Buffered Iron Composition for Duodenal Absorption

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Solution Overview

Problem

The body lacks a defined mechanism for the active excretion of iron, requiring tight regulation at the point of absorption in the proximal small intestine, where much of the ingested iron is in the oxidized or ferric form, necessitating reduction for uptake by enterocytes, and existing compositions do not effectively maintain optimal pH for iron absorption in the duodenum.

Innovation Solution

A pharmaceutical composition comprising a buffering agent with efficacy between pH 1.0 and 6.0, specifically between 2.0 and 4.0, combined with an iron compound or other pharmacological agents, to maintain or reduce duodenal fluid pH, thereby improving iron absorption and bioavailability by extending the acidic pH zone in the duodenum.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If iron compounds are administered in the ferric form, then iron can be provided in a stable oxidized state, but the iron cannot be directly taken up by enterocytes without reduction

Engineering Contradiction:
Improveiron absorption efficiencyVSAvoidabsorption mechanism complexity
Core Design Contradiction:
ReliabilityVSDevice complexity

Solution Approach 1:

The patent introduces reducing agents (such as ascorbic acid, citric acid, or other electron donors) as intermediaries that facilitate the conversion of ferric iron to ferrous iron, enabling enterocyte uptake without requiring the body to develop new active excretion mechanisms. This mediator approach resolves the contradiction by providing a simple chemical reduction step rather than complex biological machinery.

Inventive Principle:
Principle #24Intermediary (Mediator)

2Reliability

If the duodenal pH is not maintained in the optimal acidic range, then iron solubility and absorption are reduced, but maintaining acidic pH throughout the duodenum is difficult due to natural pH gradients

Engineering Contradiction:
Improveiron bioavailabilityVSAvoidpH control difficulty
Core Design Contradiction:
ReliabilityVSEase of operation

Solution Approach 1:

The patent employs pH-modifying agents (buffering agents or acidifying agents) that alter the pH parameter of the duodenal environment to maintain it within the optimal acidic range (pH 2-4) for iron absorption. These agents counteract the natural pH gradient and neutralization by pancreatic bicarbonate, ensuring sustained acidic conditions that enhance iron solubility and absorption throughout the duodenum.

Inventive Principle:
Principle #35Parameter changes

3Productivity

If iron absorption is enhanced by extending the acidic pH zone, then the absorptive surface area and exposure time increase, but the complexity of the composition increases with multiple buffering agents

Engineering Contradiction:
Improveiron absorption rateVSAvoidcomposition complexity
Core Design Contradiction:
ProductivityVSDevice complexity

Solution Approach 1:

The patent selects pH-modifying agents that perform multiple functions: they not only maintain acidic pH for iron solubility but also act as reducing agents or chelating agents that facilitate iron reduction and uptake. For example, ascorbic acid serves both as an acidifier and a reducing agent, while citric acid provides both pH buffering and chelation capabilities. This multi-functionality enhances absorption productivity without proportionally increasing composition complexity.

Inventive Principle:
Principle #6Universality (Multi-functionality)

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 composition significantly enhances the bioavailability of iron and other pharmacological agents by extending the acidic pH zone in the duodenum, increasing the absorptive surface area and exposure time, leading to improved absorption and treatment of iron deficiency conditions.

Implementation Method 1

The buffering agents are constituted to maintain or reduce the pH of the duodenal fluid in the proximal, mid and distal duodenum

Methodology Applied
Scientific EffectBuffering capacity:

Implementation Method 2

Much of the iron that enters the lumen of the duodenum in the diet is in the oxidized or ferric form and, therefore, must be reduced before it can be taken up by enterocytes

Methodology Applied
Scientific EffectReduction: Reduction

Data Source

PatentEP2758056B1Buffered upper GI absorption promoter
Publication Date: 2020.06.24 ALBION LABORATORIES INC
  • EP2758056B1 patent drawingFigure 1~2
  • EP2758056B1 patent drawingFigure 3~4B
  • EP2758056B1 patent drawingFigure 5(a)~6

AI summary

The present invention relates to compositions of an active pharmaceutical compound or nutritional ingredient with one or more buffering agents between a pH of 1.0 and 6.0, preferably 2.0 and 4.0. The buffering agents are constituted to maintain or reduce the pH of the duodenal fluid in the proximal, mid and distal duodenum. The present invention further relates to methods of improving the absorption of an iron compound or an active pharmaceutical compound within the small intestine. The present compositions and methods improve absorption or bioavailability of the administered compositions.