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Gel-based layered inorganic phosphorus binding agent and preparation method and application thereof

A phosphorus binder and inorganic technology, applied in the field of medicine, can solve the problems of long-term use limitation and side effects, and achieve the effects of improving efficiency, improving removal rate and large specific surface area.

Active Publication Date: 2019-03-29
北京市中关村医院 +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Currently commercially available phosphorus binders, such as lanthanum carbonate, lanthanum chloride, and Silamer, etc., have good phosphorus binding ability, but there are more or less side effects, and there are certain limitations in the long-term clinical use in the future

Method used

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  • Gel-based layered inorganic phosphorus binding agent and preparation method and application thereof
  • Gel-based layered inorganic phosphorus binding agent and preparation method and application thereof
  • Gel-based layered inorganic phosphorus binding agent and preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0043] Add 100g of lanthanum-based montmorillonite (cation exchange rate 40%) to 1.25L of water, stir at room temperature for 2 hours to make it fully swell, add 100g of pectin (pectin is apple pectin, methylation degree 40%, molecular weight 1000Da) , continue to stir until completely dissolved. Add the above mixture dropwise to the ferric chloride solution (2wt%) at a speed of 0.1L / min, the stirring speed is 300r / min, after the completion of the dropwise addition, continue the cross-linking reaction for 0.5h to obtain a composite gel, and use deionized water After repeated washing, until the washing liquid does not contain ferric chloride, it is freeze-dried to obtain composite gel particles. The particle size of the composite gel particles is 0.78±0.12mm, the drug loading capacity is 34.05%, the encapsulation efficiency is 70.12%, and the phosphate adsorption capacity is 12.70mg / g.

[0044] Mix 1 part by mass of composite gel particles with 5 parts by mass of lubricant ste...

Embodiment 2

[0051] Add 300g of lanthanum-based montmorillonite (cation exchange rate 40%) to 3.75L of water, stir at room temperature for 2 hours to make it fully swell; add 100g of pectin (pectin is citrus pectin, methylation degree 40%, molecular weight 5000Da) , continue to stir until completely dissolved. The above mixture was added dropwise to ferric hydroxide solution (3wt%) at a speed of 0.15 L / min, and the stirring speed was 240 r / min. After the addition was completed, the cross-linking reaction was continued for 1.5 hours to obtain a composite gel, and deionized water was used to After repeated washing, until the washing solution does not contain ferric hydroxide, it is freeze-dried to obtain composite gel particles. The particle diameter of the composite gel particles is 0.91±0.21mm, the drug loading capacity is 49.30%, the encapsulation efficiency is 80.12%, and the phosphate adsorption capacity is 19.21mg / g.

[0052] Mix 1 part by mass of composite gel particles with 5 parts ...

Embodiment 3

[0058] Add 450g of lanthanum-based montmorillonite (50% cation exchange rate) to 5.63L of water, stir at room temperature for 2 hours to make it fully swell; add 200g of pectin (pectin is a mass mixture of citrus pectin and apple pectin, the two Kylation degree is 35%, molecular weight 5000Da), continue to stir until completely dissolved. The above mixture was added dropwise to the ferric oxyhydroxide solution (5wt%) at a rate of 0.18L / min, and the stirring speed was 270r / min. After the dropwise addition was completed, the crosslinking reaction was continued for 1.5h to obtain a composite gel. After repeated washing, until the iron oxyhydroxide is not contained in the washing solution, freeze-dry to obtain composite gel particles. The particle size of the composite gel particles is 1.01±0.18mm, the drug loading capacity is 59.51%, the encapsulation efficiency is 85.10%, and the phosphate adsorption capacity is 23.41mg / g.

[0059] Mix 1 part by mass of composite gel particles ...

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Abstract

The invention discloses a gel-based layered inorganic phosphorus binding agent and a preparation method and an application thereof. The preparation method includes: preparing a layered inorganic substance, adding water and stirring the mixture at room temperature to fully swell the substance; adding a gelatinizer, continuously stirring the mixture to complete dissolution, and dropwise adding the mixture to a crosslinker solution to prepare composite gel spheres; repeatedly washing the composite gel spheres for several times with deionized water until the washing liquid does not contain the crosslinker; freeze-drying the mixture to obtain the gel-based layered inorganic phosphorus binding agent. The invention also provides an application of the gel-based layered inorganic phosphorus bindingagent in preparation of medicines for treating hyperphosphatemia or chronic renal failure. By introducing the gel system, the layered inorganic substance is protected well, and a phosphorus binding agent can arrive at intestines and stomach with full dose, thus improving the binding efficiency between the phosphorus binding agent and phosphate.

Description

technical field [0001] The invention belongs to the technical field of medicine, and in particular relates to a gel-based layered inorganic phosphorus binder, a preparation method and application thereof. Background technique [0002] As one of the main complications of chronic kidney disease, hyperphosphatemia accounts for up to 80% of patients with chronic kidney disease. If the excessive phosphorus in the patient's body cannot be removed in time, it will cause bone lesions and damage to the cardiovascular system. threatening the life of the patient. Conventional hemodialysis has limited ability to remove phosphate in patients, and the use of phosphorus binders can effectively reduce the absorption of phosphorus in the stomach through chelation. Currently commercially available phosphorus binders, such as lanthanum carbonate, lanthanum chloride, and Silamer, etc., have good phosphorus binding ability, but there are more or less side effects, and there are certain limitati...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K33/244A61K33/30A61K33/24A61K33/06A61K33/44A61K33/00A61P3/12A61P13/12
CPCA61K33/00A61K33/06A61K33/24A61K33/30A61K33/44A61P3/12A61P13/12
Inventor 张启蒙查瑞涛
Owner 北京市中关村医院
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