Potassium Phosphate Injection SiO2 Coated Vials

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Solution Overview

Problem

Potassium Phosphate Injection (PPI) products face issues with visible particulates and high aluminum content, leading to product recalls and safety concerns, especially for patients with renal insufficiency, due to inadequate storage conditions and composition.

Innovation Solution

A sterile composition comprising about 175 mg/mL potassium monobasic phosphate and 300 mg/mL potassium dibasic phosphate, with a sufficient water vehicle to maintain a total phosphate concentration of 3 mmol/mL, is developed, along with a manufacturing process that includes filtration through a 0.2 μm membrane and storage in glass or plastic vials with SiO2 coatings to minimize aluminum leaching, ensuring no visible particles and reduced aluminum content.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If conventional potassium phosphate injection formulations are stored in glass vials, then the product maintains stability, but aluminum leaching from glass increases over time causing toxicity concerns

Engineering Contradiction:
Improveproduct stabilityVSAvoidaluminum toxicity
Core Design Contradiction:
ReliabilityVSObject-affected harmful factors

Solution Approach 1:

A coating layer comprising silicon oxide (SiO2) or silicon oxynitride (SiOxNy) is applied to the inner surface of the glass vial. This coating acts as an intermediary barrier between the potassium phosphate injection and the glass, preventing aluminum leaching while maintaining product stability. The coating has been demonstrated to reduce aluminum content to below detectable levels after extended storage.

Inventive Principle:
Principle #24Intermediary (Mediator)

Solution Approach 2:

The glass vial is combined with a silicon-based coating material to create a composite structure. The glass provides mechanical strength and containment, while the silicon oxide or silicon oxynitride coating provides chemical inertness and prevents metal ion leaching. This composite approach resolves the contradiction between glass stability and aluminum toxicity.

Inventive Principle:
Principle #40Composite materials

2Quantity of substance

If concentrated potassium phosphate solution is stored, then the product remains effective for treatment, but visible particulates form compromising safety

Engineering Contradiction:
Improvephosphate concentrationVSAvoidvisible particulates
Core Design Contradiction:
Quantity of substanceVSObject-affected harmful factors

Solution Approach 1:

The pH of the potassium phosphate injection is adjusted and controlled within a specific range (pH 6.5-7.5). This parameter change prevents the formation of precipitates and visible particulates while maintaining the concentrated phosphate formulation (3 mmol/mL). The optimized pH ensures solubility of both potassium monobasic phosphate and potassium dibasic phosphate at the required concentrations.

Inventive Principle:
Principle #35Parameter changes

3Quantity of substance

If high concentrations of potassium phosphates are formulated, then treatment efficacy is improved, but the risk of particulate formation and aluminum leaching increases

Engineering Contradiction:
Improvephosphate concentrationVSAvoidparticulate matter and aluminum content
Core Design Contradiction:
Quantity of substanceVSObject-generated harmful factors

Solution Approach 1:

The silicon-based coating on the glass vial serves as a protective intermediary that prevents aluminum leaching into the concentrated phosphate solution, enabling high-concentration formulations without the harmful effect of aluminum toxicity.

Inventive Principle:
Principle #24Intermediary (Mediator)

Solution Approach 2:

The pH is optimized to maintain high phosphate concentrations while preventing precipitation. By controlling pH within the 6.5-7.5 range, the formulation achieves maximum solubility of potassium phosphates, allowing concentrated therapy without particulate formation.

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 solution effectively prevents the formation of visible particulates and significantly reduces aluminum content in the composition, ensuring product stability and safety for extended storage periods, meeting regulatory aluminum limits and maintaining efficacy for treating hypophosphatemia with reduced patient exposure to toxic aluminum levels.

Implementation Method 1

storage in glass or plastic vials with SiO2 coatings to minimize aluminum leaching

Methodology Applied
Scientific EffectAdsorption: Adsorption

Implementation Method 2

manufacturing process that includes filtration through a 0.2 μm membrane

Methodology Applied
Scientific EffectFiltration: Filter (physical)

Data Source

PatentUS10632150B1Potassium phosphates composition for injection
Publication Date: 2020.04.28 CMP DEVELOPMENT LLC

AI summary

Disclosed herein is a sterile composition for injection comprised of potassium phosphates having no visible particulate. Also disclosed herein is a manufacturing process for the sterile composition and its use.