Polysaccharide Formulations with Viscosity-Lowering Agents

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Solution Overview

Problem

High-viscosity formulations of polysaccharides and nucleic acids pose challenges in administration, manufacturing, and purification due to intramolecular interactions, leading to difficulties in injection, stability, and fermentation processes, necessitating a reduction in viscosity for effective delivery and processing.

Innovation Solution

Development of concentrated, low-viscosity liquid formulations using viscosity-lowering agents such as ionic liquids, organophosphates, and water-soluble organic dyes, which reduce the viscosity of polysaccharide and nucleic acid solutions to facilitate easier administration and processing, while maintaining stability and concentration.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Quantity of substance

If polysaccharides and nucleic acids are administered at high concentrations, then therapeutic efficacy is improved, but viscosity increases making injection difficult

Engineering Contradiction:
Improveconcentration of polysaccharide or nucleic acidVSAvoidease of injection
Core Design Contradiction:
Quantity of substanceVSEase of operation

Solution Approach 1:

The patent introduces viscosity-lowering agents (such as hydrophilic polymers, surfactants, or specific salts) as intermediary substances that mediate between the high-concentration polysaccharide/nucleic acid solution and the injection process. These agents reduce intramolecular and intermolecular interactions, lowering viscosity without reducing the concentration of the therapeutic agent, thereby enabling easy injection while maintaining efficacy

Inventive Principle:
Principle #24Intermediary (Mediator)

Solution Approach 2:

The patent changes physical or chemical parameters of the formulation system by adjusting pH, ionic strength, or temperature, and by adding viscosity-lowering agents, to transform the rheological properties of the high-concentration solution. This allows the formulation to maintain high drug concentration while achieving a viscosity range suitable for injection through various delivery devices

Inventive Principle:
Principle #35Parameter changes

2Quantity of substance

If polysaccharides and nucleic acids are formulated at high concentrations, then dosage efficiency is improved, but formulation stability deteriorates

Engineering Contradiction:
Improveconcentration of polysaccharide or nucleic acidVSAvoidformulation stability
Core Design Contradiction:
Quantity of substanceVSStability of the object's composition

Solution Approach 1:

The patent employs stability-enhancing excipients and viscosity-lowering agents as intermediaries that prevent aggregation, precipitation, or degradation of polysaccharides and nucleic acids at high concentrations. These agents maintain molecular dispersion and structural integrity, ensuring formulation stability while preserving the high concentration necessary for dosage efficiency

Inventive Principle:
Principle #24Intermediary (Mediator)

Solution Approach 2:

The patent creates composite formulations by combining polysaccharides or nucleic acids with compatible excipients, viscosity-lowering agents, and stabilizers. This composite approach allows the system to simultaneously achieve high concentration, improved stability, and reduced viscosity through synergistic interactions between components

Inventive Principle:
Principle #40Composite materials

3Productivity

If additional energy is applied to fermentation media to reduce viscosity, then mixing efficiency is improved, but organism compatibility deteriorates

Engineering Contradiction:
Improvemixing efficiency in fermentationVSAvoidorganism compatibility
Core Design Contradiction:
ProductivityVSReliability

Solution Approach 1:

The patent introduces viscosity-lowering agents into the fermentation media as intermediaries that reduce viscosity without requiring excessive mechanical energy input. These agents modify the rheological properties of the media, enabling adequate mixing and mass transfer while avoiding high shear stress and temperature that would harm the organisms

Inventive Principle:
Principle #24Intermediary (Mediator)

Solution Approach 2:

The patent changes the chemical composition parameters of the fermentation media by adding viscosity-lowering agents, which fundamentally alters the flow properties. This allows the fermentation process to proceed with reduced energy input while maintaining organism viability and productivity, as the viscosity reduction is achieved through chemical modification rather than intense physical treatment

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 low-viscosity formulations enable rapid and convenient subcutaneous or intramuscular injection, improve injectability, and simplify manufacturing and purification processes, with stability maintained over extended periods.

Implementation Method 1

Because polysaccharides and nucleic acids are both characterized by a high degree of polar functional groups, solutions of these compounds often exhibit significant intramolecular interactions, resulting in high viscosity

Methodology Applied
Scientific EffectViscosity reduction through disruption of intramolecular interactions:

Data Source

PatentUS11471479B2Polysaccharide and nucleic acid formulations containing viscosity-lowering agents
Publication Date: 2022.10.18 EAGLE BIOLOGICS INC
  • US11471479B2 patent drawing
  • US11471479B2 patent drawing
  • US11471479B2 patent drawing

AI summary

Concentrated, low-viscosity, low-volume liquid pharmaceutical formulations of polysaccharides and nucleic acids have been developed. Such formulations can be rapidly and conveniently administered by subcutaneous or intramuscular injection, rather than by lengthy intravenous infusion. These formulations include low-molecular-weight and/or high-molecular-weight polysaccharides and nucleic acids, and viscosity-lowering agents.