A kind of 2,4-dinitrophenol fat emulsion and its preparation method and application

A technology of dinitrophenol and fat emulsion, applied in the field of medicine, can solve the problems of high cost, inability to stop treatment in time, low flexibility and the like

Active Publication Date: 2021-09-10
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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  • A kind of 2,4-dinitrophenol fat emulsion and its preparation method and application

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 water for injection, heat to 60° C. to dissolve, and obtain an aqueous phase. Put the water phase and oil into the mixer at the same time, stir at 10000r / min for 5min, stir into colostrum, homogenize the colostrum with high pressure milk (800bar, 8 times), then 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 and put it in a beaker, heat 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 water for injection, heat to 60° C. to dissolve, and obtain an aqueous phase. Put the water phase and oil into the mixer at the same time, stir at 10000r / min for 5min, stir into colostrum, homogenize the colostrum with high pressure milk (800bar, 8 times), then 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 water for injection, heat to 60° C. to dissolve, and obtain an aqueous phase. Put the water phase and oil into the mixer at the same time, stir at 10000r / min for 5min, stir into colostrum, homogenize the colostrum with high pressure milk (800bar, 8 times), then 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 a kind of 2,4-dinitrophenol fat emulsion, every 1L of 2,4-dinitrophenol fat emulsion is made by the raw material of following weight: 2,4-dinitrophenol or its salt 0.1~ 20g, 50-500g oil for injection, 1-100g emulsifier, 5-100g isotonic regulator, and the balance is water for injection. The fat emulsion has good stability, can be stored for a long time without stratification, and does not precipitate drug precipitation, thereby ensuring the drug efficacy and safety of the fat emulsion when used. In addition, the fat emulsion does not add organic reagents during the preparation process, avoiding the residue of organic reagents in the final product and the stimulation of surfactants, increasing product safety and patient compliance; at the same time, avoiding the application of organic reagents in the production process, The preparation process can be reduced, and the production efficiency and safety can be improved. The fat emulsion is administered by intravenous infusion, which can stabilize the blood concentration, thereby increasing safety. In addition, fat emulsion has certain liver targeting, which can improve its distribution in the liver, thereby improving its curative effect on liver lesions.

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 Patents(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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