LCST Polymer Binder for Fast Onset Orodispersable Tablets
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Solution Overview
Problem
Conventional pharmaceutical tablets require fluid for administration, which can be inconvenient for pediatric, geriatric, or schizophrenic patients, and existing fast disintegrating tablets face challenges in balancing friability and rapid disintegration for effective bioavailability and onset.
Innovation Solution
The development of orodispersable tablets using specific combinations of binders, such as polymers with lower critical solution temperatures, and modifiers that reduce the critical solution temperature to body temperature or lower, allowing for rapid disintegration and increased bioavailability without compromising mechanical strength.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Speed
If conventional tablets are used, then mechanical strength is maintained, but rapid disintegration and fast onset cannot be achieved
Solution Approach 1:
The patent changes the physical-chemical parameters of the binder by selecting polymers with specific lower critical solution temperatures (LCST) between 40-100°C. These polymers remain solid and provide mechanical strength at room temperature but melt at body temperature, enabling rapid disintegration. This parameter change resolves the contradiction between maintaining tablet hardness and achieving fast disintegration.
Solution Approach 2:
The patent uses composite formulations combining LCST polymers with modifiers (electrolytes, polyols, or sugars) to create a binder system that exhibits both mechanical strength at ambient temperature and rapid dissolution at body temperature. The composite nature of the binder allows simultaneous achievement of hardness and fast onset.
2Loss of time
If fast disintegrating formulations are used, then onset time is reduced, but tablet friability increases
Solution Approach 1:
The patent utilizes the temperature-dependent phase transition parameter of LCST polymers to achieve low friability during handling (solid state at room temperature) while enabling rapid disintegration (melt state at body temperature). This parameter change allows the tablet to be mechanically robust during manufacturing and storage but rapidly disintegrate upon administration.
3Ease of operation
If conventional tablets requiring fluid administration are used, then manufacturing simplicity is maintained, but ease of operation deteriorates
Solution Approach 1:
The patent changes the formulation to use LCST polymers that undergo phase transition at body temperature, eliminating the need for external fluid administration. The tablet disintegrates rapidly in the buccal cavity due to the temperature difference between ambient storage conditions and body temperature, simplifying administration for pediatric, geriatric, and schizophrenic patients.
4Reliability
If rapid disintegration is achieved, then bioavailability is enhanced, but mechanical handling difficulty increases
Solution Approach 1:
The patent employs LCST polymers that maintain a solid, handleable state at room temperature (providing low friability and good mechanical strength) but transition to a liquid or soft gel state at body temperature (enabling rapid disintegration and enhanced bioavailability). This temperature-dependent parameter change resolves the contradiction between handling ease and bioavailability enhancement.
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 tablets disintegrate within 60 seconds or less, maintaining low friability and enhancing bioavailability by reducing first-pass metabolism and accelerating the time to maximal effect of the active agent.
Implementation Method 1
The binder can comprise a polymer, such as a polymer having a relatively low critical solution temperature, e.g., a lower critical solution temperature (LCST). The LCST of the polymer can be, for example, less than about 100° C. The LCST of the polymer can be greater than about 40° C.
Implementation Method 2
The modifier can be any suitable entity or composition capable of reducing the critical solution temperature of a polymer, e.g., to about body temperature or lower. For example, the modifier can reduce the critical solution temperature of a polymer to less than 40° C., and preferably less than or about 37° C.
Data Source
AI summary
The present invention provides orodispersable tablets and methods of using the same. The tablets and methods are useful, for example, for reducing first pass metabolism of orally administered active agents, enhancing bioavailability of active agents, and/or reducing the time it takes for an active agent to achieve maximal effect in a subject. The tablets, when taken orally, disintegrate or dissolve rapidly such that active agent included in the tablets is absorbed in the buccal cavity. The invention further provides methods of manufacturing any of the tablets disclosed herein and containers that include any of the tablets disclosed herein.