cell suspension to each well of a 96-well cell culture plate;

[0044] Place the 96-well cell culture plate at 37°C, 5% CO 2 Cultivate in the incubator for 24 hours; d...

Embodiment 2

[0052] According to the method of Example 1, calculate the IC of different ratios of docetaxel and elemene pharmaceutical composition for different tumor cells 50 value, the result is as follows:

[0053] Table 2 Docetaxel IC of different ratio compositions of docetaxel and elemene 50 Compare

[0054]

[0055] As can be seen from the above table, the above ratio of docetaxel and elemene composition, with 0.25:1 (IC 50 The ratio of the corresponding concentration) docetaxel IC 50 The value is the smallest.

[0056] Table 3 The corresponding elemene IC of different ratio compositions of docetaxel and elemene 50 Compare

[0057]

[0058]

[0059] As can be seen from the above table, the above ratio of docetaxel and elemene composition, at 0.25:1 (IC 50 The proportion of corresponding concentration) when the amount of elemene is larger, it shows that the amount of docetaxel can be reduced when the amount of elemene is large.

Embodiment 3

[0061] According to the method of Example 1, the different ratios of docetaxel and elemene composition are compared with the curative effect of docetaxel for different tumor cells, and the results are as follows:

[0062] Table 4 The curative effect comparison of different ratios of docetaxel and elemene composition

[0063]

[0064]

[0065] As can be seen from the above table, the composition of docetaxel and elemene in different proportions has improved curative effect on different tumor cells compared with docetaxel; when the concentration of elemene is greater than or equal to IC 50 When the concentration is high, the curative effect is obviously improved.

[0066] For the three drug-resistant tumor cells, the ratio was 1:0.25 (IC 50 Compared with docetaxel, the curative effect increased by 1.6 times for drug-resistant MCF-7 breast cancer cells, 1.4 times for drug-resistant lung adenocarcinoma cells, and 1.8 times for drug-resistant colon cancer cells. times, indi...

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Abstract

The invention discloses a molecularly compatible pharmaceutical composition of docetaxel and elemene and application thereof. The docetaxel and elemene are in a mass ratio of 20-1000. The compositioncan be applied to treatment of breast cancer, lung adenocarcinoma, colon cancer, gastric cancer and prostate cancer, and especially has very good treatment effect on taxane drug-resistant breast cancer, taxane drug-resistant lung adenocarcinoma and taxane drug-resistant colon cancer. During application to preparation of drugs treating taxane drug-resistant tumors, the molecularly compatible pharmaceutical composition has significant anti-paclitaxel resistance effect, also can remarkably reduce the toxicity and greatly alleviate the pain of tumor patients. The pharmaceutical composition provided by the invention provides a new strategy for drug-resistant tumor treatment, and has important significance and broad application prospects for drug-resistant tumor treatment.

Description

technical field [0001] The invention relates to the field of pharmaceutical compositions, in particular to a molecularly compatible pharmaceutical composition of docetaxel and elemene and its application in drug-resistant tumors. Background technique [0002] Taxanes such as paclitaxel and docetaxel, as an important part of tumor chemotherapy drugs, have become the first-line drugs in tumor chemotherapy. However, with the wide application of taxane drugs, tumors are resistant to docetaxel. The contradiction between drugs is becoming more and more prominent. [0003] The progression of many life-threatening diseases such as cancer is influenced by multiple mechanisms. Due to this complexity, success with single drug therapy is limited. Therefore, drug combinations are often used to fight cancer and enhance efficacy. For example, Yang Lei et al. found that the rare saponin component of ginseng-paclitaxel multi-component system inhibits the proliferation and growth of lung can...

Claims

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Application Information

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IPC IPC(8): A61K31/337A61K31/015A61P35/00
CPCA61K31/015A61K31/337A61P35/00A61K2300/00
Inventor 谢恬曾昭武曾义英曾义军张娜娜李晨曦
Owner HANGZHOU NORMAL UNIVERSITY
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