Methyl Cyclodextrin Compositions for HDL Elevation

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Solution Overview

Problem

Current treatments for atherosclerosis and related complications, such as atheromatous plaque formation, do not effectively increase HDL cholesterol levels, and existing drugs have limitations in therapeutic benefits and side effects, with no available medication capable of actively combating these conditions by elevating HDL cholesterol.

Innovation Solution

Pharmaceutical compositions based on methyl cyclodextrin with a specific degree of molar substitution between 0.05 and 1.5 are used to increase HDL cholesterol levels, reducing atheromatous plaques and associated complications, including cardiovascular diseases and central nervous system disorders like Alzheimer's and Niemann-Pick disease.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If conventional treatments for atherosclerosis are used, then some therapeutic effect is achieved, but HDL cholesterol levels are not effectively increased

Engineering Contradiction:

Improvetherapeutic benefitVSAvoidHDL cholesterol level

Core Design Contradiction:

ReliabilityVSQuantity of substance

Solution Approach 1:

The patent changes the chemical structure parameters of cyclodextrin by introducing methyl groups at specific positions (C2, C3, C6) with controlled molar substitution degrees (0.05-1.5), transforming it into methyl cyclodextrin derivatives that selectively interact with HDL cholesterol to increase its levels in the blood

Inventive Principle:

Principle #35Parameter changes

Solution Approach 2:

Methyl cyclodextrin acts as an intermediary substance that facilitates the transport and accumulation of HDL cholesterol in the bloodstream, mediating between cholesterol metabolism and the desired therapeutic effect of increasing protective HDL levels

Inventive Principle:

Principle #24Intermediary (Mediator)

2Reliability

If existing drugs are used to treat atherosclerosis, then some therapeutic effect is achieved, but side effects and limitations in therapeutic benefits occur

Engineering Contradiction:

Improvetherapeutic benefitVSAvoidside effects

Core Design Contradiction:

ReliabilityVSObject-affected harmful factors

Solution Approach 1:

The patent employs cyclodextrin derivatives that are naturally metabolized and excreted, avoiding the accumulation of harmful substances in the body. The methyl cyclodextrin compounds are designed to be biodegradable, eliminating long-term toxicity concerns associated with conventional cholesterol-lowering drugs

Inventive Principle:

Principle #27Cheap short-living objects (Disposable)

Solution Approach 2:

The patent converts the potential harm of cholesterol accumulation into a benefit by selectively targeting HDL cholesterol enhancement rather than broadly suppressing cholesterol synthesis, thereby treating atherosclerosis while avoiding the side effects of conventional statins and other cholesterol-modifying drugs

Inventive Principle:

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

3Quantity of substance

If no medication is available to actively combat atherosclerosis by elevating HDL cholesterol, then current treatments have limitations, but the need for effective HDL-elevating therapy remains unmet

Engineering Contradiction:

ImproveHDL cholesterol levelVSAvoidtherapeutic application range

Core Design Contradiction:

Quantity of substanceVSAdaptability or versatility

Solution Approach 1:

The patent develops methyl cyclodextrin derivatives that can be applied across multiple therapeutic scenarios including atherosclerosis treatment, prevention of cardiovascular diseases, and treatment of central nervous system disorders, making a single compound class universally applicable to diverse conditions

Inventive Principle:

Principle #6Universality (Multi-functionality)

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 compositions effectively elevate HDL cholesterol, reduce circulating fatty acids and triglycerides, and decrease atheromatous plaque surface area without the need for phospholipid vesicles, offering a therapeutic approach for atherosclerosis and central nervous system diseases without toxicity.

Implementation Method 1

The present invention relates to pharmaceutical compositions which make it possible to increase the HDL cholesterol level in an individual

Methodology Applied

Scientific EffectComplexation:

Implementation Method 2

The compositions effectively elevate HDL cholesterol, reduce circulating fatty acids and triglycerides

Methodology Applied

Scientific EffectMetabolic modulation:

Data Source

PatentUS11266680B2Compositions based on methyl cyclodextrins for the treatment and/or prevention of diseases by increasing the HDL cholesterol level

Publication Date: 2022.03.08 ROQUETTE FRERES SA

AI summary

Pharmaceutical composition and their uses are disclosed, the composition comprising at least one methyl cyclodextrin having a molar substitution (MS) degree of between 0.05 and 1.5 in the treatment and/or prevention of diseases that can be treated and/or prevented by an increase in the HDL cholesterol level.