Meldonium Orotate Cardioprotection in Myocardial Infarction

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Solution Overview

Problem

Current treatments for cardiovascular diseases, such as myocardial infarction and arrhythmia, do not fully leverage the cardioprotective properties of Meldonium, particularly in terms of its salt forms, which lack documented efficacy.

Innovation Solution

Meldonium orotate is introduced as a more stable and effective form, demonstrating cardioprotective effects in myocardial infarction models and reducing fatal outcomes in acute arrhythmia, surpassing the efficacy of Meldonium dihydrate and orotic acid alone.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If Meldonium dihydrate is used for treating cardiovascular diseases, then cardioprotective effects are achieved, but the treatment efficacy is limited compared to salt forms

Engineering Contradiction:
Improvetreatment efficacyVSAvoidsalt form utilization
Core Design Contradiction:
ReliabilityVSAdaptability or versatility

Solution Approach 1:

The patent applies parameter changes by transforming Meldonium from its dihydrate form into various salt forms (orotate, ascorbate, nicotinates, etc.). This chemical parameter transformation enhances the cardioprotective efficacy while maintaining the core mechanism of action. The salt forms demonstrate superior treatment effectiveness compared to the dihydrate form, resolving the contradiction between limited efficacy and potential for improved formulations.

Inventive Principle:
Principle #35Parameter changes

2Reliability

If conventional treatments for myocardial infarction and arrhythmia are used, then standard care is provided, but cardioprotective properties of Meldonium are not fully leveraged

Engineering Contradiction:
Improvecardioprotective effectVSAvoidtreatment optimization
Core Design Contradiction:
ReliabilityVSProductivity

Solution Approach 1:

The patent transforms conventional Meldonium dihydrate into enhanced salt forms with improved cardioprotective properties. This parameter change in chemical structure translates to superior clinical efficacy in treating myocardial infarction and arrhythmia, fully leveraging and enhancing the cardioprotective potential beyond standard care.

Inventive Principle:
Principle #35Parameter changes

Solution Approach 2:

The patent creates composite pharmaceutical formulations by combining Meldonium with various counterions to form salt compounds. These composite materials (Meldonium orotate, Meldonium ascorbate, etc.) exhibit enhanced therapeutic effects compared to the parent compound alone, resolving the contradiction between standard treatment and optimized therapy.

Inventive Principle:
Principle #40Composite materials

3Reliability

If Meldonium orotate is used instead of Meldonium dihydrate, then treatment efficacy is enhanced, but the formulation complexity increases

Engineering Contradiction:
Improvetreatment efficacyVSAvoidformulation complexity
Core Design Contradiction:
ReliabilityVSDevice complexity

Solution Approach 1:

The patent applies parameter changes by selecting specific counterions (orotate, ascorbate, nicotinates) that enhance Meldonium's efficacy. While this creates multiple possible formulations, each individual salt form maintains a straightforward chemical structure and manufacturing process, balancing enhanced efficacy with manageable formulation complexity.

Inventive Principle:
Principle #35Parameter changes

Data Source

PatentEP2070529B1Medical use of 3-(2,2,2-trimethylhydrazinium) propionate orotate
Publication Date: 2011.10.12 JOINT STOCK COMPANY GRINDEKS
  • EP2070529B1 patent drawing
  • EP2070529B1 patent drawing

AI summary

The present invention relates to highly effective treatment of cardiovascular diseases with 3-(2,2,2-trimethylhydrazinium)propionate orotate.