Disintegrating Loadable Tablets via Porous Sorbent Granules

Resolve Bottlenecks,
Find Innovative Solutions
Generate Solutions

Solution Overview

Problem

Current pharmaceutical technologies face challenges in delivering poorly water-soluble drugs with enhanced bioavailability and controlled release, as existing methods often require complex processes and struggle to maintain porosity and loading capacity in compressed tablets.

Innovation Solution

Development of a disintegrating loadable tablet comprising at least 60% sorbent material with high specific surface area and a disintegrant, achieving a porosity of 45% or more, hardness of 20 Newton or more, and a loading capacity of 30% or more for a pharmaceutically acceptable liquid formulation, allowing for rapid and complete release of active substances.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Ease of manufacture

If wet granulation is used to prepare granules, then the active substance can be incorporated into a pressed form, but the porosity and loading capacity are reduced

Engineering Contradiction:
Improvetablet formationVSAvoidporosity
Core Design Contradiction:
Ease of manufactureVSVolume of stationary object

Solution Approach 1:

The patent employs porous granules with controlled pore structures that maintain high porosity (40-60%) after compression. The porous nature allows these granules to absorb liquid formulations containing active substances, achieving both manufacturability and high loading capacity without requiring wet granulation processes.

Inventive Principle:
Principle #31Porous materials

Solution Approach 2:

The invention uses composite granule structures combining hydrophilic and hydrophobic materials to create a matrix that maintains structural integrity during compression while providing sufficient porosity for liquid absorption. This composite approach enables simultaneous achievement of tablet hardness and high porosity.

Inventive Principle:
Principle #40Composite materials

2Strength

If the tablet is compressed to increase hardness, then the mechanical strength is improved, but the porosity decreases

Engineering Contradiction:
ImprovehardnessVSAvoidporosity
Core Design Contradiction:
StrengthVSVolume of stationary object

Solution Approach 1:

The patent utilizes inherently porous granule materials that maintain their pore structure even under compression forces. The granules are designed with rigid porous frameworks that resist collapse, allowing the compressed tablet to retain sufficient porosity for liquid formulation absorption while achieving the required hardness.

Inventive Principle:
Principle #31Porous materials

Solution Approach 2:

The invention optimizes compression parameters such as pressure, duration, and granule size distribution to achieve the desired balance between hardness and porosity. By carefully controlling these parameters, the tablet maintains sufficient mechanical strength while preserving the porous structure necessary for high loading capacity.

Inventive Principle:
Principle #35Parameter changes

3Quantity of substance

If a high amount of liquid formulation is loaded into the tablet, then the bioavailability of poorly water-soluble drugs is enhanced, but the tablet stability is compromised

Engineering Contradiction:
Improveloading capacityVSAvoidtablet stability
Core Design Contradiction:
Quantity of substanceVSStability of the object's composition

Solution Approach 1:

The patent employs porous granules with controlled pore sizes and distributions that can accommodate and retain high amounts of liquid formulation (up to 50-70% w/w) while maintaining structural integrity. The porous structure provides sufficient capacity for liquid loading without causing tablet disintegration or excessive softening.

Inventive Principle:
Principle #31Porous materials

Solution Approach 2:

The invention uses composite granule compositions combining materials with different affinities for liquid formulations. This composite structure allows high liquid loading capacity while the hydrophobic components prevent excessive water uptake that would compromise tablet stability. The balanced composition maintains both loading capacity and stability.

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 tablets effectively sorb and release a substantial amount of liquid formulation, maintaining stability and bioavailability, and can be designed for immediate or modified release, addressing the limitations of existing technologies in handling poorly soluble drugs.

Implementation Method 1

the tablet will due to its porosity - suck the liquid formulation into the tablet

Methodology Applied
Scientific EffectCapillary action: Capillary Action

Implementation Method 2

at least 60% w/w of a sorbent material having a specific surface area (BET surface area) of at least 50 m2/g

Methodology Applied
Scientific EffectAdsorption: Adsorption

Implementation Method 3

incorporation of disintegrating excipients in order to influence the accessibility of the active substance

Methodology Applied
Scientific EffectSwelling:

Implementation Method 4

a disintegrating loadable tablet comprising at least 60% sorbent material with high specific surface area and a disintegrant

Methodology Applied
Scientific EffectDisintegration:

Data Source

PatentEP1973529B1Disintegrating loadable tablets
Publication Date: 2011.05.25 VELOXIS PHARMA AS
  • EP1973529B1 patent drawingFigure 1A
  • EP1973529B1 patent drawingFigure 1B
  • EP1973529B1 patent drawingFigure 2

AI summary

A disintegrating loadable tablet product in compressed form comprising i) at least 60% w/w of a sorbent material having a specific surface area (BET surface area) of at least 50 m2/g as measured by gas adsorption or mixtures of such sorbent materials, and ii) a disintegrant or a mixture of disintegrants wherein the tablet in compressed form has a) a porosity of 45% v/v or more, b) a hardness of at least 20 Newton, and c) a loading capacity of at least 30% of a liquid. The tablet is suitable for the preparation of a tablet containing an active substance by e.g. immersing the tablet in a liquid containing the active substance. The invention thus provides a safe and reproducible new method of preparing pharmaceutical tablets.