L-Ascorbic Acid Co-Administration to Block Statin-Induced Vascular Calcification

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Solution Overview

Problem

Statins, despite their benefits in reducing cardiovascular disease risk, induce vascular calcification, a significant risk factor for heart disease, and existing treatments do not effectively mitigate this side effect.

Innovation Solution

Concomitant administration of L-ascorbic acid or ascorbate with statins, either alone or in a pharmaceutical composition, to prevent or treat vascular calcification, potentially combined with coenzyme Q10 and other micronutrients, to counteract the calcification process.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If statins are administered to reduce LDL cholesterol and prevent cardiovascular disease, then cardiovascular protection is improved, but vascular calcification increases

Engineering Contradiction:
Improvecardiovascular protectionVSAvoidvascular calcification
Core Design Contradiction:
ReliabilityVSObject-affected harmful factors

Solution Approach 1:

Vitamin C acts as an intermediary substance that mediates between statin therapy and vascular calcification. The patent shows that vitamin C co-administration blocks the calcification-inducing effects of statins on vascular smooth muscle cells, allowing statins to maintain their cardiovascular protective effects while preventing the harmful calcification side effect through the intermediary action of vitamin C

Inventive Principle:
Principle #24Intermediary (Mediator)

Solution Approach 2:

The patent converts the harmful effect of statin-induced calcification into a beneficial outcome by using vitamin C to transform the calcification process. Instead of allowing calcification to proceed as a harmful side effect, vitamin C redirects the process to produce stable plaque formations that are less prone to rupture, thereby converting a harmful effect into a potentially beneficial structural stabilization

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

2Reliability

If statins are used for primary and secondary prevention of cardiovascular disease, then cardiovascular risk is reduced, but vascular calcification develops

Engineering Contradiction:
Improvecardiovascular risk reductionVSAvoidvascular calcification
Core Design Contradiction:
ReliabilityVSObject-generated harmful factors

Solution Approach 1:

Vitamin C is administered concurrently with statins to preemptively counteract the calcification-inducing effects before they can manifest as harmful vascular calcification. The patent demonstrates that vitamin C pre-treatment or co-treatment blocks the activation of calcification pathways in vascular smooth muscle cells that would otherwise be triggered by statin therapy

Inventive Principle:
Principle #9Preliminary anti-action

3Stability of the object's composition

If statin therapy is administered to lower LDL cholesterol, then atherosclerosis progression is slowed, but arterial calcification increases

Engineering Contradiction:
Improveatherosclerosis progressionVSAvoidarterial calcification
Core Design Contradiction:
Stability of the object's compositionVSObject-affected harmful factors

Solution Approach 1:

Vitamin C serves as a mediating substance that allows statins to maintain their beneficial effect of slowing atherosclerosis progression while simultaneously blocking the harmful calcification pathway. The patent shows that vitamin C interferes with the statin-induced differentiation of vascular smooth muscle cells into osteoblastic cells, thereby preventing arterial calcification without compromising the anti-atherosclerotic effects

Inventive Principle:
Principle #24Intermediary (Mediator)

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

L-ascorbic acid effectively inhibits vascular calcification by reducing alkaline phosphatase activity and calcium accumulation in smooth muscle cells, thereby mitigating the calcification process induced by statins, thus addressing the conflicting evidence on statin effects on cardiovascular health.

Implementation Method 1

L-ascorbic acid effectively inhibits vascular calcification by reducing alkaline phosphatase activity and calcium accumulation in smooth muscle cells

Methodology Applied
Scientific EffectEnzyme inhibition: Enzyme

Implementation Method 2

L-ascorbic acid effectively inhibits vascular calcification by reducing alkaline phosphatase activity and calcium accumulation in smooth muscle cells

Methodology Applied
Scientific EffectCalcium chelation or reduction:

Data Source

PatentUS11590103B2Ascorbate in the prevention of statin induced vascular calcification
Publication Date: 2023.02.28 RATH MATTHIAS
  • US11590103B2 patent drawing
  • US11590103B2 patent drawing
  • US11590103B2 patent drawing

AI summary

A method of treating or preventing vascular calcification in a patient by administering L-ascorbic acid or ascorbate to the patient and a pharmaceutical composition containing at least one statin and L-ascorbic acid or ascorbate in a dosage form that allows for the concomitant administering of the at least one statin and L-ascorbic acid or ascorbate to a patient.