Coated Pharmaceutical Vessel Reducing Polysorbate Degradation

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Solution Overview

Problem

Biologic drug formulations, particularly those containing polysorbates, face challenges with polysorbate degradation over time, leading to increased protein aggregation and particle formation, which reduces the stability of the drug product and requires higher polysorbate concentrations to compensate, potentially causing adverse reactions in patients.

Innovation Solution

A pharmaceutical package with a coating on the interior surface of the vessel, comprising SiwOxCy or SiwNxCy, that reduces polysorbate degradation, thereby minimizing protein aggregation and particle formation, allowing for lower polysorbate concentrations and improved stability of the drug product.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If high concentrations of polysorbate are used to compensate for degradation, then the stabilizing effect is maintained, but adverse reactions in patients increase

Engineering Contradiction:

Improvestabilizing effectVSAvoidadverse reactions

Core Design Contradiction:

ReliabilityVSObject-affected harmful factors

Solution Approach 1:

A coating layer is introduced as an intermediary between the polysorbate and the vessel wall. This coating prevents direct contact and interaction between the polysorbate and the vessel material, thereby reducing degradation mechanisms while maintaining the stabilizing function of the polysorbate in the drug formulation.

Inventive Principle:

Principle #24Intermediary (Mediator)

Solution Approach 2:

The patent replaces the conventional approach of using high concentrations of polysorbate (a chemical solution) with a physical barrier coating system. This substitution allows for reduced polysorbate concentrations in the formulation while maintaining stability, thus reducing adverse reactions.

Inventive Principle:

Principle #28Mechanics substitution (Replace mechanical system)

2Duration of action of stationary object

If high concentrations of polysorbate are used to account for degradation, then the shelf-life is extended, but the risk of adverse reactions increases

Engineering Contradiction:

Improveshelf-lifeVSAvoidadverse reactions

Core Design Contradiction:

Duration of action of stationary objectVSObject-affected harmful factors

Solution Approach 1:

The coating acts as a protective intermediary that prevents polysorbate degradation at the vessel wall interface. This extends the effective shelf-life by maintaining polysorbate stability without requiring elevated concentrations that would cause adverse reactions.

Inventive Principle:

Principle #24Intermediary (Mediator)

Solution Approach 2:

The patent changes the physical-chemical parameters at the vessel wall interface through coating application. This modifies the local environment to prevent polysorbate degradation, thereby extending shelf-life while allowing use of lower, safer polysorbate concentrations in the formulation.

Inventive Principle:

Principle #35Parameter changes

3Device complexity

If polysorbate degradation is allowed to occur naturally, then the formulation remains simple, but protein aggregation and particle formation increase

Engineering Contradiction:

Improveformulation simplicityVSAvoidprotein aggregation

Core Design Contradiction:

Device complexityVSStability of the object's composition

Solution Approach 1:

The coating serves as a protective intermediary layer that prevents polysorbate from degrading and forming aggregates. This maintains formulation simplicity while preventing protein aggregation and particle formation through the physical barrier provided by the coating.

Inventive Principle:

Principle #24Intermediary (Mediator)

Solution Approach 2:

The patent converts the potential harm of polysorbate degradation (which causes protein aggregation) into a benefit by using the coating to prevent degradation. The coating transforms the unstable interface between polysorbate and vessel wall into a stable, protective boundary.

Inventive Principle:

Principle #22Blessing in disguise (Convert harm into benefit)

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 coating significantly reduces polysorbate degradation and associated protein aggregation, extending the shelf-life of the drug product and reducing adverse reactions by maintaining stability and minimizing the need for high polysorbate levels.

Implementation Method 1

A pharmaceutical package with a coating on the interior surface of the vessel, comprising SiwOxCy or SiwNxCy, that reduces polysorbate degradation

Methodology Applied

Scientific EffectPhysical barrier:

Data Source

PatentUS20230303305A1Method and package for reducing the degradation of a drug and/or excipient, e.g. polysorbate stabilizer, in a pharmaceutical product

Publication Date: 2023.09.28 SIO2 MEDICAL PRODUCTS LLC

AI summary

The present disclosure is directed to a vessel having a lumen defined at least in part by a wall, the wall having an interior surface facing the lumen, and the interior surface comprising a coating. The coating is configured to prevent the leaching of metal ions from the vessel wall into a fluid contained within the lumen and stored in contact with the coating. The vessels are used to store an aqueous drug product, typically an aqueous drug product containing an active agent and one or more excepients, such as a polysorbate stabilizer. The coated vessels are effective to reduce degradation of the active agent and/or one or more excipients, e.g. a polysorbate stabilizer.