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A pharmaceutical composition for preventing and treating cardiotoxicity of anthracycline antibiotics and its application

A cardiotoxicity and anthracycline technology, which is applied in the field of pharmaceutical compositions for preventing and treating cardiotoxicity of anthracyclines, can solve the problems of use restriction, influence on the activity of adriamycin on malignant tumors, high price, etc., and achieve cardiotoxicity protection and prevention. and cardiotoxicity, reducing cardiotoxicity

Active Publication Date: 2022-03-04
CHINA PHARM UNIV +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, studies have found that such drugs may cause severe myelosuppression, and may affect the activity of doxorubicin on certain malignant tumors. Therefore, the American Association of Clinical Oncology, Chemotherapy and Radiation Therapy Specialists has made a corresponding review on the clinical use of dexrazoxane Restrictions; secondly, drugs such as dexrazoxane are expensive, and can only be slowly pushed statically after being dissolved in lactic acid solution, and their use is greatly restricted

Method used

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  • A pharmaceutical composition for preventing and treating cardiotoxicity of anthracycline antibiotics and its application
  • A pharmaceutical composition for preventing and treating cardiotoxicity of anthracycline antibiotics and its application
  • A pharmaceutical composition for preventing and treating cardiotoxicity of anthracycline antibiotics and its application

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Experimental program
Comparison scheme
Effect test

Embodiment 1

[0030] Embodiment 1, glycyrrhizin submicroemulsion

[0031] A submicron emulsion of glycyrrhizin, comprising the following components per 100mL submicron emulsion: 0.5g of liquiritinin phospholipid complex, 5.0g of soybean oil, 0.40g of lecithin, 0.40g of poloxamer 188, 0.20g of Tween 80 , 0.024g sodium oleate, 1.0g glycerol and distilled water added to 100mL, wherein the glycyrrhizin-phospholipid complex is used as a prodrug to increase the solubility of glycyrrhizin in soybean oil, and the molar ratio of glycyrrhizin and phospholipids is 1:1.

[0032] The steps for preparing the above-mentioned liquiritinin submicron emulsion are as follows: Weigh 0.5g of liquiritinin-phospholipid complex and add it to 5.0g of soybean oil as the oil phase, and heat in a water bath at 60°C. Weigh 0.40 g of lecithin, 0.40 g of poloxamer 188, 0.20 g of Tween 80, 0.024 g of sodium oleate, and 1.0 g of glycerin in an appropriate amount of distilled water at 60° C. as the water phase. Add the wa...

Embodiment 2

[0033] Embodiment 2, glycyrrhizin submicroemulsion

[0034] A submicron emulsion of glycyrrhizin is prepared from the following oil phase and water phase.

[0035] Oil phase preparation: Dissolve liquiritigenin, egg yolk phospholipid and oleic acid in absolute ethanol, add the ethanol solution to medium chain triglyceride (MCT) and soybean oil mixed oil, and remove ethanol by rotary evaporation to obtain the oil phase.

[0036] Aqueous phase preparation: weigh glycerin and poloxamer 188, add purified water to dissolve to obtain an aqueous phase.

[0037] The obtained water phase and oil phase were heated at 60° C., the water phase was slowly added to the oil phase, and the colostrum was prepared by high-speed shearing (12000 r / min) for 3 minutes. Add water to make up to 100ml, then high-pressure homogenize the colostrum (1000bar, cycle 10 times) to obtain a submicron emulsion solution, and adjust the pH value to 4.5-5.0.

Embodiment 3

[0038] Embodiment 3, glycyrrhizin submicroemulsion

[0039]Take liquiritigenin, add the prescribed amount of propylene glycol, put it in the liquid preparation tank, stir until it is completely dissolved, add 90% of the prescribed amount of water for injection, stir evenly, and adjust the pH value to 5.0 with 0.1mol / L hydrochloric acid solution or sodium hydroxide solution , add water for injection to the full amount, the measured content is qualified, after ultrafiltration with a hollow fiber ultrafiltration membrane with a molecular weight cut-off of 10kDa, the content is tested again to be qualified, filled in ampoules under aseptic conditions, and sterilized by autoclaving at 121°C and 97kPa for 15 minutes. have to.

[0040] Liquiritigenin submicron emulsion samples were diluted with ultrapure water 1:5000, and the particle size and polydispersity index were measured by Zetasizer Nano ZS90 analyzer (Malvern Instruments Co., Worcestershire, UK).

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Abstract

The invention relates to the technical field of traditional Chinese medicine, in particular to a pharmaceutical composition for preventing and treating cardiotoxicity of anthracycline antibiotics and an application thereof. Tests have proved that liquiritigenin can reduce the cardiotoxicity caused by doxorubicin, reduce the level of myocardial enzymes, improve the inflammatory response, thereby reducing the lethality caused by doxorubicin cardiotoxicity, and the present invention has a significant effect on the cardiotoxicity induced by doxorubicin protective effect. The invention can be used to prevent and alleviate cardiotoxicity induced by anthracycline antibiotics, and has clinical practicability.

Description

technical field [0001] The invention relates to the technical field of traditional Chinese medicines, in particular to a new application of liquiritigenin in resisting the cardiotoxicity of anthracycline antibiotics and a pharmaceutical composition for preventing and treating the cardiotoxicity of anthracycline antibiotics. Background technique [0002] Doxorubicin, also known as doxorubicin (DOX), is an anthracycline antibiotic extracted from the light gray strain of Streptomyces lanusum, which can intercalate between DNA base pairs and tightly bind to DNA, preventing DNA dependence The role of RNA polymerase interferes with the transcription process, inhibits the production of RNA, and also prevents DNA replication. It is a non-specific drug for the cell cycle. Since its discovery in the 1860s, due to its strong anticancer effect and high chemotherapy index, doxorubicin has been one of the most effective antitumor drugs, and it is widely used clinically in various diseases...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/353A61K45/06A61P9/00A61K31/704
CPCA61K31/353A61K45/06A61P9/00A61K31/704A61K2300/00
Inventor 蔡挺蔡宝昌史长灿
Owner CHINA PHARM UNIV
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