2,4-dinitrophenol fat emulsions and preparation method and application thereof

A technology of dinitrophenol and fat emulsion, applied in the field of medicine, can solve the problems of complicated production process of sustained-release preparations, inability to stop treatment in time, low flexibility, etc., and achieves increased product safety, patient compliance, and blood drug concentration. Easier to control and reduce the effect of the preparation process

Active Publication Date: 2019-10-08
CHENGDU MEDICAL COLLEGE
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

But this slow-release preparation also has some shortcomings clinically: (1) the flexibility of dose adjustment is low clinically, and when encountering relatively large side effects, the treatment cannot be stopped in time; (2) the production process of the slow-release preparation is complicated, high cost

Method used

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  • 2,4-dinitrophenol fat emulsions and preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0039] Embodiment 1, the preparation of 2,4-dinitrophenol fat emulsion of the present invention

[0040] Preparation of 1L 2,4-dinitrophenol fat emulsion: Weigh 100g of soybean oil and put it in a beaker, heat it to 60°C, add 12g of lecithin and 3g of 2,4-dinitrophenol into the soybean oil, 5000r / min high speed Stir to obtain an oily phase. Add 22.5 g of glycerin into the water for injection, and heat to 60° C. to dissolve to obtain an aqueous phase. Put the water phase and the oil at the same time into the mixer, stir at 10000r / min for 5min, stir into colostrum, homogenize the colostrum with high-pressure milk (800bar, 8 times), adjust the pH value to 6.5 with sodium hydroxide solution, and pack , 115 ° C autoclave for 30 minutes, you can.

Embodiment 2

[0041] Embodiment 2, the preparation of 2,4-dinitrophenol fat emulsion of the present invention

[0042] Preparation of 1L 2,4-dinitrophenol fat emulsion: Weigh 200g of soybean oil, put it in a beaker, heat to 60°C, add 12g of lecithin and 3g of 2,4-dinitrophenol into the soybean oil, and run at a high speed of 5000r / min Stir to obtain an oily phase. Add 22.5 g of glycerin into the water for injection, and heat to 60° C. to dissolve to obtain an aqueous phase. Put the water phase and the oil at the same time into the mixer, stir at 10000r / min for 5min, stir into colostrum, homogenize the colostrum with high-pressure milk (800bar, 8 times), adjust the pH value to 6.5 with sodium hydroxide solution, and pack , 115 ° C autoclave for 30 minutes, you can.

Embodiment 3

[0043] Embodiment 3, the preparation of 2,4-dinitrophenol fat emulsion of the present invention

[0044]Preparation of 1L 2,4-dinitrophenol fat emulsion: Weigh 300g of soybean oil and put it in a beaker, heat it to 60°C, add 12g of lecithin and 3g of 2,4-dinitrophenol into the soybean oil, 5000r / min high speed Stir to obtain an oily phase. Add 22.5 g of glycerin into the water for injection, and heat to 60° C. to dissolve to obtain an aqueous phase. Put the water phase and the oil at the same time into the mixer, stir at 10000r / min for 5min, stir into colostrum, homogenize the colostrum with high-pressure milk (800bar, 8 times), adjust the pH value to 6.5 with sodium hydroxide solution, and pack , 115 ° C autoclave for 30 minutes, you can.

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Abstract

The invention provides 2,4-dinitrophenol fat emulsions. Each 1L of the 2,4-dinitrophenol fat emulsions is prepared from the following raw materials by weight: 0.1-20g of the 2,4-dinitrophenol or saltof the 2,4-dinitrophenol, 50-500g of oil for injection, 1-100g of an emulgator, 5-100g of an isoosmotic adjusting agent and the balance of water for injection. The 2,4-dinitrophenol fat emulsions aregood in stability performance, can be kept for a long time and stratification does not occur, drug precipitation does not be precipitated, and drug function and safety of the fat emulsions during using are guaranteed. In addition, an organic reagent is not added into the fat emulsions in the preparation process, residue of the organic reagent of a final product and stimulation function of a surface active agent are avoided, and product safety and patient adaptability are increased; and meanwhile, application of the organic reagent in the production process is avoided, preparation process can be reduced, and the production efficiency and safety are improved. According to the 2,4-dinitrophenol fat emulsions, drug administration is carried out through intravenous drip, blood concentration canbe steady, and thus the safety is increased. In addition, the fat emulsions have certain hepar targeting ability, can improve distribution of the fat emulsions in hepar, and thus improves therapeuticeffect of the fat emulsions for hepatic pathological changes.

Description

technical field [0001] The invention belongs to the field of medicine, and in particular relates to a 2,4-dinitrophenol fat emulsion and a preparation method and application thereof. Background technique [0002] 2,4-Dinitrophenol (2,4-DNP) is a yellow compound that has historically been used in the manufacture of dyes, explosives, and fungicides. It was also used as an anti-obesity drug early in the last century due to its ability to uncouple mitochondrial oxidative phosphorylation. The compound was banned by the U.S. Food and Drug Administration in 1938 because of its potentially fatal side effects, including hyperthermia, cataracts, agranulocytosis, liver toxicity, kidney toxicity, and cardiotoxicity. At present, more and more evidence shows that 2,4-dinitrophenol plays an important role in protecting neurons from neurodegeneration and enhancing neuroplasticity. Appropriate doses of 2,4-dinitrophenol can induce mild uncoupling of mitochondria connections and promote neu...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/107A61K9/19A61K47/44A61K31/06A61P1/16A61P35/00A61P3/10A61P3/00
CPCA61K9/0019A61K9/107A61K9/19A61K31/06A61K47/44A61P1/16A61P3/00A61P3/10A61P35/00
Inventor 张全许小红叶静鲍莎朱昱锦
Owner CHENGDU MEDICAL COLLEGE
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