Fast-Disintegrating Tablet With Liquid Crystal Controlled Release
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Solution Overview
Problem
Current orally disintegrating tablets (ODTs) face limitations in delivering active ingredients with rapid absorption, leading to potential side effects and unsuitability for drugs requiring slow release or lipophilic drugs, while also having limited utility for drugs with low bioavailability through the digestive tract.
Innovation Solution
Development of an ODT that contains an amphiphilic compound capable of forming liquid crystalline particles upon contact with a hydrophilic fluid, allowing for rapid disintegration and controlled release of active ingredients, facilitating systemic administration via the oral mucosa.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Speed
If an ODT is designed for rapid disintegration and absorption, then the onset of action is fast, but the blood concentration rises too fast or too far causing side effects and/or resulting in a short therapeutic effect
Solution Approach 1:
The tablet is designed to segment into multiple smaller particles upon disintegration, increasing the surface area for absorption while controlling the release rate. This segmentation allows rapid disintegration (improving speed) while the controlled particle distribution prevents excessive blood concentration rise (reducing side effects).
Solution Approach 2:
The formulation uses specific disintegrants and binding agents in optimized proportions to control the disintegration kinetics. By adjusting parameters such as disintegrant type, amount, and interaction with the active ingredient, the system achieves rapid tablet breakdown while modulating the release rate to prevent harmful side effects.
2Speed
If an ODT is designed for rapid absorption, then the onset of action is fast, but the therapeutic effect duration is short
Solution Approach 1:
The tablet formulation incorporates sustained-release matrix materials and controlled-disintegration agents that prepare the active ingredient for gradual release. This preliminary structuring ensures that while the tablet disintegrates rapidly, the active ingredient is released in a controlled manner over an extended period, prolonging therapeutic effect.
Solution Approach 2:
The formulation design ensures continuous release of the active ingredient through the use of matrix materials and disintegrant systems that maintain controlled release kinetics. This continuity of useful action extends the therapeutic effect duration while maintaining acceptable absorption rates.
3Speed
If a traditional ODT is used, then rapid action is achieved, but it is not suitable for lipophilic drugs which have difficulty absorbing across the membrane
Solution Approach 1:
The formulation incorporates lipophilic excipients and surfactants that act as intermediaries between the lipophilic active ingredient and the aqueous oral mucosa environment. These intermediaries facilitate the absorption of lipophilic drugs across the membrane while maintaining the rapid action characteristics of ODTs.
Solution Approach 2:
The tablet uses composite formulation materials including lipophilic polymers, surfactants, and disintegrants in specific combinations. This composite approach creates a formulation that is both rapidly disintegrating and suitable for lipophilic drugs, expanding the adaptability of the ODT dosage form.
4Duration of action of moving object
If an ODT is designed to sit in the mouth for an extended period, then absorption time is increased, but patient convenience is reduced and rapid disintegration is compromised
Solution Approach 1:
The tablet formulation exhibits dynamic disintegration behavior, initially disintegrating rapidly to provide immediate patient convenience and then transitioning to a controlled release phase that extends absorption time. This dynamic behavior balances patient convenience with extended absorption duration.
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 ODT achieves fast disintegration without interfering with the formation of liquid crystalline particles, enabling prolonged release of active ingredients, enhancing bioavailability and suitability for a wider range of drugs, including lipophilic ones, while maintaining patient convenience.
Implementation Method 1
an amphiphilic compound capable of self-assembling into liquid crystalline particles when contacted with a hydrophilic solvent
Implementation Method 2
amphiphilic compound capable of self-assembling into liquid crystalline particles
Implementation Method 3
a pharmaceutically acceptable disintegrant, wherein the disintegrant is about 1 to about 60% w/w of the tablet and the oral disintegrating tablet disintegrates in less than 2 minutes
Data Source
AI summary
An oral disintegrating tablet that forms liquid crystalline particles or liquid crystalline bulk phase upon disintegration. The oral disintegrating tablet is fast disintegrating following contact with saliva and/or the oral mucosa but also provides slowed delivery of the active ingredient to avoid the difficulties associated with the speed of delivery of an active ingredient through the oral mucosa.