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A riboflavin sodium phosphate crystal compound, its pharmaceutical composition and preparation method

A technology of riboflavin sodium phosphate and crystal compounds, which is applied in the direction of drug combinations, compounds of Group 5/15 elements of the periodic table, chemical instruments and methods, etc., can solve the problems of low yield, poor quality stability, and inconvenience of preparations, To achieve the effect of convenient operation, stable quality and simple process

Active Publication Date: 2011-11-30
周晓东
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

This method has more by-products during the phosphorylation reaction, is easily oxidized, has a strong smell, and the reaction is not easy to control. During production, the inorganic salts of phosphoric acid also increase, and a large amount of solvents have to be used for elution and purification to obtain The higher content of riboflavin sodium phosphate brings a lot of inconvenience to the post-processing
The preparations made using the above raw materials have low yield and poor quality stability

Method used

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  • A riboflavin sodium phosphate crystal compound, its pharmaceutical composition and preparation method
  • A riboflavin sodium phosphate crystal compound, its pharmaceutical composition and preparation method
  • A riboflavin sodium phosphate crystal compound, its pharmaceutical composition and preparation method

Examples

Experimental program
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Effect test

Embodiment 1

[0042] Add 20ml of water, 250ml of tetrahydrofuran and 48g of riboflavin into a 1000ml three-necked bottle, stir and dissolve to form a mixture, cool to 5-10°C, slowly add 100ml of sodium metaphosphate aqueous solution (20.4g of sodium metaphosphate is dissolved in 100ml of water), the temperature Control at 28-30°C, after adding, heat up to 40°C, react for 2-3 hours, stop the reaction, cool to 15-25°C, pour the reaction solution into a large beaker, add 250ml of water, and pay attention to cooling down while stirring. Remove insolubles. Add 10% sodium hydroxide solution to the filtrate, adjust the pH value to 9, stir at room temperature for 0.5 hours, filter with suction, adjust the pH of the mother liquor to 5-6 with hydrochloric acid, and filter with suction to obtain a white solid, rinse with a small amount of 50% ethanol, Then the product was dissolved in 95% ethanol, filtered, crystallized and dried to obtain 59.2 g of orange-yellow solid with a yield of 92%. At the sam...

Embodiment 2

[0049] Mix the riboflavin raw material with water and tetrahydrofuran to form a suspension, the volume ratio of water and tetrahydrofuran is 1:30; the initial concentration of the riboflavin raw material suspension is 0.1mol / L; cool to 8 ° C, slowly add partial Sodium phosphate aqueous solution, the mol ratio of the added sodium metaphosphate and riboflavin is 1.1: 1; Temperature is 25~30 ℃; The concentration of sodium metaphosphate aqueous solution is 18g / ml; 35°C, stop the reaction after 3 hours of reaction, cool to 20°C, add water to stir, filter; add sodium hydroxide solution to the filtrate, add sodium hydroxide solution, the molar ratio of sodium hydroxide to riboflavin is 1:1 Adjust the pH to 9-9.5, stir at room temperature for 20 minutes, and filter with suction to obtain an orange-yellow solid, wash with a small amount of 50% ethanol, and dry in vacuum to obtain riboflavin sodium phosphate as a solid. The yield was 92%. At the same time, it was analyzed by high perfo...

Embodiment 3

[0051] Mix the riboflavin raw material with water and tetrahydrofuran to form a suspension, the volume ratio of water and tetrahydrofuran is 1:30; the initial concentration of the riboflavin raw material suspension is 0.22mol / L; cool to 8°C, slowly add partial Sodium phosphate aqueous solution, the mol ratio of the added sodium metaphosphate and riboflavin is 1: 1; Temperature is 25~30 ℃; The concentration of sodium metaphosphate aqueous solution is 20g / ml; After adding sodium metaphosphate aqueous solution, be warming up to Preferably 35~40 ℃, stop reaction after reacting for 2 hours, cool to 20 ℃, add water and stir, filter; Add sodium hydroxide solution in the filtrate, add the mol ratio of sodium hydroxide and riboflavin in the sodium hydroxide solution is 1.25:1; adjust the pH value to 9-9.5, stir at room temperature for 30 minutes, filter with suction to obtain an orange-yellow solid, wash with a small amount of 50% ethanol, and dry in vacuo to obtain a solid riboflavin s...

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Abstract

The invention relates to a riboflavin sodium phosphate crystalline compound, which comprises 1.5 crystal waters. The riboflavin sodium phosphate crystalline compound is measure by using Cu-Kalpha rays. Characteristic peaks are shown when X-ray powder is diffracted at 2theta of 6.1 DEG, 11.2 DEG, 13.4 DEG, 14.8 DEG, 19.7 DEG, 20.8 DEG, 23.9 DEG, 24.5 DEG, 26.9 DEG, 27.7 DEG, 29.1 DEG, 31.0 DEG, and 31.6 DEG. The invention also relates to a preparation method of the compound, and a pharmaceutical composition containing the compound. The invention further relates to a synthesizing method of riboflavin sodium phosphate. As a result of experiments, the riboflavin sodium phosphate crystalline compound provided by the invention has high stability.

Description

technical field [0001] The invention relates to a riboflavin phosphate, in particular to a riboflavin sodium phosphate crystal compound, a pharmaceutical composition and a preparation method thereof. Background technique [0002] Riboflavin (riboflavin), also known as VB2, chemically named 6,7-dimethyl-10-(1′-D-ribitolyl)-isoxazine, is a water-soluble substance necessary for maintaining normal metabolism of the body Vitamins are the important prosthetic groups of many enzyme systems in the body - the components of flavin adenine dinucleotide (FAD) and flavin mononucleotide (FMN), and participate in the body's energy metabolism and material metabolism. If the body lacks riboflavin, it will affect the normal oxidation in the body, cause material metabolism disorder, cause a series of diseases in the body, and even lead to death in severe cases. Given that riboflavin has extensive and important physiological functions, the World Health Organization lists it as one of the six ...

Claims

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Application Information

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IPC IPC(8): C07F9/6561A61K31/661A61P3/02
Inventor 周晓东丁平
Owner 周晓东
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