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Disulfiram lipid microsphere preparation for injection for treating tumor and preparation method thereof

A technology for lipid disulfiram and injection, which is applied in the directions of antitumor drugs, inactive ingredients of oil/fat/wax, powder delivery, etc., can solve the problem of low blood concentration of disulfiram, and achieve sterilization stability Good, high drug loading, and the effect of improving drug bioavailability

Inactive Publication Date: 2012-02-01
SHENYANG PHARMA UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

In the blood, DS will quickly form mixed disulfides with the sulfhydryl groups of endogenous proteins or be reduced to DDC by the glutathione reductase system in red blood cells, but the blood concentration of disulfiram remains the same after a single administration. below detection limit

Method used

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  • Disulfiram lipid microsphere preparation for injection for treating tumor and preparation method thereof
  • Disulfiram lipid microsphere preparation for injection for treating tumor and preparation method thereof
  • Disulfiram lipid microsphere preparation for injection for treating tumor and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0039] The most preferred disulfiram lipid microsphere formulation of the present invention:

[0040] Take 20.0g of disulfiram, 100.0g of medium-chain triglycerides, 18.0g of lecithin, 5.0g of vitamin E, and 5.0g of polyethylene glycol phospholipids, heat to 70°C under nitrogen protection, and stir for about 10 minutes to make The various lipid compounds added are fully dissolved and dissolved evenly; take another 800ml of water for injection, add 22.5g of glycerin, 1.0g of sodium oleate and 5.0g of amino acid block copolymer, stir and dissolve, adjust the pH to 5.0-8.0, and dissolve evenly ;Under the condition of nitrogen protection, the oil solution containing the drug is added to the aqueous solution of glycerin and sodium oleate under shearing and stirring to make colostrum, and the total amount is adjusted to 1000ml, and the high-pressure homogenizer is homogenized 6-15 times , the homogenization pressure is about 80MPa, and the particle size ranges from 180nm to 250nm, f...

Embodiment 2

[0045] Disulfiram lipid microsphere formulation with the lowest disulfiram content

[0046] Take 1.0g of disulfiram, 100.0g of soybean oil, 18.0g of hydrogenated egg yolk lecithin, and 5.0g of vitamin E. Under nitrogen protection, heat to 70°C and stir for about 10 minutes to fully dissolve the various lipid compounds added. Dissolve evenly; take another 850ml of water for injection, add 22.5g of glycerin and 1.0g of sodium oleate, stir to dissolve, adjust the pH to 5.0-8.0, and dissolve evenly; Add glycerin and sodium oleate aqueous solution to make colostrum, and adjust the total amount to 1000ml with water for injection, homogenize 6-15 times with a high-pressure homogenizer, the homogenization pressure is about 80MPa, and the particle size ranges from 180nm-250nm , filtered, subpackaged, fed with nitrogen, sealed, 121 ° C rotary sterilization for 10 minutes, after passing the light inspection, packaged, and stored below 25 ° C.

[0047] The lecithin described in this embo...

Embodiment 3

[0049] Disulfiram lipid microsphere formulation with the highest disulfiram content

[0050] Take 40.0g of disulfiram, 150.0g of garlic oil, 24.0g of egg yolk lecithin, and 3.0g of vitamin E. Under nitrogen protection, heat to 70°C and stir for about 10 minutes to fully dissolve the various lipid compounds added. Uniformly; take another 800ml of water for injection, add 22.5g of glycerin and 1.0g of sodium oleate, stir to dissolve, adjust pH5.0-8.0, dissolve evenly; under the condition of nitrogen protection, add the oil solution containing the drug under shearing and stirring In the aqueous solution of glycerin and sodium oleate, colostrum is made, and the total amount is adjusted to 1000ml with water for injection, homogenized by a high-pressure homogenizer for 6-15 times, the homogenization pressure is about 80MPa, and the particle size ranges from 180nm to 250nm. Filter, sub-package, inject nitrogen, seal, 121 ℃ rotation sterilization for 10 minutes, after passing the ligh...

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Abstract

The invention relates to a disulfiram lipid microsphere preparation for injection for treat tumor and a preparation method thereof, belonging to the field of pharmaceutical preparations. The disulfiram lipid microsphere preparation is prepared from the following components in mass percent: 0.1-4% of disulfiram or derivatives thereof, 5-30% of vegetable oil, 0.6-3% of lecithin, 0-4% of polyethylene glycol phospholipid or derivatives thereof, 0-4% of amino acid block copolymer, 0-0.6% of oleic acid or oleate, 0-1% of antioxidant, 0-0.4% of complexing agent, 1-3% of glycerol and balance of water for injection. According to the invention, due to the introduction of the polyethylene glycol phospholipid or derivatives thereof and the amino acid block copolymer, a fat emulsion can be kept in the blood for a longer time, an additional passive target function on tumor is provided for the medicament, the stability of the fat emulsion preparation is improved, and the effect of disulfiram on treating tumor is enhanced.

Description

technical field [0001] The invention relates to a disulfiram lipid microsphere preparation for injection for treating tumors and a preparation method thereof, belonging to the field of pharmaceutical preparations. Background technique [0002] Disulfiram (disulfiram, DS), also known as tetraethylthiuram disulfide, disulfiram, was first synthesized in 1881, and was originally used as a catalyst for rubber vulcanization in the rubber industry; in the 1830s, DS first As a drug, it is used as a treatment for scabies; later, it was found that disulfiram has a strong chelation effect on copper ions, which can reduce the activity of copper-containing respiratory enzymes, and intestinal worms are extremely sensitive to disulfiram, so disulfiram Disulfiram is used as an insect repellent again; in 1948, two doctors in Copenhagen, Hald and Jacobsen, accidentally discovered that drinking a small amount of alcohol after taking the insect repellent disulfiram could immediately cause facia...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/14A61K31/145A61K47/34A61K47/44A61P35/00
Inventor 唐星何海冰张宇吴春福杨静玉
Owner SHENYANG PHARMA UNIVERSITY
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