Albuvirtide Lyophilized Composition With Acidic Buffer Stability

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Solution Overview

Problem

Existing compositions of albuvirtide, an HIV-1 fusion inhibitor, face challenges in stability and manufacturing efficiency, requiring tailored pharmaceutical excipients to achieve optimal physical and pharmaceutical properties.

Innovation Solution

Development of liquid and lyophilized compositions of albuvirtide with defined buffer systems, organic solvent ratios, and pH ranges between 1.0 and 3.5, along with specific concentrations of albuvirtide and acidic buffers, enhancing stability and ease of administration.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Stability of the object's composition

If conventional compositions of albuvirtide are used, then manufacturing can proceed with standard excipients, but stability and purity are compromised

Engineering Contradiction:
Improvealbuvertide stabilityVSAvoidmanufacturing complexity
Core Design Contradiction:
Stability of the object's compositionVSEase of manufacture

Solution Approach 1:

The patent changes critical parameters of the composition including pH (adjusted to acidic range), buffer concentration, and excipient ratios to optimize stability. By systematically adjusting these parameters, the invention achieves improved albuvirtide stability while maintaining manufacturability through defined formulation guidelines.

Inventive Principle:
Principle #35Parameter changes

Solution Approach 2:

The patent introduces specific buffer systems and excipients as intermediary substances that mediate between the albuvirtide and the formulation environment. These intermediaries protect the albuvirtide from degradation while allowing standard manufacturing processes to be used, thus resolving the contradiction between stability and ease of manufacture.

Inventive Principle:
Principle #24Intermediary (Mediator)

2Reliability

If albuvirtide compositions are formulated with specific buffer systems and pH control, then stability and purity are improved, but formulation complexity increases

Engineering Contradiction:
Improvecomposition reliabilityVSAvoidformulation complexity
Core Design Contradiction:
ReliabilityVSDevice complexity

Solution Approach 1:

The patent establishes specific parameter ranges for pH (acidic condition), buffer concentration, and excipient ratios that optimize composition reliability. By defining these parameters within optimal ranges rather than requiring exact values, the invention maintains reliability while reducing formulation complexity through flexible specification ranges.

Inventive Principle:
Principle #35Parameter changes

Solution Approach 2:

The patent designs buffer systems that serve multiple functions: maintaining pH, providing stability, and facilitating manufacturing. This multi-functionality reduces the need for separate components, thereby improving reliability without proportionally increasing formulation complexity.

Inventive Principle:
Principle #6Universality (Multi-functionality)

3Stability of the object's composition

If lyophilization is performed to improve storage stability, then purity is maintained, but manufacturing steps increase

Engineering Contradiction:
Improvestorage stabilityVSAvoidmanufacturing efficiency
Core Design Contradiction:
Stability of the object's compositionVSProductivity

Solution Approach 1:

The patent incorporates stabilizing excipients and buffer systems into the formulation before lyophilization. This preliminary action prepares the composition to withstand the lyophilization process and storage conditions, maintaining purity while reducing the need for additional post-lyophilization interventions that would decrease manufacturing efficiency.

Inventive Principle:
Principle #10Preliminary action

Solution Approach 2:

The patent optimizes formulation parameters (pH, buffer concentration, excipient ratios) specifically for lyophilization compatibility. By adjusting these parameters in advance, the invention enables stable storage while minimizing the complexity of the lyophilization process itself, thus protecting productivity.

Inventive Principle:
Principle #35Parameter changes

Data Source

PatentEP3965795B1Stable albuvirtide compositions
Publication Date: 2025.11.26 NANJING QIANYAN BIOTECH
  • EP3965795B1 patent drawingFigure 1
  • EP3965795B1 patent drawingFigure 2
  • EP3965795B1 patent drawingFigure 3

AI summary

A liquid compositions and stable lyophilized compositions comprising albuvirtide, an HIV-1 fusion inhibitor. The present invention also provides the manufacturing process thereof and use of these compositions for the prevention, treatment or prophylaxis of diseases caused by HIV.