Mg-Fe-Cl Cationic Binder for Hyperphosphatemia Treatment

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Solution Overview

Problem

Patients with chronic kidney disease often suffer from hyperphosphatemia, leading to secondary hyperparathyroidism and osteoporosis due to impaired calcium and phosphorous regulation, for which existing phosphate binders may cause aluminum intoxication or cardiac calcification, necessitating a more effective and safer oral phosphate binder.

Innovation Solution

A cationic binder composed of magnesium, iron (III), and chloride, synthesized with a specific atomic ratio of Mg+2 to Fe+3 between 2:1 and 60:1, exhibiting a high anion uptaking capacity greater than 100 ppm/(g/L), is developed to effectively bind phosphate in the gastrointestinal tract, reducing serum phosphorus levels.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If existing phosphate binders are used to treat hyperphosphatemia, then phosphorus levels can be controlled, but aluminum intoxication or cardiac calcification may occur

Engineering Contradiction:
Improvephosphorus level controlVSAvoidaluminum intoxication and cardiac calcification
Core Design Contradiction:
ReliabilityVSObject-affected harmful factors

Solution Approach 1:

The invention changes the chemical composition parameters of phosphate binders by using magnesium, iron (III), and chloride in specific atomic ratios (Mg:Fe between 2:1 and 60:1). This parameter change eliminates aluminum content entirely, preventing aluminum intoxication and cardiac calcification while maintaining effective phosphorus binding capacity greater than 100 ppm/(g/L).

Inventive Principle:
Principle #35Parameter changes

Solution Approach 2:

The invention creates a composite material system combining magnesium, iron (III), and chloride in a hydrotalcite-like structure. This composite approach provides synergistic effects where the combination of cations creates a material with superior phosphate binding capacity while eliminating the harmful aluminum component, thus resolving the contradiction between effectiveness and safety.

Inventive Principle:
Principle #40Composite materials

2Reliability

If phosphate binders are used to prevent secondaryhyperparathyroidism, then phosphorus accumulation can be reduced, but safer alternatives are needed to avoid existing binder side effects

Engineering Contradiction:
Improveprevention of secondaryhyperparathyroidismVSAvoidside effects of existing binders
Core Design Contradiction:
ReliabilityVSObject-affected harmful factors

Solution Approach 1:

The invention modifies the compositional parameters of phosphate binders by eliminating aluminum and using specific Mg:Fe atomic ratios between 2:1 and 60:1. This parameter change maintains the ability to prevent secondaryhyperparathyroidism through effective phosphorus control while removing the harmful side effects associated with aluminum-based and other conventional binders.

Inventive Principle:
Principle #35Parameter changes

3Reliability

If a cationic binder with high anion uptaking capacity is designed, then phosphate binding effectiveness is improved, but synthesis complexity may increase

Engineering Contradiction:
Improvephosphate binding effectivenessVSAvoidsynthesis process complexity
Core Design Contradiction:
ReliabilityVSDevice complexity

Solution Approach 1:

The invention optimizes synthesis parameters by controlling the atomic ratio of Mg to Fe between 2:1 and 60:1 during the formation of the hydrotalcite-like structure. This parameter control achieves high phosphate binding effectiveness (anion uptaking capacity greater than 100 ppm/(g/L)) while maintaining a relatively simple synthesis process using conventional ceramic processing methods.

Inventive Principle:
Principle #35Parameter changes

Applied Scientific Principles

This section explains which scientific principles are used to turn an abstract innovation direction into a practical engineering solution.

Function Achieved in This Case

The Mg-Fe-Cl hydrotalcite-like nanoplatelet binder demonstrates a phosphate uptaking capacity of up to 325 ppm/(g/L) in cow milk, reducing phosphorus levels by 65% in 90 minutes with no cellular cytotoxicity, and effectively lowers serum phosphorus and creatinine levels when administered orally, providing a safer alternative for treating hyperphosphatemia.

Implementation Method 1

The cationic binder includes magnesium, iron (III) and chloride... an anion uptaking capacity of the cationic binder is greater than 100 ppm/(g/L)

Methodology Applied
Scientific EffectIon exchange: Ion Exchange

Implementation Method 2

The Mg-Fe-Cl hydrotalcite-like nanoplatelet binder demonstrates a phosphate uptaking capacity of up to 325 ppm/(g/L) in cow milk

Methodology Applied
Scientific EffectAdsorption: Adsorption

Data Source

PatentUS10517893B2Cationic binder, pharmaceutical composition comprising the same and method of using the same
Publication Date: 2019.12.31 AIGA BIOMEDICAL CORP
  • US10517893B2 patent drawing
  • US10517893B2 patent drawing
  • US10517893B2 patent drawing

AI summary

The present invention provides a pharmaceutical composition for treating a patient suffering from or predisposed to hyperphosphatemia, which contains Mg—Fe—Cl HCln. In one embodiment, the Mg—Fe—Cl HCln is shown in formula (I). The phosphorus uptaking capacity of the pharmaceutical composition is greater than 100 ppm/(g/L). The present invention further provides a method for treating a patient suffering from or predisposed to hyperphosphatemia by using said pharmaceutical composition. The present invention further provides a method of manufacturing the pharmaceutical composition.