Polyphenol-Citrate Composition for Inhibiting COM Crystal Growth
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Solution Overview
Problem
Current treatments for kidney stones, particularly those focusing on calcium oxalate monohydrate (COM) crystals, have limited efficacy in inhibiting crystal growth and preventing stone formation, necessitating the development of synergistic drug combinations to enhance treatment and prevention effects.
Innovation Solution
A pharmaceutical composition comprising polyphenols with 6 to 14 carbon atoms and citric acid or its derivatives, administered alone or in combination, to inhibit COM crystal growth through mechanisms like step pinning and kink blocking, achieving a synergistic effect that surpasses individual inhibitor performance.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If single inhibitors (metal ions, small organic molecules, or macromolecules) are used to inhibit COM crystal growth, then some inhibition effect is achieved (30-60%), but complete inhibition of COM crystal growth and stone formation cannot be achieved
Solution Approach 1:
The patent combines multiple inhibitors with different mechanisms of action into a single pharmaceutical composition. Specifically, it integrates metal ions (such as Mg2+, Ca2+), small organic molecules (such as citric acid and its derivatives), and macromolecules (such as urine proteins like osteopontin and chondroitin sulfate) to achieve synergistic inhibition of COM crystal growth, overcoming the limitation of single inhibitors that can only achieve 30-60% inhibition.
Solution Approach 2:
The invention creates a composite inhibitor system comprising multiple types of substances with different chemical properties and mechanisms. The composition includes inorganic components (metal ions), organic components (small molecules and macromolecules), which work together to provide comprehensive inhibition of calcium oxalate crystallization, thereby improving both reliability and productivity in stone prevention.
2Reliability
If combined administration of drugs is used to achieve synergistic effect, then disease treatment effect is enhanced, but drug interactions may produce opposite results
Solution Approach 1:
The pharmaceutical composition is designed to perform multiple functions simultaneously: reducing supersaturation of calcium oxalate, inhibiting nucleation of solute, blocking crystal growth, and preventing crystal aggregation. By integrating multiple inhibitors with complementary mechanisms into a single formulation, the composition achieves comprehensive stone prevention without requiring separate administration of multiple drugs, thus reducing complexity while maintaining synergistic effects.
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 combined pharmaceutical composition significantly enhances the inhibition of COM crystal growth, reducing stone formation and recurrence by leveraging synergistic mechanisms between polyphenols and citric acid, even at reduced doses.
Implementation Method 1
inhibit COM crystal growth through mechanisms like step pinning and kink blocking
Implementation Method 2
inhibit COM crystal growth through mechanisms like step pinning and kink blocking
Implementation Method 3
a substance that is metabolizable into polyphenol having 6 to 14 carbon atoms in human body
Data Source
AI summary
Provided are a pharmaceutical composition and use thereof. The pharmaceutical composition includes a component A and a component B. The component A includes polyphenol having 6 to 14 carbon atoms and/or a substance that is metabolizable into polyphenol having 6 to 14 carbon atoms in the human body. The component B includes any one of citric acid, citrate, a citric acid derivative, or a citric acid derivative salt, or a combination of at least two thereof. The pharmaceutical composition not only has a synergistic enhancement effect in inhibiting the growth of calcium oxalate crystals, but also can be used for a synergistic treatment of kidney stones.