Microcapsule Compression Stability via Deformable Overcoating
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Solution Overview
Problem
Existing orally dispersible tablets with prolonged release microcapsules face challenges in maintaining the stability of the release profile and mechanical properties during compression, leading to degradation and reduced active ingredient content, especially when administering high doses.
Innovation Solution
The development of microcapsules with a non-deformable core coated with a deformable organic overcoating layer, which provides mechanical strength during compression without affecting the prolonged release properties, allowing for high doses of active principles in a convenient and easily swallowable tablet form.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Duration of action of moving object
If microcapsules with prolonged release coating are compressed to form tablets, then the active principle is released in a controlled manner over time, but the coating degrades under mechanical stress leading to loss of prolonged release properties
Solution Approach 1:
The microcapsule structure is segmented into three distinct layers: a hard core containing the active principle, an intermediate prolonged release coating layer, and an outer protective overcoating layer. This segmentation allows each layer to perform its specific function independently, with the outer layer protecting the inner prolonged release coating during compression.
Solution Approach 2:
The outer overcoating layer acts as a protective cushion applied beforehand to shield the prolonged release coating from mechanical stresses during tablet compression. This pre-protective layer prevents degradation of the functional coating while allowing the tablet to be formed.
2Quantity of substance
If high doses of active principle are administered in tablet form, then therapeutic efficacy is improved, but tablet size increases making it difficult to swallow
Solution Approach 1:
The microcapsules utilize thin film coatings that provide prolonged release functionality without adding significant bulk. The flexible yet protective overcoating allows high loading of active principle in the core while maintaining a compact overall structure that is easy to swallow.
Solution Approach 2:
The structure employs a nested configuration where the active principle core is enclosed within the prolonged release coating, which is in turn enclosed within the outer protective overcoating. This nested arrangement maximizes the active principle content within a small, swallowable form factor.
3Strength
If the coating is made mechanically strong to withstand compression, then tablet formation is improved, but the prolonged release function is compromised
Solution Approach 1:
Different regions of the microcapsule are assigned different mechanical and functional properties: the outer overcoating layer has high mechanical strength for compression resistance, while the inner prolonged release coating maintains its original composition and properties for controlled release functionality. This local differentiation resolves the contradiction between strength and function.
Solution Approach 2:
The outer overcoating layer serves as an intermediary between the compression force and the prolonged release coating. It absorbs and distributes mechanical stresses, preventing direct transmission of compressive forces to the functional coating, thereby preserving both tabletability and prolonged release properties.
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 solution maintains the stability of the release profile and mechanical properties of the microcapsules after compression, enabling the administration of high doses of active principles in a stable and effective manner, facilitating patient compliance and treatment success.
Implementation Method 1
each comprising at least one outer overcoating envelope based on at least one deformable organic constituent having a melting point of between 40° C. and 120° C.
Data Source
AI summary
A multi(micro)particulate tablet is provided comprising microparticles which comprise a mechanically non-deformable core of active principle (AP). The tablet is formed from reservoir microcapsules with prolonged release of the AP, which are each made up of a non-deformable core comprising AP and covered with at least one film coating controlling release of the AP in vivo. The microcapsules have a particle size of between 50 and 1000 microns and are coated with at least one outer overcoating envelope comprising at least one deformable organic constituent having a melting point of between 40° C. and 120° C. The envelope allows the prolonged release of the AP in vivo without modification of the release profile when the microcapsules are compressed to form a tablet, even for microparticles not specifically formulated for compression.