Ferric Citrate Dissolution for Lower-Dose CKD Phosphate Binding

Resolve Bottlenecks,
Find Innovative Solutions
Generate Solutions

Solution Overview

Problem

Current treatments for chronic kidney disease, particularly those involving ferric compounds, are inefficient due to low solubility and require large doses, leading to gastrointestinal adverse effects and inadequate phosphate binding, which fails to effectively manage serum phosphate levels and progression of the disease.

Innovation Solution

Development of pharmaceutical-grade ferric citrate with enhanced solubility and dissolution rates, synthesized through specific methods, allowing for rapid phosphate binding and reduced gastrointestinal adverse effects.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If conventional ferric compounds are used to treat chronic kidney disease, then phosphate binding function is provided, but solubility is low requiring large doses which cause gastrointestinal adverse effects

Engineering Contradiction:
Improvephosphate binding functionVSAvoidgastrointestinal adverse effects
Core Design Contradiction:
ReliabilityVSObject-affected harmful factors

Solution Approach 1:

The patent applies parameter changes by modifying the chemical composition parameters of ferric compounds, specifically using ferric citrate instead of conventional ferric salts. This chemical parameter change results in enhanced solubility characteristics, allowing the compound to dissolve more effectively in gastrointestinal fluids, thereby reducing the required dosage while maintaining phosphate binding function and minimizing gastrointestinal adverse effects.

Inventive Principle:
Principle #35Parameter changes

Solution Approach 2:

The patent employs composite materials by creating ferric citrate, which combines ferric iron with citrate anions. This composite approach produces a compound that integrates the phosphate binding capability of ferric compounds with the enhanced solubility properties of citrate, resulting in a material that achieves both effective phosphate binding and reduced gastrointestinal irritation compared to conventional ferric salts.

Inventive Principle:
Principle #40Composite materials

2Reliability

If large doses of ferric compounds are administered to achieve phosphate binding, then phosphate binding efficacy is improved, but gastrointestinal adverse effects increase

Engineering Contradiction:
Improvephosphate binding efficacyVSAvoidgastrointestinal adverse effects
Core Design Contradiction:
ReliabilityVSObject-affected harmful factors

Solution Approach 1:

The patent applies parameter changes by modifying the dosing parameter through enhanced solubility. The ferric citrate compound achieves the same phosphate binding efficacy at lower doses compared to conventional ferric compounds, because its improved solubility parameter allows for better absorption and utilization in the gastrointestinal tract, thereby reducing the total amount of material required and minimizing gastrointestinal adverse effects.

Inventive Principle:
Principle #35Parameter changes

3Reliability

If conventional ferric compounds are used, then phosphate binding is achieved, but solubility is insufficient leading to inadequate phosphate level management

Engineering Contradiction:
Improvephosphate level managementVSAvoidsolubility
Core Design Contradiction:
ReliabilityVSQuantity of substance

Solution Approach 1:

The patent applies parameter changes by fundamentally altering the solubility parameter through the selection of ferric citrate as the active compound. This chemical parameter modification enables the substance to achieve adequate dissolution in gastrointestinal fluids, ensuring sufficient availability for phosphate binding and effective management of serum phosphate levels, which was insufficient with conventional ferric compounds.

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 enhanced solubility of ferric citrate effectively reduces serum creatinine, phosphorus, and calcium-phosphorus levels, preventing or delaying the progression of chronic kidney disease and associated complications.

Implementation Method 1

administration of a phosphate binder... binds phosphate in the gastrointestinal tract

Methodology Applied
Scientific EffectPrecipitation: Precipitation

Implementation Method 2

enhanced solubility and dissolution rates... rapid phosphate binding

Methodology Applied
Scientific EffectSolvation: Solvation

Data Source

PatentEP3066923B1Method of treating chronic kidney disease
Publication Date: 2025.11.05 PANION & BF BIOTECH INC
  • EP3066923B1 patent drawingFigure 1
  • EP3066923B1 patent drawingFigure 2
  • EP3066923B1 patent drawingFigure 3

AI summary

The present invention discloses pharmaceutical-grade ferric organic compounds having enhanced dissolution rate. These ferric organic compounds, including but are not limited to ferric citrate, are useful for treating chronic kidney disease.