Anti-IL-4R Antibody Liquid Formulation for Stability and Low Viscosity
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Solution Overview
Problem
Therapeutic antibodies, such as those targeting the human interleukin-4 receptor alpha (hIL-4Rα), face challenges in maintaining stability during storage and administration due to degradation, aggregation, and chemical modifications in liquid formulations, necessitating a need for improved pharmaceutical formulations.
Innovation Solution
A liquid pharmaceutical formulation comprising a human antibody that binds to hIL-4Rα, combined with a buffer, organic cosolvent, thermal stabilizer, and viscosity reducer, at specific concentrations and pH, to enhance stability and reduce viscosity.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Ease of operation
If therapeutic antibodies are formulated in liquid solution to enable administration, then the antibody becomes suitable for patient administration, but the antibody is prone to degradation, aggregation, or undesired chemical modifications
Solution Approach 1:
The patent modifies formulation parameters by adjusting pH to a specific range (5.0-6.5) and incorporating stabilizing excipients at optimized concentrations to prevent antibody degradation while maintaining liquid formulation suitability for administration
Solution Approach 2:
The patent introduces stabilizing excipients (such as sugars, amino acids, or peptides) as intermediary substances that mediate between the antibody and the formulation environment, protecting the antibody from degradation, aggregation, or chemical modifications while maintaining liquid solution properties
2Quantity of substance
If the antibody concentration is increased to improve therapeutic efficacy, then the treatment effectiveness is enhanced, but the formulation viscosity increases and visual quality deteriorates
Solution Approach 1:
The patent adjusts formulation parameters including pH, excipient concentrations, and additive compositions to enable higher antibody concentrations while maintaining acceptable viscosity and visual quality characteristics
Solution Approach 2:
The patent uses visual and physical property matching to create a formulation that replicates desirable characteristics of ideal solutions, using excipients to mimic the behavior of pure antibody solutions at high concentrations
3Stability of the object's composition
If excipients are added to improve antibody stability, then the antibody stability is enhanced, but the formulation complexity and manufacturing difficulty increase
Solution Approach 1:
The patent optimizes excipient concentrations and pH levels to achieve maximum stability with minimal excipient amounts, reducing formulation complexity while maintaining antibody stability
Solution Approach 2:
The patent identifies and removes unnecessary excipients from the formulation, extracting only the essential stabilizing components needed to maintain antibody stability, thereby simplifying the formulation and reducing manufacturing complexity
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 formulation maintains at least 90% of the antibody in its native form after six months at 5°C and eight weeks at 45°C, with minimal aggregation and acidic forms, achieving a stable and convenient administration.
Implementation Method 1
a thermal stabilizer
Implementation Method 2
an organic cosolvent
Implementation Method 3
a viscosity reducer
Data Source
AI summary
The present invention provides pharmaceutical formulations comprising a human antibody that specifically binds to human interleukin-4 receptor (hIL-4R). The formulations may contain, in addition to an anti-hIL-4R antibody, at least one amino acid, at least one sugar, or at least one non-ionic surfactant. The pharmaceutical formulations of the present invention exhibit a substantial degree of antibody stability after storage for several months.