T2R Receptor Blocking Compounds for Bitter API Oral Formulations
Find Innovative SolutionsGenerate Solutions
Solution Overview
Problem
Many active pharmaceutical ingredients (APIs) impart a noticeable bitter taste, making oral administration difficult or impossible, and existing encapsulation or coating methods are not effective for all APIs, adding unnecessary costs and complications.
Innovation Solution
Identify compounds that selectively block specific T2R taste receptors responsible for bitter taste perception by using polypeptide sequences of SEQ ID NO: 1-6 or their functional fragments, and measure their response to test compounds to determine bitterness reduction.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Object-affected harmful factors
If encapsulation or coating methods are used to reduce bitter taste, then the bitter taste of APIs is reduced, but manufacturing complexity and costs increase
Solution Approach 1:
The patent extracts and identifies specific T2R receptors (SEQ ID NO: 1-6) that are principally responsible for bitter taste perception of APIs. By focusing on these specific receptors rather than attempting to block all bitter taste pathways, the solution simplifies the approach to reducing bitter taste while avoiding complex encapsulation or coating methods.
Solution Approach 2:
The patent introduces bitter blocking compounds as intermediary substances that selectively bind to and block the identified T2R receptors. These compounds act as mediators between the API and the taste receptors, preventing the bitter taste signal from being transmitted while allowing the API to remain in a simple oral formulation without complex encapsulation.
2Object-affected harmful factors
If encapsulation or coating methods are used to reduce bitter taste, then the bitter taste of APIs is reduced, but manufacturing costs increase
Solution Approach 1:
The patent extracts and identifies specific T2R receptors (SEQ ID NO: 1-6) that are principally responsible for bitter taste perception of APIs. By focusing on these specific receptors rather than attempting to block all bitter taste pathways, the solution simplifies the approach to reducing bitter taste while avoiding complex encapsulation or coating methods.
Solution Approach 2:
The patent introduces bitter blocking compounds as intermediary substances that selectively bind to and block the identified T2R receptors. These compounds act as mediators between the API and the taste receptors, preventing the bitter taste signal from being transmitted while allowing the API to remain in a simple oral formulation without complex encapsulation.
3Object-affected harmful factors
If all 25 T2R bitter taste receptors are blocked to eliminate bitter taste, then bitter taste is completely blocked, but the complexity of blocking increases significantly
Solution Approach 1:
The patent extracts and identifies specific T2R receptors (SEQ ID NO: 1-6) that are principally responsible for bitter taste perception of APIs. By focusing on these specific receptors rather than attempting to block all bitter taste pathways, the solution simplifies the approach to reducing bitter taste while avoiding complex encapsulation or coating methods.
Solution Approach 2:
The patent applies local quality by targeting specific T2R receptors (SEQ ID NO: 1-6) that are principally responsible for bitter taste perception of APIs, rather than attempting to uniformly block all 25 T2R receptors. This localized approach to receptor blocking reduces complexity while maintaining effectiveness.
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 identified compounds effectively reduce the bitter taste of APIs by blocking relevant T2R receptors, enabling simpler and more cost-effective oral formulations.
Implementation Method 1
compounds that can selectively block one or more of these certain T2R receptors
Data Source
AI summary
The present disclosure generally provides methods for identifying compounds that attenuate the bitter taste of active pharmaceutical ingredients (APIs). In some aspects, the disclosure provides methods of identifying compounds that attenuate the bitter taste of APIs by determining whether the compounds modulate certain T2R bitter taste receptors. In some other aspects, the disclosure provides uses of such identified compounds to attenuate the bitter taste of an ingestible composition that comprises one or more APIs, such as liquid or solid dosage forms for oral administration. In some further aspects, the disclosure provides flavored products, such as pharmaceutical products, that incorporate such ingestible compositions.