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Anti-tumor pharmaceutical composition containing total flavonoids of apocynum venetum leaves

The technology of an anti-tumor drug and a composition is applied in the field of anti-tumor drug compositions containing total flavonoids from apocynum leaves, and can solve the problems of lack of effective therapeutic drugs and intervention methods for chemotherapy efficacy, increased mortality, and high risk.

Active 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.
Research by Oeffinger KC and others pointed out [New England Journal of Medicine in 2006] that the long-term survivors of breast cancer patients after chemotherapy have problems: 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, 10 times higher risk of cardiovascular disease
[0007] The study found that there is still a lack of effective therapeutic drugs and intervention methods for both protecting the cardiotoxicity of anthracycline drugs and enhancing the efficacy of anthracycline drug chemotherapy, and its systemic treatment is still blank.

Method used

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  • Anti-tumor pharmaceutical composition containing total flavonoids of apocynum venetum leaves
  • Anti-tumor pharmaceutical composition containing total flavonoids of apocynum venetum leaves
  • Anti-tumor pharmaceutical composition containing total flavonoids of apocynum venetum leaves

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0050] The preparation of embodiment 1 Apocynum leaf total flavonoids

[0051] Preparation:

[0052] a) Grinding the dried Apocynum leaves through a 20-50 mesh sieve to form a medicinal powder, heating and refluxing with 10 times the amount of 75% ethanol for 2 hours, extracting twice, combining the extracts, filtering, recovering the ethanol, and concentrating to obtain Concentrate;

[0053] b) Purify the concentrate in step a with D101 macroporous resin, wash with water, then elute with 50% ethanol, combine and concentrate the filtrates to obtain the final product.

[0054] Detection method: determine the content of total flavonoids in the extract by spectrophotometry;

[0055] c) Accurately weigh the rutin sample, dissolve it with 30% ethanol, accurately measure different volumes of the solution, measure the absorbance at 506 nm, and draw a standard curve.

[0056] d) Precisely weigh 0.0193g of total flavonoids of Apocynum basil leaves and place in a 50ml volumetric flas...

Embodiment 2～13

[0063] Examples 2-13 Examples and Experimental Examples of Antitumor Pharmaceutical Compositions Containing Total Flavonoids of Apocynum Folium

[0064] Each composition was prepared according to the proportions in Table 2 below.

[0065] For the preparation of the liquid compositions in Examples 2 to 13, 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 made into solutions of corresponding concentrations respectively, 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.

[0066] For the preparation of the solid compositions in Examples 2-13, the medicines of the corresponding quality can be directly mixed and taken at the same time; they can also be prepared ...

experiment example 1

[0077] Experimental example 1 in vitro test

[0078] 1.1.1 Effect of different proportions of total flavonoids of Apocynum leaf and pirarubicin composition on H9c2 cell inhibition rate (MTT method)

[0079] experiment method:

[0080] H9c2 cardiomyocytes were inoculated in a 96-well culture plate. 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) Apocynum leaves with different concentrations of 30, 60 and 90 μg / ml were given respectively Total flavonoids (TFF) was pretreated for 1 hour, discarded, washed twice with PBS, and then cultured with 3.32 μg / ml pirarubicin for 24 hours; μg / ml 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 the cell inhibition rate, and the measurement results are shown in Table 3 and figure 2 .

[008...

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Abstract

Relating to the field of pharmacy, the invention in particular provides an anti-tumor pharmaceutical composition containing total flavonoids of apocynum venetum leaves. The pharmaceutical composition is composed of total flavonoids of apocynum venetum leaves and an anthracycline drug, wherein the anthracycline drug is pirarubicin or epirubicin. 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 effects.

Description

technical field [0001] The invention relates to the field of pharmacy, in particular to an antitumor pharmaceutical composition containing total flavonoids of apocynum leaves 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, epir...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K36/24A61P35/00A61P9/00A61K31/704
CPCA61K31/704A61K36/24A61K2300/00
Inventor 任立群李相军王亚帝张洋孙波胡彦武
Owner 任立群
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