Xanthine Oxidase Inhibitor Formulations for Improved Solubility
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Solution Overview
Problem
Existing xanthine oxidase inhibitors, such as allopurinol and oxypurinol, are poorly soluble and poorly bioavailable, leading to issues like nausea, gastrointestinal discomfort, and poor absorption, making them ineffective in treating conditions associated with hyperuricemia.
Innovation Solution
Formulations incorporating organic bases, particularly basic amino acids and dipeptides, enhance the solubility and bioavailability of xanthine oxidase inhibitors, forming liquid compositions that improve dissolution and absorption.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Ease of manufacture
If xanthine oxidase inhibitors are formulated in traditional tablet form, then they are easy to manufacture and administer, but they exhibit poor solubility and poor bioavailability
Solution Approach 1:
The patent changes the chemical form of the xanthine oxidase inhibitor by converting it into a salt form (e.g., oxypurinol sodium salt) or complex form, which fundamentally alters its solubility parameters while maintaining its pharmacological activity. This parameter change enables the drug to achieve both manufacturability and improved bioavailability.
Solution Approach 2:
The patent creates composite formulations by combining the xanthine oxidase inhibitor with specific carriers, excipients, or solubilizing agents. These composite materials enhance the solubility and bioavailability of the active ingredient while maintaining the ease of manufacture through standardized formulation processes.
2Reliability
If xanthine oxidase inhibitors are used to treat hyperuricemia, then they reduce uric acid levels, but they cause gastrointestinal discomfort and nausea
Solution Approach 1:
The patent introduces intermediaries such as solubilizing agents, protective carriers, or pH-modifying excipients that mediate between the drug and the gastrointestinal tract. These intermediaries reduce direct irritation to the GI lining while ensuring the drug remains soluble and absorbable, thereby maintaining therapeutic efficacy while reducing side effects.
Solution Approach 2:
The patent converts potentially harmful properties of the xanthine oxidase inhibitor (such as its acidity or solubility characteristics that cause GI irritation) into beneficial features by forming salts or complexes that have reduced irritancy while maintaining or enhancing therapeutic effectiveness.
3Reliability
If organic bases are added to enhance solubility, then bioavailability increases, but formulation complexity increases
Solution Approach 1:
The patent systematically evaluates and optimizes parameters such as pH, ionic strength, and solvent composition to achieve enhanced solubility without requiring complex formulation strategies. By carefully controlling these parameters, the patent achieves improved bioavailability through relatively simple formulation approaches.
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 formulations increase solubility and bioavailability of xanthine oxidase inhibitors, reducing side effects and enhancing therapeutic efficacy by increasing nitric oxide availability and decreasing oxygen radical production, thus effectively treating conditions like gout and hypertension.
Implementation Method 1
organic base that enhances or effects solubilisation of the xanthine oxidase inhibitor
Implementation Method 2
increased dissolution rate and solubility of XOI
Data Source
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AI summary
Disclosed herein are methods and compositions for involving a xanthine oxidase inhibitor that has enhanced solubility. The compositions described herein include a xanthine oxidase inhibitor combined with an organic base. The compositions can be used to treat a disease or medical condition that involves elevated uric acid levels.