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Anti-tumor pharmaceutical composition containing rutin drug

An anti-tumor drug and composition technology, applied in the direction of drug combination, anti-tumor drug, medical preparation containing active ingredients, etc., can solve the problem of high risk of cardiovascular disease, lack of effective therapeutic drugs and intervention methods, and high risk question

Inactive Publication Date: 2017-09-01
任立群
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the most prominent chemotherapy toxicity of this type of drug is cardiotoxicity (Anthracycline-Induced Cardiotoxicity, AIC), which mainly manifests as severe acute, chronic, and delayed myocardial toxicity, which is dose-limiting.
Oeffinger KC et al [3] The study pointed out [New England Journal of Medicine in 2006], the problems of long-term survivors of breast cancer patients after chemotherapy: the mortality rate caused by cardiac causes is 8.2 times higher than that of normal people; the risk of heart failure is 15 times higher, and cardiovascular disease 10 times higher risk
[0007] The inventor tracked the relevant research progress and found that there is still a lack of effective therapeutic drugs and intervention methods for simultaneously protecting the cardiotoxicity of anthracycline drugs and enhancing the curative effect of anthracycline drug chemotherapy, which is still a technical blank in this field

Method used

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  • Anti-tumor pharmaceutical composition containing rutin drug
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  • Anti-tumor pharmaceutical composition containing rutin drug

Examples

Experimental program
Comparison scheme
Effect test

experiment example

[0062] The compositions were prepared according to the ratios in Table 1 below.

[0063] For the preparation of the liquid compositions in Examples 1 to 32, the compositions of the present invention with corresponding concentrations can be prepared into the same solution, and then used directly when applied; they can also be prepared into solutions with corresponding concentrations, and then carried out They can be mixed and used directly at the time of administration; they can also be administered after being mixed at the time of use, or administered to the subject separately, and the sequence of their administration is not limited.

[0064] For the preparation of the solid compositions in Examples 1-32, the medicines of corresponding quality can be mixed directly and taken at the same time; they can also be made into unit preparations and taken to the subject at the same time when administered, or successively Take them, but the sequence of their use is not limited.

[0065...

experiment example 1

[0076] Experimental example 1 in vitro test

[0077] 1.1.1 Effect of different ratios of rutin and pirarubicin compositions on the inhibitory rate of H9c2 cells (MTT method)

[0078] experiment method:

[0079] H9c2 cardiomyocytes were seeded in 96-well culture plates. When the cells grew to about 80% of the culture well area, different treatments were carried out according to the needs of the experiment: (1) 10, 30, 50, 70 and 100 μmol / L different concentrations of Rutin (Rutin) was pretreated for 1 hour, discarded, washed twice with PBS, and cultured with 5 μmol / L pirarubicin for 24 hours; L-pirarubicin was cultured for 24 hours; 8 replicate wells were set up for each treatment factor. After terminating the culture, add 10 μL MTT to each well, shake gently, and incubate at 37°C. Then measure cell inhibition rate=(1-OD value of experimental group / OD value of control group)×100%. The measurement results are shown in Table 2 and figure 1 .

[0080] Data statistics The SPS...

experiment example 2

[0125] Experimental Example 2 In vivo test

[0126] Protective effects of different ratios of rutin and pirarubicin compositions on acute cardiotoxicity (injury) in Wistar rats

[0127] Preparation of anthracycline acute cardiotoxicity model: According to the replication method of animal model of human disease and the method in the article "The protective effect of schisandrin B and dexrazine on doxorubicin-induced cardiotoxicity".

[0128] Medicines, reagents and animals:

[0129] Drugs: Pirarubicin Hydrochloride (THP, Shenzhen Wanle Co., Ltd.), Dexpropylimine for Injection (DZR, Jiangsu Osaikang Pharmaceutical Co., Ltd.), Rutin (Rutin, Nanjing Jingzhu Pharmaceutical Technology Co., Ltd.) .

[0130] Reagents: Rat serum brain natriuretic peptide BNP (MEXN-R0119), serum cardiac troponin T (MEXN-R099) and creatine kinase isoenzyme MB (MEXN-R0995) kits were purchased from Shanghai Meixuan Biotechnology Co., Ltd. company. Malondialdehyde (A003-1), lactate dehydrogenase LDH (A0...

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Abstract

Relating to the field of pharmacy, the invention in particular provides an anti-tumor pharmaceutical composition containing a rutin drug. The pharmaceutical composition is composed of a rutin drug and an anthracycline drug, wherein the rutin drug is rutin or troxerutin, and the anthracycline drug is epirubicin or pirarubicin. The pharmaceutical composition provided by the invention has better antitumor effect than anthracycline drugs, also effectively alleviates or avoids the cardiac toxicity of patients, and reduces the toxic and side effect of drugs.

Description

technical field [0001] The invention relates to the field of pharmacy, in particular to an antitumor pharmaceutical composition with synergistic effect and cardiotoxicity protection. Background technique [0002] Tumor disease is currently one of the frequently-occurring diseases of human beings, which has brought great pain to patients. At present, chemotherapy is the main treatment for tumors. Pain other than the disease itself, mild such as headache, nausea, fatigue, severe such as hair loss, liver and kidney and heart toxicity and so on. [0003] Anthracyclines, such as epirubicin and pirarubicin, have been widely used in the treatment of hematological malignancies and solid tumors, such as breast cancer, lymphoma, and acute leukemia. It has good effect on anti-tumor. The 2014 "NCCN Guidelines for Breast Cancer" recommended that the preferred adjuvant chemotherapy regimen for breast cancer is AC×4→T(P)×4 (doxorubicin, epirubicin, pirarubicin / cyclophosphamide-paclitaxel...

Claims

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Application Information

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IPC IPC(8): A61K31/7048A61P35/00A61P9/00A61K31/704
CPCA61K31/704A61K31/7048A61K2300/00
Inventor 任立群王亚帝张洋胡彦武李相军李敏
Owner 任立群
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