Sustained Release Dysoxylum binectariferum Formulation

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Solution Overview

Problem

Rohitukine, a bioactive compound from Dysoxylum binectariferum, has a short biological half-life, leading to decreased efficacy and the need for frequent dosing. Additionally, conventional herbal extract formulations face challenges due to their hygroscopic nature, making them difficult to encapsulate effectively.

Innovation Solution

Development of novel oral sustained release formulations that incorporate rohitukine-rich Dysoxylum binectariferum extract or fraction with biodegradable and non-biodegradable polymers, creating a hydrophilic matrix that slows the release of rohitukine over 16 to 24 hours, thereby enhancing its therapeutic efficacy.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Ease of manufacture

If conventional herbal extract formulations are used, then the formulation is simple to prepare, but the hygroscopic nature of the extract makes it difficult to encapsulate effectively

Engineering Contradiction:

Improveformulation preparationVSAvoidencapsulation

Core Design Contradiction:

Ease of manufactureVSEase of operation

Solution Approach 1:

The patent uses binders and fillers as intermediary materials to bridge the hygroscopic extract and the capsule structure. These intermediaries absorb excess moisture and provide a stable matrix that facilitates encapsulation while maintaining the extract's therapeutic properties.

Inventive Principle:

Principle #24Intermediary (Mediator)

Solution Approach 2:

The formulation creates a composite material system combining the hygroscopic herbal extract with non-hygroscopic excipients, binders, and encapsulating agents. This composite approach maintains the simplicity of extract preparation while solving the encapsulation difficulty through material composition optimization.

Inventive Principle:

Principle #40Composite materials

2Reliability

If frequent dosing is administered to maintain therapeutic levels of rohitukine, then the biological efficacy is improved, but the dosing frequency and patient compliance deteriorate

Engineering Contradiction:

Improvebiological efficacyVSAvoiddosing frequency

Core Design Contradiction:

ReliabilityVSEase of operation

Solution Approach 1:

The sustained-release formulation creates a continuous release profile of rohitukine over 24 hours, maintaining steady plasma concentrations without requiring frequent dosing. This continuous action ensures reliable biological efficacy while improving patient compliance by reducing dosing frequency to once daily.

Inventive Principle:

Principle #20Continuity of useful action

Solution Approach 2:

The patent changes the release rate parameter of rohitukine from rapid (conventional formulation) to sustained (controlled release formulation). This parameter change extends the duration of therapeutic action, allowing less frequent dosing while maintaining reliable biological efficacy throughout the dosing interval.

Inventive Principle:

Principle #35Parameter changes

3Productivity

If sustained release formulation is developed, then the dosing frequency is reduced and therapeutic concentration is maintained, but the formulation complexity increases

Engineering Contradiction:

Improvedosing efficiencyVSAvoidformulation structure

Core Design Contradiction:

ProductivityVSDevice complexity

Solution Approach 1:

The patent achieves sustained release by changing the physical-chemical parameters of the formulation system, including polymer selection, matrix density, and release rate constants. These parameter changes enable 24-hour dosing efficiency without requiring complex multi-component systems or sophisticated delivery mechanisms.

Inventive Principle:

Principle #35Parameter changes

Solution Approach 2:

The formulation uses composite materials consisting of the herbal extract combined with sustained-release polymers and excipients in optimized ratios. This composite approach achieves complex sustained-release functionality through material composition rather than structural complexity, maintaining relatively simple formulation preparation and manufacturing.

Inventive Principle:

Principle #40Composite materials

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 sustained release formulation achieves prolonged systemic availability of rohitukine, reducing dosing frequency and improving therapeutic effectiveness by maintaining steady plasma concentrations over 24 hours, while also addressing the hygroscopicity issues of herbal extracts.

Implementation Method 1

incorporate rohitukine-rich Dysoxylum binectariferum extract or fraction with biodegradable and non-biodegradable polymers, creating a hydrophilic matrix that slows the release of rohitukine over 16 to 24 hours

Methodology Applied

Scientific EffectHydrophilic matrix swelling: Absorption (physical)

Data Source

PatentUS12201727B2Sustained release formulations of <i>Dysoxylum binefacterum</i>

Publication Date: 2025.01.21 COUNCIL OF SCI & IND RES

AI summary

The present invention relates to the novel formulation for sustained or delayed release of rohitukine-rich Dysoxylum binectariferum extract/fraction and a process for preparing the same wherein the extract is wet-granulated using excipients i.e. biodegradable polymers and/or non-biodegradable polymers alone or in combination, and the said granules are either filled into a capsule or compressed into a tablet. The said formulation comprising a granulated extract/fraction of rohitukine-rich Dysoxylum binectariferum with polymers has resulted in a sustained release of the extract or fraction over a period of 16-24 hrs. The said formulations are useful in the treatment of inflammatory diseases.