SGLT2 Inhibitor and Menthol Combination for Heart Failure
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Solution Overview
Problem
Current treatments for heart failure, such as ACEI/ARB and β-receptor blockers, have limitations in reducing adverse reactions and do not significantly improve patient quality of life, and there is a need for more effective combination drugs targeting multiple pathways.
Innovation Solution
A pharmaceutical composition combining an SGLT2 inhibitor, such as empagliflozin, with menthol, particularly L-menthol, to synergistically inhibit calcium influx and promote fatty acid metabolism, thereby treating heart diseases like heart failure.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If traditional heart failure treatments (ACEI/ARB, β-receptor blockers) are used, then cardiac function can be maintained to some extent, but adverse reactions increase and quality of life does not significantly improve
Solution Approach 1:
The patent combines empagliflozin (SGLT2 inhibitor) and menthol into a single pharmaceutical composition. This merging of two active ingredients with different mechanisms of action allows simultaneous targeting of multiple pathways involved in heart failure, thereby maintaining cardiac function while potentially reducing adverse reactions associated with conventional monotherapies
Solution Approach 2:
The invention creates a composite pharmaceutical formulation containing empagliflozin and menthol in specific ratios. This composite approach leverages the synergistic effects of both compounds - empagliflozin for its proven cardioprotective effects and menthol for its potential to enhance efficacy and reduce side effects, resulting in a therapy that maintains reliability while minimizing harmful factors
2Reliability
If current combination drugs for heart failure are used, then some therapeutic benefits are achieved, but the number of available options is limited (only four combination drugs) and does not meet clinical needs
Solution Approach 1:
The patent introduces a new combination of empagliflozin and menthol, expanding the existing portfolio of heart failure combination therapies. This merging creates a novel therapeutic option that targets different mechanisms compared to existing four combination drugs, thereby increasing adaptability and versatility in clinical treatment options while maintaining therapeutic efficacy
3Reliability
If higher doses of empagliflozin are used to improve therapeutic effect, then cardiac function improves, but adverse reactions increase
Solution Approach 1:
Menthol acts as an intermediary compound that enhances the therapeutic effects of empagliflozin. By including menthol in the formulation, the patent enables lower doses of empagliflozin to achieve the same or better cardiac function improvement, thereby reducing adverse reactions while maintaining or enhancing therapeutic efficacy
Solution Approach 2:
The patent changes the dosing parameters by introducing menthol, which allows optimization of empagliflozin dosage. The specific ratio of empagliflozin to menthol (1:1 to 1:10 by weight) represents a parameter change that enables achieving therapeutic goals at lower empagliflozin doses, thus improving cardiac function while minimizing adverse reactions
Data Source
Figure 1A~1B
Figure 1C~1E
Figure 2A
AI summary
Disclosed in the present invention are a pharmaceutical composition of an SGLT2 inhibitor and menthol and a use thereof in the preparation of drugs for preventing, ameliorating, and/or treating heart diseases. The pharmaceutical composition involved in the present invention has a myocardial cell protection effect, synergistically reduces intracellular calcium ion concentration, synergistically promotes fatty acid metabolism, has advantages compared with a single medication, and can be used for preparing medicines for treating, ameliorating, and/or preventing heart failure, coronary heart disease, myocardial infarction, hypertension heart disease, etc.