Carrier Composition for Biologically Active Compound Delivery

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Solution Overview

Problem

Current drug delivery technologies face challenges in compatibility with pharmaceutical compounds, maintaining effective duration, and patient convenience, often resulting in suboptimal bioavailability and increased side effects.

Innovation Solution

A carrier composition comprising a mixture of mono-(tocopheryl) phosphate and di-(tocopheryl) phosphate as an electron transfer agent combined with a high concentration of a polar protic solvent, such as C2-C3 acyclic alcohols, to enhance the delivery of lipophilic biologically active compounds with a logP value between 1 and 5 and a molecular mass less than 1000 Daltons.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If conventional drug delivery technologies are used, then drug administration is achieved, but bioavailability is suboptimal and side effects increase

Engineering Contradiction:
ImprovebioavailabilityVSAvoidside effects
Core Design Contradiction:
ReliabilityVSObject-affected harmful factors

Solution Approach 1:

The patent introduces a carrier composition as an intermediary system comprising C1-C4 alcohols, polyols, polymers, water, and electron transfer agent phosphate derivatives. This carrier composition mediates between the pharmaceutical compound and the biological system, improving bioavailability through enhanced solubility and stability while reducing side effects by controlling drug release and minimizing unwanted interactions.

Inventive Principle:
Principle #24Intermediary (Mediator)

Solution Approach 2:

The patent employs a composite carrier composition integrating multiple components (C1-C4 alcohols, polyols, polymers, water, and electron transfer agent phosphate derivatives) that work synergistically. This composite material provides improved drug solubility, stability, and controlled release properties, thereby enhancing bioavailability and reducing side effects compared to conventional single-component delivery systems.

Inventive Principle:
Principle #40Composite materials

2Duration of action of moving object

If drug delivery duration is extended, then therapeutic effect is maintained, but compatibility issues arise

Engineering Contradiction:
ImprovedurationVSAvoidcompatibility
Core Design Contradiction:
Duration of action of moving objectVSStability of the object's composition

Solution Approach 1:

The patent modifies the chemical and physical parameters of the drug delivery system by incorporating electron transfer agent phosphate derivatives and optimizing the composition ratios of C1-C4 alcohols, polyols, and polymers. These parameter changes enhance the stability and compatibility of the formulation over extended periods, allowing for prolonged therapeutic action without compromising composition integrity.

Inventive Principle:
Principle #35Parameter changes

3Speed

If drug release is accelerated, then onset is shortened, but control over release becomes difficult

Engineering Contradiction:
ImproveonsetVSAvoidrelease control
Core Design Contradiction:
SpeedVSEase of operation

Solution Approach 1:

The patent creates a dynamic drug release system where the carrier composition can adjust its release characteristics. The electron transfer agent phosphate derivatives and the combination of C1-C4 alcohols, polyols, and polymers provide a balanced release mechanism that achieves rapid onset when needed while maintaining controllable release profiles through the synergistic interactions of the carrier components.

Inventive Principle:
Principle #15Dynamics

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 carrier composition improves the bioavailability and transdermal delivery of biologically active compounds, reducing side effects and extending the duration of action while shortening onset, thereby enhancing patient compliance and therapeutic efficacy.

Implementation Method 1

a phosphate compound of an electron transfer agent which is mixture of a mono-(tocopheryl) phosphate and a di-(tocopheryl) phosphate

Methodology Applied
Scientific EffectElectron transfer: Redox Reactions

Implementation Method 2

a polar protic solvent, wherein the polar protic solvent is a C2-C3 acyclic alcohol; and the polar protic solvent concentration is within the range of 60%w/w to 90%w/w of the total concentration of the carrier composition

Methodology Applied
Scientific EffectSolvation: Solvation

Data Source

PatentEP2516011B1Carrier composition for delivery of a biologically active compound
Publication Date: 2017.07.12 PHOSPHAGENICS LTD
  • EP2516011B1 patent drawingFigure 1
  • EP2516011B1 patent drawingFigure 2A~2B
  • EP2516011B1 patent drawingFigure 3

AI summary

A carrier composition of the present invention comprises a phosphate compound of an electron transfer agent and a relatively high concentration of a polar protic solvent. A biologically active compound may be formulated with a carrier composition of the present invention to provide a formulation.