Lyophilized Anti-α4β7 Antibody Formulation for High-Concentration Stability
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Solution Overview
Problem
Existing lyophilized formulations of therapeutic antibodies, such as anti-α4β7 antibodies, face challenges in maintaining stability and biological activity due to factors like temperature, pH changes, and aggregation, especially at high concentrations, making them unsuitable for intravenous or subcutaneous administration.
Innovation Solution
A stable lyophilized pharmaceutical formulation of anti-α4β7 antibody comprising specific components like buffer, sugar, bulking agent, viscosity reducer, antioxidant, and surfactant, with a molar ratio of sucrose to antibody less than 600:1 and pH between 6.0 to 7.0, ensuring stability and activity.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Productivity
If high concentration liquid formulation is used, then injection volume and administration frequency are reduced, but the formulation becomes susceptible to degradation and aggregation
Solution Approach 1:
The patent optimizes the concentration of excipients including buffer (10-100 mM), sugar (50-150 mg/mL), bulking agent (20-50 mg/mL), viscosity reducer (5-15 mg/mL), antioxidant (1-5 mg/mL), and surfactant (0.1-1 mg/mL) to maintain formulation stability at high antibody concentrations (50-200 mg/mL), enabling reduced injection volume and administration frequency without sacrificing stability
Solution Approach 2:
The patent creates a composite liquid formulation system combining multiple excipients (buffer, sugar, bulking agent, viscosity reducer, antioxidant, and surfactant) with the therapeutic antibody, where each component contributes specific protective functions that collectively maintain stability at high concentrations suitable for frequent subcutaneous or intravenous administration
2Reliability
If lyophilized formulation is used, then stability is improved, but reconstitution requires significant vial overfill and involves high production cost
Solution Approach 1:
The patent optimizes the concentration of excipients including buffer (10-100 mM), sugar (50-150 mg/mL), bulking agent (20-50 mg/mL), viscosity reducer (5-15 mg/mL), antioxidant (1-5 mg/mL), and surfactant (0.1-1 mg/mL) to maintain formulation stability at high antibody concentrations (50-200 mg/mL), enabling reduced injection volume and administration frequency without sacrificing stability
Solution Approach 2:
The patent creates a composite liquid formulation system combining multiple excipients (buffer, sugar, bulking agent, viscosity reducer, antioxidant, and surfactant) with the therapeutic antibody, where each component contributes specific protective functions that collectively maintain stability at high concentrations suitable for frequent subcutaneous or intravenous administration
3Ease of operation
If liquid formulation is used, then ease of preparation and administration is improved, but proteins are susceptible to denaturation and aggregation under stress
Solution Approach 1:
The patent optimizes the concentration of excipients including buffer (10-100 mM), sugar (50-150 mg/mL), bulking agent (20-50 mg/mL), viscosity reducer (5-15 mg/mL), antioxidant (1-5 mg/mL), and surfactant (0.1-1 mg/mL) to maintain formulation stability at high antibody concentrations (50-200 mg/mL), enabling reduced injection volume and administration frequency without sacrificing stability
Solution Approach 2:
The patent creates a composite liquid formulation system combining multiple excipients (buffer, sugar, bulking agent, viscosity reducer, antioxidant, and surfactant) with the therapeutic antibody, where each component contributes specific protective functions that collectively maintain stability at high concentrations suitable for frequent subcutaneous or intravenous administration
Data Source
AI summary
The invention provides stable lyophilized formulation of anti-α4ß7 antibody comprising buffer, sugar, bulking agent, viscosity reducer, antioxidant and surfactant.