Menaquinone-9 Nanoparticles for Solubility and Absorption

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Solution Overview

Problem

Existing formulations of vitamin K2, particularly MK-9, suffer from poor solubility and stability issues, limiting their effectiveness in treating conditions associated with vitamin K deficiency, such as cardiovascular disease and bone diseases in patients with chronic kidney disease, due to low absorption in the gastrointestinal tract.

Innovation Solution

Development of nano-sized particles of vitamin K2, specifically MK-9, with sizes ranging from 0.1 nm to 1,000 nm, stabilized by emulsifiers and bioavailability enhancers, enhancing solubility and absorption in the body.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If vitamin K2 (MK-9) is administered in conventional formulations, then it provides vitamin K supplementation, but it suffers from poor solubility and low absorption in the gastrointestinal tract

Engineering Contradiction:

Improveabsorption effectivenessVSAvoidsolubility

Core Design Contradiction:

ReliabilityVSQuantity of substance

Solution Approach 1:

The vitamin K2 (MK-9) is formulated as nano-sized particles with sizes ranging from 0.1 nm to 1,000 nm. This segmentation of the vitamin into nanoscale particles dramatically increases the surface area and improves solubility in the gastrointestinal tract, thereby enhancing absorption effectiveness while maintaining adequate quantity of the active substance.

Inventive Principle:

Principle #1Segmentation

2Reliability

If conventional vitamin K2 formulations are used, then they can be administered, but they exhibit poor stability issues that limit effectiveness

Engineering Contradiction:

Improvetreatment effectivenessVSAvoidformulation stability

Core Design Contradiction:

ReliabilityVSStability of the object's composition

Solution Approach 1:

The patent employs stabilizing agents and emulsifiers as intermediary substances to protect the nano-sized vitamin K2 particles from degradation. These intermediaries form protective matrices around the unstable vitamin molecules, preventing oxidation and degradation while maintaining treatment effectiveness throughout the shelf life and during gastrointestinal transit.

Inventive Principle:

Principle #24Intermediary (Mediator)

3Quantity of substance

If nano-sized particles of MK-9 are developed, then solubility and absorption are enhanced, but formulation complexity increases due to need for stabilizers and emulsifiers

Engineering Contradiction:

ImprovesolubilityVSAvoidformulation complexity

Core Design Contradiction:

Quantity of substanceVSDevice complexity

Solution Approach 1:

The patent creates a composite formulation system that integrates nano-sized MK-9 particles with stabilizing agents and emulsifiers into a unified nanosuspension or nanoparticle formulation. This composite approach combines multiple functional components (vitamin core, stabilizing matrix, emulsifying agents) into a single integrated system that achieves enhanced solubility while managing the inherent complexity through synergistic interactions between components.

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 nano-sized particles significantly increase serum levels of MK-9, effectively treating conditions like vascular calcification, bone diseases, and other vitamin K-related disorders by improving solubility and bioavailability.

Implementation Method 1

nanoparticles of vitamin K2, specifically MK-9, with sizes ranging from 0.1 nm to 1,000 nm, stabilized by emulsifiers and bioavailability enhancers, enhancing solubility and absorption in the body

Methodology Applied

Scientific EffectNanoparticle dissolution: Solvation