Compound and application thereof

A compound and drug compound technology, which is applied in the direction of drug combination, medical preparations with non-active ingredients, medical preparations containing active ingredients, etc., can solve the problems of multi-drug resistance and toxicity, and achieve multi-drug resistance Effects of improving and promoting cell apoptosis and good application prospects

Active Publication Date: 2022-04-15
CHINA PHARM UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0006] The purpose of the present invention is to overcome the problems of multi-drug resistance and high toxicity caused by a single drug treatment of liver cancer, and develop a method for the combination of two drug micelles for the treatment of liver cancer, so as to realize the attenuated and synergistic treatment of liver cancer

Method used

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  • Compound and application thereof
  • Compound and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0041] Weigh 0.15mmol of cholic acid and dissolve in N,N-dimethylformamide, 0.1mmol of 1-(3-dimethylaminopropyl)-3-ethylcarbodiimide and 0.1mmol of 1-hydroxybenzotriazole Dissolve in dichloromethane respectively, mix the three, stir for 1 hour, then dissolve 0.1mmol methoxypolyethylene glycol amine in dichloromethane, add dropwise to the above reaction solution, continue to react for 24 hours, add excess The product was precipitated with glacial diethyl ether, vacuum-dried overnight after suction filtration. Dissolved in pure water, dialyzed for 24 hours, and freeze-dried to obtain the cholic acid-polyethylene glycol material. The yield was 83.5%.

Embodiment 2

[0043] Weigh 24mg of cholic acid-polyethylene glycol, 56mg of vitamin E polyethylene glycol succinate, and 4mg of paclitaxel, mix and dissolve in dichloromethane, and evaporate the organic solvent at 45°C to form a film on the bottle wall. Add 5 mL of pure water to hydrate by rotating at 35°C, sonicate for 15 min with an ultrasonic cell disruptor at 200 W, and pass through the membrane to obtain paclitaxel micelles. The measured particle size is 281.62±2.66nm, PDI is 0.069±0.018, and zeta potential is -2.59±0.197mV. The encapsulation efficiency and drug loading were 28.78±0.049% and 1.42±0.025%, respectively.

Embodiment 3

[0045] Weigh 40mg of cholic acid-polyethylene glycol, 40mg of vitamin E polyethylene glycol succinate, and 4mg of paclitaxel, mix and dissolve in dichloromethane, and evaporate the organic solvent at 45°C to form a film on the bottle wall. Add 5 mL of pure water to hydrate by rotating at 35°C, sonicate for 15 min with an ultrasonic cell disruptor at 200 W, and pass through the membrane to obtain paclitaxel micelles. The measured particle size is 169.07±7.31nm, PDI is 0.163±0.04, and zeta potential is -0.787±0.555mV. The encapsulation efficiency and drug loading were 76.35±1.76% and 3.68±0.081%, respectively.

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Abstract

The invention relates to the field of new dosage forms and new technologies of medicines, in particular to a compound and application thereof, and the compound comprises two medicines, namely paclitaxel and bufalin. As the two drugs are poor in water solubility, the two drugs are respectively encapsulated in carriers of cholic acid-polyethylene glycol/vitamin E polyethylene glycol succinate to form mixed polymer micelles, and then the mixed polymer micelles are combined to treat liver cancer. The combined application of the paclitaxel micelles and the bufalin micelles improves the problems of drug resistance of paclitaxel and high toxicity of bufalin, and results of toxicity reduction and efficacy enhancement are generated.

Description

technical field [0001] The present invention relates to the field of new drug dosage forms and new technologies, in particular to a compound and its application, in particular to a combination of two drug micelles for the treatment of liver cancer, the two drugs are paclitaxel and Toad poison spirit. The micellar carrier material is cholic acid-polyethylene glycol / vitamin E polyethylene glycol succinate. Background technique [0002] Hepatocellular carcinoma has become one of the most common malignant tumors in the world, and its morbidity and mortality have gradually increased in recent years. According to the statistics of the World Health Organization, liver cancer is the sixth most common tumor in the world, and the death rate related to liver cancer ranks third among all cancers in 2020, with a mortality rate of about 8.3%. Rapid development and poor prognosis are its main features. Surgical resection is the most important means to achieve radical treatment of liver ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/107A61K31/585A61K47/22A61K47/28A61P1/16A61P35/00A61K31/337
CPCA61K9/1075A61K31/337A61K31/585A61K47/22A61K47/28A61P1/16A61P35/00A61K2300/00
Inventor 吕慧侠张振海刘雨嘉
Owner CHINA PHARM UNIV
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