Glucose iodine derivative, preparation method thereof and application thereof in pharmacy

A technology of glucose and derivatives, applied in the field of pharmaceutical preparations and sugar iodides, can solve problems such as activity decline, affecting genetic information proteins, cell death, etc., and achieve good clinical application prospects

Active Publication Date: 2014-06-04
SUZHOU HARMONY BIOTECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

At the same time, it also causes the activity of glucose-6-phosphate dehydrogenase and lactate dehydrogenase-alkaline phosphatase to decrease

Method used

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  • Glucose iodine derivative, preparation method thereof and application thereof in pharmacy
  • Glucose iodine derivative, preparation method thereof and application thereof in pharmacy
  • Glucose iodine derivative, preparation method thereof and application thereof in pharmacy

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0033] Example 1 The preparation of 3,4,6-triacetyl-D-glucose iodine

[0034] Disperse 5.45g of 3,4,6-triacetyl-D-glucal, 4.39g of copper sulfate and 6.09g of iodine in 120ml of acetic acid and stir at 80°C for 4 hours. Cool to 25°C and concentrate under reduced pressure to 10ml. The residue was diluted with 250ml of ethyl acetate, and the solution was neutralized to pH=7 with saturated aqueous sodium bicarbonate solution, then washed with 50ml of saturated aqueous sodium thiosulfate solution, and finally washed with water. The organic phase was dried with anhydrous sodium sulfate, then filtered, concentrated under reduced pressure to a volume of 8 ml, and finally crystallized with 30 ml of ethanol at 5°C to finally obtain 7.74 g of 3,4,6-triacetyl-D-glucose iodine.

[0035] product testing:

[0036] 1. Melting point. The melting point is 107°C, which is consistent with the literature value (108°C);

[0037] 2. GC: 98.55%.

[0038] testing method:

[0039] Accurately w...

Embodiment 2

[0046] Example 2 Preparation of 3,4,6-triacetyl-D-glucose iodine spray

[0047] Dissolve 2 g of 3,4,6-triacetyl-D-glucose iodine in 500 ml of ethanol, fully dissolve, then add 200 ml of glycerin and 300 ml of water, mix well and put it into a 30 ml spray bottle to obtain 30 bottles.

Embodiment 3

[0048] Example 3 Preparation of 3,4,6-triacetyl-D-glucose iodine ointment

[0049] Oil phase components: 70g glyceryl stearate, 100g stearic acid, 100g liquid paraffin, 120g white vaseline and water phase components: 1g ethylparaben, 119g glycerin were dissolved in 480ml distilled water, heated to 80°C respectively, Add the melted oil phase components into the water phase components, stir for 30 minutes, cool to 25° C., add 10 g of 3,4,6-triacetyl-D-glucose iodine, and stir evenly to obtain 1000 g of ointment.

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Abstract

The invention provides a 3, 4, 6-substituted-D-glucose iodine derivative and a preparation method and application thereof. A drug is prepared from the 3, 4, 6-substituted-D-glucose iodine derivative as an active component and a medicinal auxiliary material. Bactericidal tests of the 3, 4, 6-substituted-D-glucose iodine derivative on pseudomonas aeruginosa, staphylococcus aureus and escherichia coli are performed, and results show that the 3, 4, 6-substituted-D-glucose iodine derivative has bactericidal effects on the staphylococcus aureus, pseudomonas aeruginosa and escherichia coli. Antiviral tests of a 3, 4, 6-triacetyl-D-glucose iodine preparation are performed, results show that the 3, 4, 6-triacetyl-D-glucose iodine preparation has a direct inactivation effect on EV71 (Human enterovirus 71) virus, and the therapeutic index is 5.5 times of that of contrast drug ribavirin injection. Therefore, the 3, 4, 6-substituted-D-glucose iodine derivative can be used for the preparation of antibacterial and antiviral drugs, especially can be used for the preparation of drugs for treatment of hand foot and mouth disease, provides a new drug for the treatment of the hand foot and mouth disease, and has a good prospect of clinical application. The present invention provides a preparation method.

Description

technical field [0001] The invention relates to a pharmaceutical preparation, in particular to a sugar iodide, in particular to a 3,4,6-triacetyl-D-glucose iodine derivative, a preparation method thereof and an application in pharmacy. Background technique [0002] Hand foot and mouth disease (HFMD) is an infectious disease in children, also known as exanthematous vesicular stomatitis, which mostly occurs in children under 5 years old and can cause herpes on hands, feet, mouth and other parts. The disease is the main clinical symptom with the formation of ulcers after herpes or ulceration of the hands, feet and oral mucosa. There are more than 20 types of enteroviruses that cause HFMD, among which enterovirus 71 (EV 71) is the most common. [0003] At present, the preparations with iodine as the active ingredient are mostly used for antibacterial, such as iodine tincture, iodophor, povidone iodine, complex iodine, double-chain quaternary ammonium salt complex iodine solutio...

Claims

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Application Information

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IPC IPC(8): C07H13/06C07H1/00A61K31/7024A61P31/14A61P31/04
CPCY02A50/30
Inventor 冒华
Owner SUZHOU HARMONY BIOTECH
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