Lanthanum Polystyrene Sulfonate for Gastrointestinal Phosphate Removal

Resolve Bottlenecks,
Find Innovative Solutions
Generate Solutions

Solution Overview

Problem

Current treatments for hyperphosphatemia, such as dialysis and oral administration of aluminum or calcium compounds, cause significant adverse reactions and are ineffective across the entire gastrointestinal tract, while existing phosphate removal drugs like lanthanum carbonate are costly and inefficient in intestinal environments.

Innovation Solution

A drug formulation using lanthanum polystyrene sulfonate, with a lanthanum weight percentage of 14-22%, which forms insoluble conjugates in the gastrointestinal tract, allowing for effective phosphate removal across the entire alimentary tract through various dosage forms like powders, capsules, and tablets.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If lanthanum carbonate aquated complex is used to treat hyperphospheremia, then phosphate removal in gastric environment is improved, but effectiveness in intestinal environment deteriorates due to pH limitations

Engineering Contradiction:
Improvephosphate removal effectivenessVSAvoideffectiveness across different gastrointestinal pH environments
Core Design Contradiction:
ReliabilityVSAdaptability or versatility

Solution Approach 1:

The patent changes the chemical form of lanthanum from carbonate to polystyrene sulfonate complex, which fundamentally alters its solubility characteristics and pH independence. This parameter change enables the drug to maintain effectiveness across the entire gastrointestinal tract regardless of pH variations.

Inventive Principle:
Principle #35Parameter changes

Solution Approach 2:

The invention creates a composite material by combining lanthanum ions with polystyrene sulfonate polymer chains, forming a new compound with enhanced properties. This composite structure provides both the phosphate-binding capability of lanthanum and the pH-resistant characteristics of the polymer backbone.

Inventive Principle:
Principle #40Composite materials

2Reliability

If aluminum or calcium compounds are administered orally to treat hyperphospheremia, then phosphate binding capability is improved, but systematic adverse reactions and organ damage worsen

Engineering Contradiction:
Improvephosphate binding capabilityVSAvoidsystematic adverse reactions and organ damage
Core Design Contradiction:
ReliabilityVSObject-affected harmful factors

Solution Approach 1:

The patent extracts the harmful metallic ion component (aluminum or calcium) from the treatment system and replaces it with lanthanum, which has similar phosphate-binding capabilities but significantly reduced toxicity. The polystyrene sulfonate carrier further isolates the lanthanum, preventing systemic absorption while maintaining local effectiveness in the gastrointestinal tract.

Inventive Principle:
Principle #2Taking out (Extraction)

Solution Approach 2:

The polystyrene sulfonate acts as an intermediary carrier that mediates between the lanthanum ions and the gastrointestinal environment. It provides a safe interface that allows lanthanum to bind phosphate effectively while preventing direct contact with tissues that would cause damage, thus enabling therapeutic action without harmful side effects.

Inventive Principle:
Principle #24Intermediary (Mediator)

3Quantity of substance

If dialysis is used to treat hyperphospheremia, then phosphate concentration reduction is achieved, but serious damage to body and limited effectiveness worsen

Engineering Contradiction:
Improvephosphate concentration reductionVSAvoidserious damage to body
Core Design Contradiction:
Quantity of substanceVSObject-affected harmful factors

Solution Approach 1:

The patent enables the gastrointestinal tract to perform phosphate removal function itself through oral administration of the binding agent. The lanthanum polystyrene sulfonate complex travels through the digestive system, binds phosphate locally, and is excreted naturally, allowing the body's own elimination systems to handle phosphate removal without requiring external dialysis intervention.

Inventive Principle:
Principle #25Self-service

4Reliability

If existing phosphate removal drugs are used, then treatment effectiveness is improved, but economic burden on patients worsens due to high costs

Engineering Contradiction:
Improvetreatment effectivenessVSAvoidproduction cost and economic burden
Core Design Contradiction:
ReliabilityVSEase of manufacture

Solution Approach 1:

The patent employs a disposable oral formulation that acts locally in the gastrointestinal tract without requiring expensive manufacturing processes or complex delivery systems. The lanthanum polystyrene sulfonate complex is designed for single-use oral administration, eliminating the need for costly infrastructure like dialysis centers while providing effective phosphate removal at a lower cost.

Inventive Principle:
Principle #27Cheap short-living objects (Disposable)

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

Lanthanum polystyrene sulfonate effectively reduces phosphate levels in the stomach, small intestine, and large intestine, reducing the economic burden on patients by providing a cost-effective solution with minimal side effects and improved phosphate removal compared to existing treatments.

Implementation Method 1

Lanthanum polystyrene sulfonate effectively reduces phosphate levels in the stomach, small intestine, and large intestine by making phosphate in alimentary tract become insoluble conjugates

Methodology Applied
Scientific EffectAdsorption: Adsorption

Data Source

PatentUS7662364B2Drug for hyperphospheremia and its preparative method
Publication Date: 2010.02.16 GRAND LIFE SCI (LIAONING) CO LTD
  • US7662364B2 patent drawing
  • US7662364B2 patent drawing
  • US7662364B2 patent drawing

AI summary

This invention reports a drug for hyperphospheremia and its preparative method. The preparation includes active constituents, lanthanum polystyrene sulfonate, and excipients. The preparative method in the invention can be summarized as follows: Polystyrene sulfonic acid is obtained by treating polystyrene sulfosalt with hydrochloric acid, soaked or eluted with water soluble lanthanum-contained solution, and washed with water till its PH is neutral. Then, the lanthanum polystyrene sulfonate solution is washed till the superfluous La− unexchanged is washed out. Lanthanum polystyrene sulfonate is taken out and crushed to powder after being dried. The lanthanum polystyrene sulfonate, whose weight percentage of lanthanum is 14-22%, is used as active constituents to prepare gastrointestinal tract preparations together with general amount of excipients with routine preparative method. In the invention, lanthanum polystyrene sulfonate is adopted as active constituents, mixed with excipients, and the preparation is obtained. It makes phosphate in alimentary tract become insoluble conjugates after gastrointestinal tract administration. The insoluble conjugates would be discharged. Thus, the drug can achieve the purpose of treating hyperphospheremia.