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Etoposide long-circulating emulsion and preparation method thereof

A technology of etoposide and long-term etoposide, applied in the field of etoposide long-circulating emulsion and its preparation, can solve problems such as difficulty in drug loading, and achieve the advantages of avoiding drug degradation, reducing vascular irritation and potential toxicity, and prolonging distribution time. Effect

Inactive Publication Date: 2011-11-23
TIANJIN INSTITUTE OF PHARMA RESEARCH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0009] Another object of the present invention is to provide the etoposide long-circulation submicroemulsion lipid carrier, which can overcome the difficulty of drug loading of drugs with poor water-solubility and fat-solubility, has high encapsulation efficiency, and the preparation can be stored stably

Method used

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  • Etoposide long-circulating emulsion and preparation method thereof
  • Etoposide long-circulating emulsion and preparation method thereof
  • Etoposide long-circulating emulsion and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0046] Add 1.0 g of lecithin, 0.02 g of PEG-DSPE, 0.05 g of oleic acid, and 0.01 g of etoposide into 10 g of soybean oil, and heat in an ultrasonic water bath (40° C.) to dissolve to obtain an oil phase. Take 2.25g of glycerin and dissolve it in 70ml of water for injection as the water phase. In a water bath at 50°C, add the oil phase to the water phase, stir while adding, and cut at 15,000rpm for 20min to obtain colostrum, adjust the pH to about 4.5-5, and make up the injection Water to 100ml, in a microfluidizer, the pressure 80MPa milk evenly 5 times, filling, nitrogen gas, melting seal, 121 ℃ rotary autoclaving for 10 minutes to obtain the final milk.

[0047] Average particle size = 193.7nm, PI = 0.092, encapsulation efficiency = 95.8%

Embodiment 2

[0049] Take 1.2 g of soybean lecithin, 0.1 g of PEG-DSPE, 0.10 g of oleic acid, and 0.05 g of etoposide, add them to 20 g of soybean oil, and heat them in an ultrasonic water bath (50° C.) to dissolve to obtain an oil phase. Take 2.25g of glycerin and dissolve it in 70ml of water for injection as the water phase. In a water bath at 60°C, add the oil phase to the water phase, stir while adding, and cut at 15,000 rpm for 20 minutes to obtain colostrum. Adjust the pH to about 4.5-5, and make up the injection Water to 100ml, in a microfluidizer, the pressure 80MPa milk evenly 5 times, filling, nitrogen gas, melting seal, 121 ℃ rotary autoclaving for 10 minutes to obtain the final milk.

[0050] Average particle size = 196.9nm, PI = 0.052, encapsulation efficiency = 96.7%

Embodiment 3

[0052] Get soybean oil and MCT, prepare mixed liquid oil 20g according to 1:1, get soybean lecithin 1.4g, PEG-DSPE0.4g, oleic acid 0.05g, etoposide 0.1g join in above-mentioned mixed oil phase, ultrasonic water bath heating ( 50°C) to obtain an oily phase. Take 2.25g of glycerin and dissolve it in 70ml of water for injection as the water phase. In a water bath at 70°C, add the oil phase to the water phase, stir while adding, and cut at 15,000rpm for 20min to obtain colostrum, adjust the pH to about 4.5-5, and make up the injection Water to 100ml, in a microfluidizer, the pressure 80MPa milk evenly 5 times, filling, nitrogen gas, melting seal, 121 ℃ rotary autoclaving for 10 minutes to obtain the final milk.

[0053] Average particle size = 191.7nm, PI = 0.082, encapsulation efficiency = 97.8%

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Abstract

The invention belongs to the field of medicinal preparations, and relates to an etoposide long-circulating emulsion for injection, and a preparation method thereof. The etoposide long-circulating emulsion comprises etoposide, fluid oil, emulsifiers, polyethylene glycol (PEG) modified esters and the like, and has the characteristics of high entrapment rate, good stability and low toxicity. The etoposide long-circulating emulsion improves the solubility and the stability of etoposide, reduces irritation effects of etoposide on blood vessels, prolongs cycle time of etoposide in blood, and improves distribution of etoposide in vivo thus improves drug curative effects. The preparation method of the etoposide long-circulating emulsion solves the carrying problems of drugs with poor water-solubility and fat-solubility and realizes stable preservation and no drug precipitation. The preparation method has the characteristics of simple process, low cost and good applicability for industrializedproduction.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, and relates to an etoposide long-circulation emulsion and a preparation method thereof. More specifically, the invention relates to a polyethylene glycol (PEG)-modified, which can avoid the reticuloendothelial system in the body. Etoposide long-circulation emulsion capable of being phagocytized and stored stably and its preparation method. technical background [0002] Etoposide (Etoposide), also known as etoposide, etoposide, VP-16, is a sugar metabolite of podophyllotoxin, a cell cycle-specific antineoplastic drug, acting on DNA topoisomerase II , forming a drug-enzyme-DNA stable reversible complex, hindering DNA repair and exerting an anti-tumor effect. At different concentrations, etoposide has different effects on cell division. High concentration (≥10 μg / mL) etoposide dissolves cells entering mitosis, while low concentration (0.3-10 μg / mL) inhibits cells entering mitosis early s...

Claims

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Application Information

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IPC IPC(8): A61K9/107A61K31/7048A61K47/44A61K47/34A61P35/00A61P35/02
Inventor 王杏林尹东东司端运陆榕
Owner TIANJIN INSTITUTE OF PHARMA RESEARCH
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