Calcium Citrate Suspension Formulation for Bioavailability

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Solution Overview

Problem

Current calcium supplementation methods, particularly using calcium carbonate, face challenges such as side effects like kidney stones, poor bioavailability, and difficulties in formulation, especially for elderly and pediatric patients, due to the low calcium content and solubility issues of calcium citrate, leading to compliance problems and inefficient dosage forms.

Innovation Solution

An aqueous suspension formulation comprising calcium citrate, xanthan gum, and lactic acid, which provides a stable, ready-to-use, and easily consumable form of calcium supplementation, allowing for higher dosages in smaller volumes, reducing the need for multiple tablets and improving bioavailability and patient compliance.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Quantity of substance

If calcium carbonate is used for supplementation, then calcium dosage is high, but kidney stones risk increases and bioavailability decreases

Engineering Contradiction:
Improvecalcium dosageVSAvoidkidney stones risk
Core Design Contradiction:
Quantity of substanceVSObject-affected harmful factors

Solution Approach 1:

The patent changes the chemical form of calcium from carbonate to citrate, altering its solubility characteristics and absorption properties. Calcium citrate has lower risk of kidney stone formation while maintaining adequate bioavailability, directly resolving the contradiction between high calcium dosage and kidney stones risk

Inventive Principle:
Principle #35Parameter changes

Solution Approach 2:

The invention uses a composite formulation containing calcium citrate combined with citric acid and buffering agents. This composite approach enhances the solubility and bioavailability of calcium citrate, allowing high calcium dosage without the harmful effects of calcium carbonate while maintaining patient compliance

Inventive Principle:
Principle #40Composite materials

2Reliability

If calcium citrate is used for supplementation, then bioavailability improves and kidney stones risk reduces, but formulation stability deteriorates due to solubility issues

Engineering Contradiction:
ImprovebioavailabilityVSAvoidformulation stability
Core Design Contradiction:
ReliabilityVSStability of the object's composition

Solution Approach 1:

The patent introduces citric acid as an intermediary substance that forms soluble complexes with calcium citrate. This intermediary mechanism enhances the solubility of calcium citrate in aqueous environments, maintaining formulation stability while preserving the high bioavailability and low kidney stone risk benefits of calcium citrate

Inventive Principle:
Principle #24Intermediary (Mediator)

3Reliability

If calcium citrate is used for supplementation, then bioavailability improves, but volume required for effective dosage increases

Engineering Contradiction:
ImprovebioavailabilityVSAvoidsupplementation volume
Core Design Contradiction:
ReliabilityVSVolume of moving object

Solution Approach 1:

The patent changes the pH parameters of the formulation by adding citric acid and buffering agents. This parameter change increases the solubility of calcium citrate, allowing higher concentrations of elemental calcium to be delivered in smaller volumes while maintaining the high bioavailability advantage of calcium citrate

Inventive Principle:
Principle #35Parameter changes

4Ease of manufacture

If calcium carbonate is used for supplementation, then manufacturing is simple, but patient compliance deteriorates due to side effects

Engineering Contradiction:
Improvemanufacturing simplicityVSAvoidpatient compliance
Core Design Contradiction:
Ease of manufactureVSEase of operation

Solution Approach 1:

The invention uses a composite formulation with calcium citrate, citric acid, and buffering agents that can be manufactured using standard pharmaceutical techniques. This composite approach maintains manufacturing simplicity while dramatically improving patient compliance by eliminating the side effects associated with calcium carbonate, such as kidney stones and gastrointestinal discomfort

Inventive Principle:
Principle #40Composite materials

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 formulation achieves stable suspensions that are easy to take, providing effective calcium supplementation with reduced side effects, enhanced bioavailability, and improved patient compliance, particularly suitable for elderly and pediatric patients, effectively preventing bone mass loss diseases like osteoporosis.

Implementation Method 1

An aqueous suspension formulation comprising calcium citrate, xanthan gum, and lactic acid

Methodology Applied
Scientific EffectSuspension: Suspension

Implementation Method 2

xanthan gum, and lactic acid, which provides a stable, ready-to-use, and easily consumable form

Methodology Applied
Scientific EffectThickening: Viscoelasticity

Implementation Method 3

calcium citrate, xanthan gum, and lactic acid, which provides a stable, ready-to-use, and easily consumable form of calcium supplementation, allowing for higher dosages in smaller volumes, reducing the need for multiple tablets and improving bioavailability

Methodology Applied
Scientific EffectSolubility enhancement: Solvation

Data Source

PatentEP3678497B1Composition for calcium supplementation
Publication Date: 2021.07.21 ABIOGEN PHARMA SPA

AI summary

The present invention relates to a formulation in the form of an aqueous suspension comprising calcium citrate. Said formulation exhibits excellent stability and compliance and finds use in calcium supplementation in subjects in need of such supplementation.