Sublingual Fentanyl Tablet with Drug-Free Core
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Solution Overview
Problem
Sublingual tablets with active substances uniformly dispersed in the mass face challenges such as dependency on tablet size for dosage, risk of segregation, low hardness leading to rapid disintegration, and incomplete absorption due to swallowing reflex, especially for low-dose fentanyl which is highly diluted and difficult to uniformly distribute.
Innovation Solution
A sublingual coated tablet design featuring a compressed core devoid of active substance with a coating containing fentanyl, allowing independent dosage regulation through coating thickness, independent of tablet size and disintegration rate, ensuring complete absorption before swallowing.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Quantity of substance
If active substance is uniformly dispersed in the tablet mass, then dosage can be adjusted by tablet size, but manufacturing precision deteriorates due to segregation risk and difficulty in uniform distribution
Solution Approach 1:
The tablet is segmented into two distinct parts: a compressed core containing excipients and a coating layer containing the active substance. This segmentation eliminates the need to uniformly disperse the active substance throughout the entire tablet mass, thereby avoiding segregation issues while maintaining dosage control through coating thickness adjustment.
Solution Approach 2:
The active substance is relocated from the three-dimensional bulk of the tablet to a two-dimensional surface layer (coating). This dimensional change allows dosage to be controlled by the thickness and surface area of the coating rather than by dispersing the substance throughout the tablet volume, significantly improving manufacturing precision and uniformity.
2Adaptability or versatility
If active substance is uniformly dispersed in the tablet mass, then dosage can be varied, but device complexity increases due to need for different tablet sizes for different dosages
Solution Approach 1:
A single compressed core design serves as the base for multiple dosages, with the coating layer providing the variable dosage component. This allows one core formulation to be used universally across different dosage strengths by simply adjusting the coating thickness or active substance content in the coating, eliminating the need to develop different core formulations for each dosage.
Solution Approach 2:
Instead of changing the physical dimensions (size) of the tablet to vary dosage, the invention changes the parameter of coating thickness or coating composition. This allows dosage variation while maintaining a constant core size and shape, simplifying the overall device design and manufacturing process.
3Speed
If tablet has low hardness to disintegrate rapidly, then absorption speed improves, but reliability deteriorates due to incomplete absorption from swallowing reflex
Solution Approach 1:
The tablet exhibits different properties in different locations: the compressed core maintains structural integrity and resists disintegration, while the coating layer is designed to dissolve rapidly. This local quality differentiation ensures that the active substance in the coating is released quickly for rapid absorption, while the core provides mechanical stability to prevent premature disintegration and ensure complete absorption before swallowing.
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
This design ensures uniform and complete absorption of fentanyl, independent of tablet size and disintegration rate, improving bioavailability and eliminating the need for varying tablet sizes, while maintaining rapid release and absorption.
Implementation Method 1
the layer forming the coating and comprising the pharmaceutically active substance is completely solubilized in the fluids of the buccal cavity, in particular in the saliva
Implementation Method 2
systemic passage is very rapid due to the considerable permeability and vascularization of the buccal mucosa
Data Source
AI summary
The present invention relates to a fentanyl coated tablet and to the method for the preparation thereof.