Niclosamide Delayed-Release Composition for Antiviral Use
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Solution Overview
Problem
Conventional niclosamide formulations have low water solubility and intestinal permeability, leading to rapid clearance and low bioavailability, making it difficult to achieve and maintain effective blood drug concentrations for antiviral activity against coronavirus infections.
Innovation Solution
A delayed-release composition of niclosamide or its pharmaceutically acceptable salt, combined with an anionic polysaccharide cellulose derivative such as carboxymethyl cellulose, and optionally phosphate salts and mannitol, to enhance solubility and bioavailability, allowing for prolonged effective blood drug concentrations.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If conventional niclosamide formulations are used, then the drug can be administered orally, but water solubility and intestinal permeability are low, leading to rapid clearance and low bioavailability
Solution Approach 1:
The patent changes the physical and chemical parameters of niclosamide by formulating it as a delayed-release composition. This modifies the drug's release characteristics, improving water solubility and intestinal permeability while extending blood drug concentration maintenance from rapid clearance to sustained release over time.
Solution Approach 2:
The patent creates a composite pharmaceutical formulation combining niclosamide with delayed-release technology. This composite structure allows the drug to be protected until the appropriate release site, thereby improving bioavailability and extending duration of action simultaneously.
2Reliability
If conventional niclosamide formulations are used, then the formulation is simple, but it is impossible to achieve and maintain effective blood drug concentrations for antiviral activity
Solution Approach 1:
By modifying the formulation parameters to include delayed-release technology, the patent achieves effective blood drug concentrations necessary for antiviral activity. The increased formulation complexity is justified by the critical need to maintain therapeutic drug levels.
3Reliability
If conventional niclosamide formulations are used, then manufacturing is straightforward, but clearance is extremely fast and bioavailability is low
Solution Approach 1:
The patent modifies formulation parameters to create a delayed-release composition that addresses rapid clearance and low bioavailability. While manufacturing becomes more complex, the improvement in bioavailability is the priority outcome.
Data Source
AI summary
The present invention relates to a pharmaceutical composition for prevention or treatment of coronavirus infections, comprising a delayed-release composition of niclosamide or a pharmaceutically acceptable salt thereof, and a method for preventing or treating coronavirus infections by using the same.