Dibenzo-α-pyrone Solid Dispersion via Hot Melt Extrusion

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Solution Overview

Problem

Current formulations of natural or synthetic N-alkylamides, such as dibenzo-α-pyrone, face challenges due to low solubility and bioavailability in aqueous phases, leading to restricted manufacturing processes and ineffective bioavailability in biological systems.

Innovation Solution

A composition comprising a thermoformed extrudate of natural or synthetic dibenzo-α-pyrone dispersed within a thermoplastic support, utilizing hot melt extrusion to create a solid dispersion with enhanced solubility and bioavailability, where the dibenzo-α-pyrone is distributed homogeneously within the support, forming a glassy structure with increased bioaccessibility.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If natural or synthetic dibenzo-α-pyrone is used as active substance, then therapeutic efficacy is achieved, but solubility and bioavailability in aqueous phases are low

Engineering Contradiction:

Improvetherapeutic efficacyVSAvoidsolubility

Core Design Contradiction:

ReliabilityVSQuantity of substance

Solution Approach 1:

The patent introduces a thermoplastic support as an intermediary carrier that facilitates the dissolution and absorption of dibenzo-α-pyrone in aqueous environments. The support acts as a bridge between the hydrophobic active substance and hydrophilic biological systems, enabling improved bioavailability without compromising therapeutic efficacy.

Inventive Principle:

Principle #24Intermediary (Mediator)

Solution Approach 2:

The patent modifies the physical state and solubility parameters of dibenzo-α-pyrone by formulating it within a thermoplastic support matrix. This parameter change transforms the compound from a poorly soluble solid to a bioavailable formulation that can be effectively absorbed in aqueous phases, while maintaining its pharmacological activity.

Inventive Principle:

Principle #35Parameter changes

2Ease of manufacture

If conventional formulations are used, then manufacturing is simple, but bioavailability in biological systems is ineffective

Engineering Contradiction:

Improveformulation simplicityVSAvoidbioavailability

Core Design Contradiction:

Ease of manufactureVSReliability

Solution Approach 1:

The patent creates a composite formulation combining dibenzo-α-pyrone with a thermoplastic support material. This composite structure maintains manufacturing simplicity while significantly improving bioavailability, as the composite can be processed using conventional extrusion methods to produce formulations with enhanced biological performance.

Inventive Principle:

Principle #40Composite materials

3Quantity of substance

If dibenzo-α-pyrone is dispersed in thermoplastic support via hot melt extrusion, then solubility and bioavailability are enhanced, but manufacturing process complexity increases

Engineering Contradiction:

ImprovesolubilityVSAvoidmanufacturing process complexity

Core Design Contradiction:

Quantity of substanceVSDevice complexity

Solution Approach 1:

The patent replaces complex multi-step formulation processes with a single hot melt extrusion operation. By using thermal energy to melt the thermoplastic support and simultaneously dissolve the dibenzo-α-pyrone, the process eliminates the need for separate mixing, coating, or encapsulation steps, thereby reducing overall process complexity while achieving enhanced solubility.

Inventive Principle:

Principle #28Mechanics substitution (Replace mechanical system)

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 exhibits significantly improved solubility and bioavailability of dibenzo-α-pyrone, maintaining stability and controlled release over time, particularly in intestinal media, compared to existing formulations.

Implementation Method 1

hot melt extrusion to create a solid dispersion with enhanced solubility and bioavailability, where the dibenzo-α-pyrone is distributed homogeneously within the support, forming a glassy structure

Methodology Applied

Scientific EffectMelting: Melting

Implementation Method 2

The extruder is then used to extrude the mixture under the action of a heating element and a screw, with the aim of obtaining an extrudate in which the active principle and/or the support used are melted to lead to a solid dispersion

Methodology Applied

Scientific EffectShear mixing:

Data Source

PatentUS20240299340A1Composition comprising at least one natural or synthetic dibenzo-alpha-pyrone as active substance and its manufacturing process

Publication Date: 2024.09.12 ELEONOR SPRL

AI summary

Compositions in the form of a thermoformed extrudate, possibly packaged in pellet, flake, granule, powder, effervescent tablet or not, in injectable solution or not, in drink, in suspension, in gel, in ointment or in any other suitable form allowing administration to an animal or a human being, comprising at least one natural or synthetic dibenzo-α-pyrone as active substance and at least one natural or synthetic support.