Co-processed Carbohydrate Excipients for Tablet Strength and Disintegration

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Solution Overview

Problem

Existing excipients and excipient systems face challenges in producing tablets at low compression forces that are robust enough for high-speed tabletting machines, while maintaining rapid disintegration or dissolution properties, especially for high-dose active pharmaceutical ingredients (APIs) or APIs coated with polymers, waxes, and other coatings.

Innovation Solution

A highly compactable solid dispersion system comprising co-processed carbohydrates with different solubilities and concentrations, forming a microcrystalline plate structure, which allows for uniform densification, low friability, and constant disintegration times at various hardnesses, enabling direct compression into solid dosage forms with superior organoleptics and robustness.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Strength

If higher compression pressures are used to achieve robust tablets, then tablet strength and durability are improved, but disintegration time increases and porosity is lost

Engineering Contradiction:

Improvetablet strengthVSAvoiddisintegration time

Core Design Contradiction:

StrengthVSDuration of action of moving object

Solution Approach 1:

The patent changes the physical and chemical parameters of the excipient system by using co-processed carbohydrates with specific properties (different solubilities, microcrystalline plate structure) to achieve both high strength and rapid disintegration without requiring extreme compression pressures

Inventive Principle:

Principle #35Parameter changes

Solution Approach 2:

The patent employs composite excipient systems combining multiple carbohydrates (e.g., mannitol, sorbitol, maltitol) with complementary properties to achieve synergistic effects that simultaneously provide tablet robustness and rapid disintegration

Inventive Principle:

Principle #40Composite materials

2Strength

If higher compression pressures are used to achieve packagable tablets, then tablet robustness is improved, but coating integrity deteriorates due to rupturing

Engineering Contradiction:

Improvetablet robustnessVSAvoidcoating rupture

Core Design Contradiction:

StrengthVSObject-affected harmful factors

Solution Approach 1:

The patent modifies the compression pressure parameter by developing excipients that enable adequate tablet robustness at lower compression forces, thereby protecting coated APIs from coating rupture while maintaining tablet strength

Inventive Principle:

Principle #35Parameter changes

3Strength

If higher compression pressures are used to achieve durable tablets, then tablet durability is improved, but API surface area is reduced due to agglomeration

Engineering Contradiction:

Improvetablet durabilityVSAvoidAPI surface area

Core Design Contradiction:

StrengthVSArea of stationary object

Solution Approach 1:

The patent optimizes the compression pressure parameter by using highly compactable excipients that achieve durable tablets at lower pressures, preventing API particle agglomeration and preserving the surface area needed for rapid dissolution

Inventive Principle:

Principle #35Parameter changes

4Strength

If higher compression pressures are used to achieve robust tablets, then tablet integrity is improved, but disintegration performance deteriorates due to excipient behavior

Engineering Contradiction:

Improvetablet integrityVSAvoiddisintegration performance

Core Design Contradiction:

StrengthVSDuration of action of moving object

Solution Approach 1:

The patent uses composite excipient systems combining carbohydrates with different solubility characteristics to achieve both tablet integrity and rapid disintegration, where the less soluble carbohydrate provides structural strength and the more soluble carbohydrate facilitates rapid water penetration and disintegration

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 system enables the production of tablets with increased compactability, reduced friability, and consistent disintegration times, even at higher compression forces, without compromising the integrity of API coatings, thus facilitating efficient tablet production and delivery.

Implementation Method 1

co-processed carbohydrates which have different solubilities and/or concentrations, and microcrystalline plate structure

Methodology Applied

Scientific EffectCrystallization: Crystallisation

Data Source

PatentUS20230255891A1Highly Compactable and Durable Direct Compression Excipients and Excipient Systems

Publication Date: 2023.08.17 SPI PHARMACEUTICALS INC

AI summary

The present invention relates to solid dispersions including, but not limited to, co-processed carbohydrates with different solubilities and concentrations, which have a microcrystalline plate structure. The solid dispersions, excipient systems and formulations of the present invention are highly compactable and durable and when compressed into solid dosage forms demonstrate uniform densification, low friability at low pressures, and and/or relatively constant low disintegration times at various hardnesses. The solid dosage forms of the present invention demonstrate superior organoleptics, disintegration, and/or robustness.