Porous Silica Particle Composition for Pharmaceutical Tablet Compression

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Solution Overview

Problem

Porous silica particle compositions used in pharmaceutical and cosmetic applications face limitations in compression moldability, flowability, and oil absorption capacity, which affect their suitability for various formulations and bitterness masking of bitter drugs.

Innovation Solution

A porous silica particle composition with specific properties, including a BET specific surface area of 250-1000 m2/g, average particle diameter of 1-150 μm, pore volume of 0.1-8.0 cm3/g, and oil absorption capacity of 2.2-5.0 mL/g, is developed to enhance compression moldability, flowability, and bitterness masking.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Stability of the object's composition

If porous silica particle composition is used as an adsorption carrier in tablets, then drug stability is improved due to neutrality, but compression moldability deteriorates due to excessively high specific volume

Engineering Contradiction:
Improvedrug stabilityVSAvoidcompression moldability
Core Design Contradiction:
Stability of the object's compositionVSEase of manufacture

Solution Approach 1:

The patent applies parameter changes by precisely controlling the pore volume (0.1-8.0 cm³/g) and specific surface area (250-1000 m²/g) of the porous silica particles. By optimizing these parameters within specific ranges, the invention achieves a balance between maintaining high drug stability through porosity while reducing excessive specific volume to improve compression moldability for tablet fabrication.

Inventive Principle:
Principle #35Parameter changes

2Quantity of substance

If porous silica particle composition is added to tablet, then adsorption capacity is improved, but flowability deteriorates

Engineering Contradiction:
Improveadsorption capacityVSAvoidflowability
Core Design Contradiction:
Quantity of substanceVSEase of operation

Solution Approach 1:

The invention uses parameter changes by controlling particle size distribution (D10, D50, D90 values) and surface properties of the porous silica. By adjusting these parameters, the patent achieves improved adsorption capacity while maintaining adequate flowability for pharmaceutical processing operations.

Inventive Principle:
Principle #35Parameter changes

3Adaptability or versatility

If conventional silica is used, then availability is improved, but oil absorption capacity deteriorates

Engineering Contradiction:
Improveapplicability to formulationsVSAvoidoil absorption capacity
Core Design Contradiction:
Adaptability or versatilityVSQuantity of substance

Solution Approach 1:

The patent applies porous materials principle by utilizing silica particles with controlled pore structures (pore volume 0.1-8.0 cm³/g). This porous structure provides enhanced oil absorption capacity compared to conventional non-porous silica, while maintaining broad applicability to various pharmaceutical and cosmetic formulations through neutral chemical properties.

Inventive Principle:
Principle #31Porous 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 composition improves disintegration of tablets, enhances oil absorption, and effectively masks the bitterness of drugs, providing improved performance in pharmaceutical and cosmetic applications.

Implementation Method 1

porous silica particle composition which is excellent in oil absorption capacity

Methodology Applied
Scientific EffectAdsorption: Adsorption

Implementation Method 2

pore volume from 0.1 to 8.0 cm3/g

Methodology Applied
Scientific EffectCapillary action: Capillary Action

Data Source

PatentUS12116285B2Porous silica particle composition
Publication Date: 2024.10.15 FUJI CHEM IND CO LTD
  • US12116285B2 patent drawing
  • US12116285B2 patent drawing
  • US12116285B2 patent drawing

AI summary

A silica that is superior in terms of fluidity, oil absorption ability, and compression moldability to conventional silica used as a pharmaceutical additive, and is suitable as an additive for formulations such as pharmaceuticals. A porous silica particle composition having the following properties: (1) a BET specific surface area from 250 to 1,000 m2/g; (2) an average particle diameter from 1 to 150 μm; (3) a pore volume from 0.1 to 8.0 cm3/g; and (4) an oil absorption capacity from 2.2 to 5.0 mL/g.