Antiviral Salt Compounds for Solubility and Oral Bioavailability

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Solution Overview

Problem

Existing oral drug formulations face challenges with low aqueous solubility, instability, and low permeability, leading to poor oral bioavailability and irregular distribution, which affects the effectiveness and safety of treatments for viral infections.

Innovation Solution

Development of compounds with improved solubility, stability, and permeability properties, formulated into pharmaceutical compositions for oral administration, enhancing systemic circulation and bioavailability.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Ease of operation

If oral administration is used for drug delivery, then patient compliance and convenience are improved, but oral bioavailability deteriorates due to poor physicochemical properties

Engineering Contradiction:
Improvepatient complianceVSAvoidoral bioavailability
Core Design Contradiction:
Ease of operationVSReliability

Solution Approach 1:

The patent modifies the physicochemical parameters of the drug molecule by forming salt compounds with specific bases (e.g., arginine, lysine, ornithine) to improve solubility and stability while maintaining antiviral activity, thereby enhancing oral bioavailability

Inventive Principle:
Principle #35Parameter changes

Solution Approach 2:

The patent creates composite pharmaceutical compositions combining the antiviral compound with pharmaceutically acceptable excipients and bases to form stable salt forms that simultaneously improve solubility, stability, and permeability properties for better oral delivery

Inventive Principle:
Principle #40Composite materials

2Reliability

If the drug molecule has high potency, then treatment effectiveness is improved, but aqueous solubility deteriorates leading to poor oral bioavailability

Engineering Contradiction:
Improvetreatment effectivenessVSAvoidaqueous solubility
Core Design Contradiction:
ReliabilityVSQuantity of substance

Solution Approach 1:

The patent changes the chemical form of the antiviral compound by forming salts with different bases, which maintains the active pharmacological moiety while improving aqueous solubility parameters for better oral absorption

Inventive Principle:
Principle #35Parameter changes

3Ease of operation

If the drug is administered orally, then non-invasiveness is improved, but instability in intestinal fluid deteriorates leading to low bioavailability

Engineering Contradiction:
Improvenon-invasivenessVSAvoidinstability
Core Design Contradiction:
Ease of operationVSStability of the object's composition

Solution Approach 1:

The patent modifies the chemical stability parameters by forming salt compounds that are resistant to degradation in intestinal fluid, thereby maintaining drug integrity during oral passage while preserving non-invasive administration benefits

Inventive Principle:
Principle #35Parameter changes

Data Source

PatentUS12448383B2Compounds and methods for treatment of viral infections
Publication Date: 2025.10.21 GILEAD SCIENCES INC
  • US12448383B2 patent drawing
  • US12448383B2 patent drawing
  • US12448383B2 patent drawing

AI summary

Compounds and methods of using said compounds, singly or in combination with additional agents, and salts or pharmaceutical compositions of said compounds for the treatment of viral infections are disclosed.