Methylxanthine-Stilbenoid Cocrystals for Bitterness Masking
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Solution Overview
Problem
Methylxanthines such as caffeine and theacrine have a bitter taste that limits their use in nutraceutical formulations due to poor palatability, which affects patient adherence.
Innovation Solution
The formation of cocrystals with stilbenoids like pterostilbene and resveratrol through co-crystallization, which masks the bitterness and improves taste.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If methylxanthines are used in nutraceutical formulations, then health benefits are provided, but bitter taste reduces patient adherence
Solution Approach 1:
The patent applies composite material formation by creating cocrystals that combine methylxanthine molecules with coformer molecules (such as amino acids or organic compounds). This composite crystalline structure masks the bitter taste of methylxanthines while preserving their therapeutic effects, thereby improving patient adherence without sacrificing the health benefits
Solution Approach 2:
The patent uses coformers as intermediary substances that interact with methylxanthines to form cocrystals. These coformers act as mediators that modify the sensory properties (taste) of methylxanthines without altering their pharmacological activity, thus resolving the contradiction between maintaining therapeutic effect and reducing bitter taste
2Object-affected harmful factors
If co-crystallization with stilbenoids is performed, then bitterness is masked and taste is improved, but formulation complexity increases
Solution Approach 1:
The patent employs parameter changes by modifying the physical and chemical parameters of methylxanthines through cocrystallization. By changing the crystalline lattice structure and molecular arrangement through controlled co-crystallization with stilbenoids, the bitter taste is masked while the process remains relatively simple and scalable for pharmaceutical manufacturing
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 cocrystals exhibit a pleasant taste and improved bioavailability, making them suitable for nutraceutical and pharmaceutical compositions.
Implementation Method 1
The debittering of Methylxanthines is carried out by co-crystallization using Stilbenoids as coformers
Data Source
AI summary
The present invention relates to cocrystals of Methylxanthines with Stilbenoids as coformers, their polymorphic forms and to the process for preparation thereof. The debittering of Methylxanthines is carried out by co-crystallization using Stilbenoids as coformers. The invention further relates to the preparation of polymorphic forms of debittered cocrystals and their use in nutraceutical and pharmaceutical compositions.