Iron-based hydroxide-degraded carbohydrate phosphate binder as well as preparation method and application thereof

A carbohydrate and phosphorus binding agent technology, applied in the direction of carbohydrate active ingredients, applications, drug combinations, etc., can solve the problems of patient side effects, low phosphorus adsorption capacity, etc.

Inactive 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

[0102] A kind of preparation method of preferred phosphorus binding agent is as follows:

[0103] Mix the hydrolyzate and iron salt in water, heat, react for 1 to 240 hours, and the reaction temperature is 20 to 100 degrees Celsius; then cool to 0 to 40 degrees Celsius, add alkali until precipitation occurs, and adjust the pH of the system to 6 to 13, preferably 7 to 10; the precipitate was separated to obtain the product.

[0104] The preparation method of another kind of preferred phosphorus binder is as follows:

[0105] Mix the hydrolyzate and alkali in water, the solution temperature is 30 to 100 degrees Celsius; then add iron salt and alkali dropwise at the same time, control the pH of the system between 5 and 12, preferably 7 to 9; continue to stir for 1-24 hours; cool Bring to room temperature, add 1-10 times of ethanol, separate the precipitate, and obtain the product.

[0106] In the present invention, the iron salt is not particularly limited, and a preferred iron...

Embodiment 1

[0134] experimental method:

[0135] Dissolve 100g of gum arabic in 1000g of water, add concentrated sulfuric acid dropwise to adjust the pH of the system to 1, heat to 80°C, keep the temperature, and stir for 4 hours; add 25g of sodium citrate, raise the temperature to 90°C, and stir to fully dissolve; Add 20% by mass ferric chloride hexahydrate aqueous solution dropwise to the solution at a temperature of 90°C, and simultaneously add 20% by mass NaOH aqueous solution dropwise to control the pH of the reaction solution to be 8.0-9.0 until there is obvious precipitation and stop Add dropwise, and stir at 90°C for 5 hours to obtain a reddish-brown solution; after cooling to room temperature, centrifuge to remove the solids in the solution, add 4 times the volume of 95% ethanol to the supernatant, centrifuge after the precipitation is complete, and use Wash the solid twice with 70% ethanol and 80% ethanol; the resulting product was spray-dried to obtain a total of 145.6 g of the...

Embodiment 2

[0139] experimental method:

[0140] Dissolve 10g gum arabic in 100g water, add concentrated hydrochloric acid dropwise to adjust the pH value of the system to 1, heat to 70°C, keep the temperature, stir for 20 hours, and add 20% mass ratio of hexahydrate chloride to the solution dropwise at 70°C 150ml of iron aqueous solution, continue to stir for 4 hours after the dropwise addition, and then cool down to room temperature; dropwise add 20% NaOH aqueous solution by mass ratio, adjust the pH of the system to 8.0, and a large amount of precipitation precipitates; centrifuge to separate the precipitate, wash the precipitate with water 3 times, and the obtained product After drying, the product was 4.5 g in total, and the product was reddish brown.

[0141] Experimental results:

[0142] After hydrolysis for 20 hours, the number-average molecular weight of the gum arabic was 64,000. After the product was ground and pulverized, the iron content was 31.5% by the above-mentioned gen...

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Abstract

The invention provides an iron-based hydroxide-degraded carbohydrate 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 a degraded carbohydrate, wherein based on the total weight of the phosphate binder, the mass ratio of the iron is 5-45wt%; the number-average molecular weight of the degraded carbohydrate is 1000-300000Da; and a ratio (D1/D2) of the number-average molecular weight D1 of the degraded carbohydrate to a number-average molecular weight D2 of the carbohydrate before degradation is 0.05-0.8. 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 present invention relates to a phosphorus binder, in particular to a phosphorus binder based on iron salt-degraded carbohydrates, its preparation method and its 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-effi...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K33/26A61P3/00A61P3/12A61P5/16A61P3/14A61P9/00A61P19/00A23L33/00A61K31/70A61K31/715A61K31/736A61K31/191
CPCA23V2002/00A61K31/191A61K31/70A61K31/715A61K31/736A61K33/26A61K2300/00A23V2200/30A23V2250/1592A23V2250/502A23V2250/5028A23V2250/5042A23V2250/5072
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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