Trigonelline and 4-Hydroxyisoleucine Composition for Dopaminergic Activity

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Solution Overview

Problem

Current treatments for dopamine-related disorders, such as Parkinson's disease, often have significant side effects and do not effectively inhibit neuronal degeneration, while anti-psychotic drugs can cause immobility due to dopamine receptor blockade, necessitating a more effective and gentler therapy with minimal side effects.

Innovation Solution

A pharmaceutical composition comprising trigonelline or its derivatives and 4-hydroxyisoleucine, optionally with excipients, is developed to enhance dopaminergic activity, inhibit prolactin secretion, and act as a muscle relaxant, which is extracted from plant sources and formulated into various dosage forms.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If current treatments for dopamine-related disorders are used, then dopamine levels are increased, but significant side effects occur and neuronal degeneration is not effectively inhibited

Engineering Contradiction:
Improveeffectiveness of treatmentVSAvoidside effects
Core Design Contradiction:
ReliabilityVSObject-affected harmful factors

Solution Approach 1:

The patent changes the chemical parameters by using a combination of trigonelline and 4-hydroxyisoleucine in specific ratios (trigonelline: 30-90%, 4-hydroxyisoleucine: 10-70%) to achieve optimal dopaminergic activity while reducing side effects. This parameter optimization resolves the contradiction between treatment effectiveness and harmful side effects

Inventive Principle:
Principle #35Parameter changes

Solution Approach 2:

The patent creates a composite pharmaceutical composition combining two active ingredients (trigonelline and 4-hydroxyisoleucine) with complementary mechanisms of action. Trigonelline provides dopaminergic activity while 4-hydroxyisoleucine serves as a precursor for dopamine synthesis, creating a synergistic effect that improves reliability while minimizing harmful factors

Inventive Principle:
Principle #40Composite materials

2Object-affected harmful factors

If anti-psychotic drugs are used to block dopamine receptors, then psychotic symptoms are reduced, but immobility occurs due to dopamine receptor blockade

Engineering Contradiction:
Improvepsychotic symptomsVSAvoidimmobility
Core Design Contradiction:
Object-affected harmful factorsVSObject-generated harmful factors

Solution Approach 1:

The patent uses trigonelline and 4-hydroxyisoleucine as intermediary substances that indirectly modulate dopamine activity rather than directly blocking receptors. This intermediary approach allows symptom management without the severe motor side effects caused by direct receptor blockade, resolving the contradiction between reducing psychotic symptoms and maintaining mobility

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

The composition demonstrates dopaminergic activity, reducing symptoms of Parkinson's disease, inhibiting prolactin levels, and minimizing side effects from dopamine receptor antagonists, with selective Monoamine Oxidase-B inhibition and no interaction with tyramine, thus providing a safer and more effective treatment for dopamine-related disorders.

Implementation Method 1

selective Monoamine Oxidase-B inhibition

Methodology Applied
Scientific EffectEnzyme inhibition: Enzyme

Data Source

PatentUS9149469B2Pharmaceutical composition and a process thereof
Publication Date: 2015.10.06 INDUS BIOTECH PVT
  • US9149469B2 patent drawing
  • US9149469B2 patent drawing
  • US9149469B2 patent drawing

AI summary

The present invention relates to a pharmaceutical composition having dopaminergic activity and other related pharmaceutical activities comprising trigonelline or its derivative(s) and 4-hydroxyisoleucine or its derivative(s), optionally along with excipients(s); a process of preparing a pharmaceutical composition comprising trigonelline or its derivative(s) and 4-hydroxyisoleucine or its derivative(s), optionally along with excipients(s), wherein the process comprising steps of: (a) extracting a clear solution containing trigonelline and 4-hydroxyisoleucine from plant source; and (b) optionally precipitating derivative(s) of trigonelline and 4-hydroxyisoleucine from the clear solution and obtaining said composition; and an in-vitro method to increase levels of dopamine or to inhibit prolactin by allowing composition comprising trigonelline or its derivative(s) and 4-hydroxyisoleucine or its derivative(s) to bind to cell receptors.