Biphasic Core-Shell Tablet for Stable Once-Daily Drug Release
Find Innovative SolutionsGenerate Solutions
Solution Overview
Problem
Current dosage forms for hygroscopic and highly soluble active ingredients face challenges in providing stable, storable, and cost-effective formulations that allow for once-daily administration without the need for multiple daily doses, as they often suffer from rapid release and instability due to hygroscopicity and acidity, leading to ineffective plasma levels and side effects.
Innovation Solution
A shell-core tablet design with an enteric-resistant intermediate layer and a jacket, where the active ingredient is released in two phases: an immediate release in the stomach and a delayed release in the small intestine, optimizing the absorption and extending the therapeutic effect beyond 10 hours.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Duration of action of moving object
If a single dosage form contains high amounts of highly soluble active ingredient, then once-daily administration is achieved, but the active ingredient releases too rapidly and cannot maintain therapeutic plasma levels
Solution Approach 1:
The dosage form is divided into three distinct layers: a first layer containing the active ingredient for rapid release to achieve quick therapeutic effect, a second layer providing delayed release to maintain plasma levels, and a third layer protecting from moisture. This segmentation allows different release profiles from different layers, solving the contradiction between rapid initial release and sustained maintenance of therapeutic levels.
2Stability of the object's composition
If the dosage form is protected from moisture to prevent hygroscopic damage, then storage stability is improved, but the structure becomes more complex and costly
Solution Approach 1:
The protective function is localized to only the third layer of the dosage form, which is dedicated to moisture protection. This allows the first two layers to focus on drug release functions without moisture protection complexity, achieving stability while maintaining relative structural simplicity through functional specialization.
3Ease of operation
If the dosage form size is reduced for easy swallowing, then patient compliance improves, but the amount of active ingredient that can be contained is limited
Solution Approach 1:
The dosage form uses a composite layered structure where each layer serves a specific function. This allows efficient packing of high amounts of active ingredient in the first two layers while keeping the overall size manageable for swallowing. The third protective layer adds minimal size while providing crucial moisture protection.
4Duration of action of moving object
If matrix embedding is used to delay release, then extended duration is achieved, but it is ineffective for highly soluble active ingredients that dissolve too quickly
Solution Approach 1:
Instead of relying on a single matrix mechanism that fails for highly soluble ingredients, the invention segments the release function across two distinct layers: the first layer provides rapid release and the second layer provides delayed release. This segmentation allows each layer to be optimized for its specific release profile, achieving reliable extended duration control that works specifically for highly soluble active ingredients.
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 a stable and effective once-daily administration of hygroscopic and highly soluble active ingredients, reducing healthcare costs and improving patient compliance by mimicking multiple daily doses with a single tablet, while maintaining mechanical stability and storage integrity.
Implementation Method 1
an enteric-resistant intermediate layer which is arranged on the surface of the core
Implementation Method 2
Hygroscopic agents tend to absorb moisture from the environment, usually in the form of water vapor from the humidity
Implementation Method 3
such active ingredients can adsorb moisture from capsule shells, resulting in cracks in the capsule shell
Data Source
Figure 1
Figure 2
AI summary
This invention is concerned with the provision of medicament forms which enable effective administration of a medicament which is usually taken twice or more daily by way of a single daily dose. This is achieved in accordance with the invention by provision of a medicament form comprising a core, a gastric juice-resistant intermediate layer disposed on the surface of the core, and a shell disposed on the opposite side of the intermediate layer from the core. Both the core and the shell comprise a proportion of an active ingredient. The active ingredient is released in at least biphasic form from the medicament form, the first phase relating to the immediate release of the active ingredient after ingestion into the gastric juice. The present invention additionally relates to a process for producing the medicament form and to uses thereof.