Iron-based hydroxide-low molecular weight sugar phosphate binder as well as preparation method and application thereof

A low-molecular-weight sugar and phosphorus binding agent technology, applied in the directions of non-active components, applications, and drug combinations of polymer compounds, can solve the problems of patients' side effects and low phosphorus adsorption capacity, and achieve the purpose of reducing side effects, improving phosphorus adsorption capacity, reducing Effects of Cardiovascular Complications

Active Publication Date: 2017-11-28
CINKATE PHARMA INTERMEDIATES
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] Because the patient's daily diet contains a large amount of phosphorus, and the phosphorus adsorption capacity of the existing phosphorus binders is too low, in order to control the blood phosphorus concentration to a normal level, the patient needs to use a large amount of phosphate binders every day, and overdose other side effects for patients

Method used

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Examples

Experimental program
Comparison scheme
Effect test

preparation example Construction

[0088] A kind of preparation method of preferred phosphorus binding agent comprises the following steps:

[0089] Ⅰ Dissolution: Dissolve sugar and weak base in water, the solution temperature is 30-100°C;

[0090] II Complexation: Add an aqueous solution of iron salt dropwise to the solution at a temperature of 30-100°C, and at the same time add an alkali solution dropwise to control the pH of the reaction solution. After dropping a certain amount of iron salt solution and alkali solution, stop the dropwise addition, and Continue stirring for 1-48h to obtain a product solution;

[0091] Ⅲ Separation: After cooling to room temperature, centrifuge or filter to separate the reddish-brown liquid, add 1-5 times the volume of ethanol, centrifuge or filter to separate the precipitate completely, and wash with ethanol or ether;

[0092] Ⅳ collecting powder: drying and separating the product obtained in step III;

[0093] Ⅴ preparation: the powder obtained in step Ⅳ is prepared.

...

Embodiment 1

[0121] experimental method:

[0122] Dissolve 20g of galactooligosaccharide in 200g of water, add 4g of sodium citrate, raise the temperature to 80°C, stir until fully dissolved; add 20% by mass ferric chloride hexahydrate aqueous solution dropwise to the solution at a temperature of 80°C 250g, while adding 20% ​​NaOH aqueous solution dropwise to control the pH of the reaction solution to be 7.5-8.5, after the dropwise addition, stir at 90°C for 4h to obtain a reddish-brown solution; after cooling to room temperature, add 3 times the volume of 95% Ethanol, centrifuged after the precipitation was completely separated out, and the solid was washed twice with 80% ethanol; the obtained product was heated and dried, and a total of 28.6 g of the product was obtained, which was dark brown.

[0123] Experimental results:

[0124] After the product was ground and pulverized, the iron content was measured to be 32.4%, and the phosphorus absorption was 271.9 mg / g.

Embodiment 2

[0126] experimental method:

[0127] Dissolve 300g fructooligosaccharide in 2000g water, add 40g sodium citrate and 20g sodium carbonate, increase the temperature to 90°C, stir until fully dissolved; add 30% mass ratio of chlorine hexahydrate dropwise to the solution at a temperature of 90°C 2500g of ferric chloride aqueous solution, while adding dropwise 20% NaOH aqueous solution to control the pH of the reaction solution to be 7.0-8.5, after the dropwise addition, stir at 90°C for 8h to obtain a reddish-brown suspension; after cooling to room temperature, add 4 Double the volume of 95% ethanol, centrifuge after complete precipitation, and wash the solid twice with 80% ethanol; the resulting product is heated and dried, and a total of 402.4 g of the product is obtained, which is dark brown.

[0128] Experimental results:

[0129] After the product was ground and pulverized, the iron content was measured to be 32.4%, and the phosphorus absorption was 342.1 mg / g.

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PUM

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Abstract

The invention provides an iron-based hydroxide-low molecular weight sugar phosphate binder as well as a preparation method and application thereof. Specifically, the invention provides a phosphate binder which comprises an iron-based hydroxide and low molecular weight sugar, wherein the number of monosaccharide units of the low molecular weight sugar is 3-20, and based on the total weight of the phosphate binder, the mass ratio of the iron is 2-45wt%. Experiments prove that the phosphate binder has an obvious effect of lowering the serum phosphate level. Therefore, the phosphate binder has wide application prospects.

Description

technical field [0001] The invention relates to a phosphorus binder, in particular to a phosphorus binder based on iron salt-low molecular weight sugar, its preparation method and application. Background technique [0002] Hyperphosphatemia is one of the main complications of chronic renal insufficiency (CKD). Increased blood phosphorus concentration is closely related to the mortality of CKD patients, and increased blood phosphorus concentration will lead to further decline of renal function and secondary thyroid function resistance. , vascular calcification and minerals, bone metabolism disorders. It is generally believed that regulating phosphorus metabolism is the key to reducing cardiovascular complications, improving the quality of life of dialysis patients, and reducing morbidity and mortality. [0003] In recent years, new phosphorus binders have been developed continuously. Among them, the iron-containing phosphorus binder has been proved to be a high-efficiency p...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K33/26A61K31/7016A61K31/702A61K31/715A61K31/724A61K47/26A61K47/36A61K47/40A61K47/12A61P37/04A61P3/12A61P5/16A61P13/12A61P19/08A61P9/00A61P3/00A23L33/00A61K31/295
CPCA23V2002/00A61K31/7016A61K31/702A61K31/715A61K31/724A61K33/26A61K47/12A61K47/26A61K47/36A61K47/40A61K2300/00A23V2200/324A23V2200/30A23V2200/306A23V2200/326
Inventor 梁星崔洋洋许婧陆佳美包丽霞刘荣军袁西伦肖飞
Owner CINKATE PHARMA INTERMEDIATES
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