Composite Structural Material Sustained Release Formulation

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Solution Overview

Problem

Current sustained release formulations using hydrophilic polymer materials face challenges such as water absorption leading to stability issues, production waste, and environmental concerns due to the use of organic solvents, particularly when dealing with low or high water-soluble active pharmaceutical ingredients.

Innovation Solution

A composite structural material comprising a hydrophobic and hydrophilic material blend, with specific ratios, is used to create a sustained release formulation that reduces water absorption and simplifies production, allowing for controlled release of active pharmaceutical ingredients over an extended period without the need for excessive organic solvents.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Duration of action of moving object

If hydrophilic polymer materials are used as sustained release matrix, then sustained release effect is achieved, but water absorption causes stability issues and production waste

Engineering Contradiction:
Improvesustained release durationVSAvoidproduction waste
Core Design Contradiction:
Duration of action of moving objectVSLoss of substance

Solution Approach 1:

The patent uses a composite structural material comprising both hydrophobic structural material and hydrophilic structural material. The hydrophobic material (e.g., fatty acid glycerides, waxes) provides water resistance and structural stability, while the hydrophilic material (e.g., HPMC, HPC) enables sustained release through controlled water absorption and gel formation. This composite approach allows the formulation to achieve sustained release duration while reducing excessive water absorption and production waste.

Inventive Principle:
Principle #40Composite materials

2Duration of action of moving object

If hydrophilic structural materials are used for sustained release, then drug release is controlled, but film coating becomes difficult

Engineering Contradiction:
Improvecontrolled release durationVSAvoidfilm coating difficulty
Core Design Contradiction:
Duration of action of moving objectVSEase of manufacture

Solution Approach 1:

The composite structural material combines hydrophobic materials (which provide good film-forming properties and water resistance) with hydrophilic materials (which provide sustained release capability). The hydrophobic component facilitates film coating processes by providing a stable, water-resistant matrix that can be properly coated, while the hydrophilic component ensures controlled drug release through gel formation.

Inventive Principle:
Principle #40Composite materials

3Duration of action of moving object

If sustained release formulation absorbs water easily, then drug release is sustained, but drug stability is affected in storage

Engineering Contradiction:
Improvesustained release effectVSAvoiddrug stability
Core Design Contradiction:
Duration of action of moving objectVSStability of the object's composition

Solution Approach 1:

The hydrophobic structural material in the composite formulation provides a water-resistant barrier that limits excessive water absorption during storage, thereby maintaining drug stability. Simultaneously, the hydrophilic structural material enables sustained release by absorbing sufficient water to form a gel matrix that controls drug diffusion. The synergistic combination balances water absorption needs for sustained release with water resistance needs for stability.

Inventive Principle:
Principle #40Composite materials

4Duration of action of moving object

If osmotic pump technology is used, then sustained release is achieved, but large amounts of organic solvents are required

Engineering Contradiction:
Improvesustained release durationVSAvoidorganic solvent consumption
Core Design Contradiction:
Duration of action of moving objectVSLoss of substance

Solution Approach 1:

The patent eliminates the need for osmotic pump technology and its associated organic solvents by using a simpler composite structural material approach. The sustained release is achieved through the natural gel formation and diffusion properties of the hydrophilic material combined with the water-resistant matrix of the hydrophobic material, removing the requirement for complex osmotic mechanisms and large amounts of organic solvents.

Inventive Principle:
Principle #2Taking out (Extraction)

5Duration of action of moving object

If laser drilling is used after film coating, then sustained release formulation is completed, but rejection rate is high and process is complicated

Engineering Contradiction:
Improvesustained release formulation completionVSAvoidprocess complexity
Core Design Contradiction:
Duration of action of moving objectVSDevice complexity

Solution Approach 1:

The patent removes the laser drilling step from the formulation process by designing a composite structural material that achieves sustained release through its inherent gel formation and diffusion properties. The hydrophilic material forms a gel matrix upon water absorption that naturally controls drug release, eliminating the need for complex laser drilling operations to create release channels, thereby reducing process complexity and rejection rate.

Inventive Principle:
Principle #2Taking out (Extraction)

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 composite material ensures stable and controlled release of pharmaceuticals over 4 to 24 hours, reducing production costs and environmental impact while enabling the formulation of high-dose, water-soluble, and insoluble active ingredients.

Implementation Method 1

a composite structural material comprising a hydrophobic structural material and a hydrophilic structural material

Methodology Applied
Scientific EffectHydrophobic effect: Hydrophobe

Implementation Method 2

a composite structural material comprising a hydrophobic structural material and a hydrophilic structural material

Methodology Applied
Scientific EffectHydrophilic effect: Hydrophile

Implementation Method 3

water insinuates into tablet to dissolve active pharmaceutical ingredients, and make hydrophilic structural materials swell to form high viscosity gel

Methodology Applied
Scientific EffectSwelling:

Implementation Method 4

For the active pharmaceutical ingredients having lower or higher pKa value, the pH of dissolution medium has great influence on solubility and dissolution of drugs

Methodology Applied
Scientific EffectpH-dependent solubility:

Data Source

PatentUS10507185B2Composite structural material and pharmaceutical composition thereof
Publication Date: 2019.12.17 INNOVACO PHARMA INC

AI summary

A composite structural material and pharmaceutical composition comprising same, the use of the composite structural material in preparing a sustained release formulation, and a pharmaceutical composition formulation method; the composite structural material comprises a hydrophobic structural material and a hydrophilic structural material; the proportion of the hydrophobic structural material to the hydrophilic structural material ranges from 1:0.01 to 1:5, preferably 1:0.05 to 1:4, more preferably 1:0.1 to 1:3, and most preferably 1:0.4 to 1:2, such as 1:0.4 to 1:1.3. The pharmaceutical composition comprises the composite structural material and one or more active pharmaceutical ingredients, and preferably the proportion of the composite structural material to the active pharmaceutical ingredients ranges from 1:0.01 to 1:8, more preferably 1:0.02 to 1:5, and most preferably 1:0.03 to 1:1, such as 1:0.3 to 1:0.7.