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Application of combination of 5-fluorouracil and paclitaxel in preparation of medicine for treating breast cancer

A technology of fluorouracil and paclitaxel, which is applied in the field of preparing drugs for the treatment of breast cancer, can solve problems affecting patient acceptance and adverse reactions in the blood system, and achieve the effects of improving anti-tumor effects, reducing systemic toxicity, and improving safety

Pending Publication Date: 2021-10-22
CHENGDU MEDICAL COLLEGE
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Nevertheless, the therapeutic effects of these chemotherapy drugs still need to be further improved
[0004] On the other hand, the administration of chemotherapy drugs is likely to cause adverse reactions in the blood system, nausea and vomiting, diarrhea, hair loss, liver and kidney function damage and other toxic and side effects, which seriously affects the acceptance of patients.

Method used

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  • Application of combination of 5-fluorouracil and paclitaxel in preparation of medicine for treating breast cancer
  • Application of combination of 5-fluorouracil and paclitaxel in preparation of medicine for treating breast cancer
  • Application of combination of 5-fluorouracil and paclitaxel in preparation of medicine for treating breast cancer

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Experimental program
Comparison scheme
Effect test

Embodiment 1

[0042] Embodiment 1 The present invention treats the pharmaceutical composition of breast cancer

[0043] The pharmaceutical composition of the present invention consists of the following two components:

[0044] Component 1: 3 mg of 5-FU;

[0045] Component 2: 2 mg of PTX.

Embodiment 2

[0046] Embodiment 2 The present invention treats the dual drug-loaded liposome of breast cancer

[0047] Accurately weigh soybean lecithin (SPC, 6mg), cholesterol (2mg), DSPE-PEG2000 (2mg), and paclitaxel (2mg) in a 50mL eggplant-shaped flask, fully dissolve with 5mL chloroform, and rotate in a constant temperature water bath at 25°C ( 60rpm / min) for 30 minutes to form a uniform transparent film on the bottle wall, and leave it overnight to completely evaporate the organic solvent.

[0048] Precisely weigh 5-fluorouracil (3 mg) and dissolve it in 10 mL of PBS with pH 7.4, hydrate and dry the film, ultrasonicate in a water bath at 37°C for 15 min, and then probe with an ultrasonic cell disruptor for 5 min (power 100w, ultrasonic for 5 s, intermittent for 5 s), The double-loaded liposome suspension 5-FU / PTX Lps was obtained and stored at 4°C for future use.

Embodiment 3

[0049] Example 3 Polypeptide-modified dual-drug-loaded liposome for treating breast cancer according to the present invention

[0050] 1. Synthesis of DSPE-PEG-KLA

[0051] Dissolve DSPE-PEG-MAL in chloroform, then add KLA polypeptide dissolved in methanol to the DSPE-PEG-MAL solution, the molar ratio of DSPE-PEG-MAL to KLA polypeptide is 37:55.5. Under the protection of nitrogen, the mixed solution was stirred at room temperature and protected from light for 24 hours (the synthetic route is as follows: figure 1 shown). After confirming the completion of the DSPE-PEG-MAL reaction using thin layer chromatography, the organic solvent was removed using a rotary evaporator. The obtained white precipitate was washed three times with methanol, and the filter cake was collected by suction filtration to obtain DSPE-PEG-KLA.

[0052] 2. Preparation of peptide-modified dual drug-loaded liposomes

[0053] Accurately weigh soybean lecithin (SPC, 6mg), cholesterol (2mg), DSPE-PEG-KLA (...

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Abstract

The invention provides application of combination of 5-fluorouracil and paclitaxel in preparation of a medicine for treating breast cancer, and belongs to the field of pharmacy. The invention particularly provides a pharmaceutical composition for treating breast cancer. The composition is a preparation prepared by taking 5-fluorouracil and paclitaxel as active ingredients and adding a pharmaceutically acceptable carrier, wherein the mass ratio of the 5-fluorouracil to the paclitaxel is (2-4):2. According to the invention, it is found for the first time that when 5-fluorouracil and paclitaxel are combined in a specific ratio, the inhibition effect on triple negative breast cancer cells has a synergistic effect. Experimental results show that compared with a free drug and an unmodified double-drug-loading liposome which are used in a combined manner, the polypeptide modified double-drug-loading liposome provided by the invention has a remarkably improved in-vivo anti-tumor effect; and moreover, while the anti-tumor effect is improved, the polypeptide modified double-drug-loading liposome provided by the invention also reduces the systemic toxicity, improves the safety of tumor treatment, and has a wide application prospect.

Description

technical field [0001] The invention belongs to the field of pharmacy, and specifically relates to the use of 5-fluorouracil in combination with paclitaxel in preparing a medicine for treating breast cancer. Background technique [0002] Breast cancer has become the most common female malignant tumor in the world, and its morbidity and mortality are the first among female tumors, seriously threatening and endangering women's physical and mental health. Different types of breast cancer have significantly different biological characteristics and clinical manifestations. At present, immunohistochemical methods are mainly used clinically. According to estrogen receptor (ER), progesterone receptor (PR) and human epidermal growth factor receptor 2 (HER-2) detection results divide breast cancer into four molecular subtypes: luminal A type (ER positive or PR positive, HER-2 negative, low Ki67 expression), luminal B type (ER positive or PR positive, HER-2 is also positive), HER-2 ov...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/513A61K47/64A61K47/69A61P35/00A61K31/337
CPCA61K31/513A61K31/337A61P35/00A61K47/64A61K47/6911A61K2300/00
Inventor 吴敏陈天宇蒋漪纯
Owner CHENGDU MEDICAL COLLEGE
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