High-Concentration IL-17A Antibody Formulation With Excipient Stabilization
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Solution Overview
Problem
Existing IL-17A monoclonal antibody formulations suffer from instability due to aggregation, hydrolysis, and oxidation, affecting their safety and efficacy, and require improved stability to enhance clinical medication effectiveness.
Innovation Solution
A pharmaceutical composition comprising an IL-17A antibody with a concentration of 125-155 mg/mL, buffered with acetate-acetic acid or histidine-acetic acid, and stabilized with sodium chloride, sugars, and surfactants like polysorbate, maintaining stability under stress conditions.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Productivity
If the IL-17A antibody concentration is increased to reduce administration frequency, then the effectiveness and convenience of clinical medication is improved, but the stability of the antibody deteriorates due to aggregation, hydrolysis, and oxidation
Solution Approach 1:
The patent optimizes formulation parameters including buffer composition (acetate-acetic acid or histidine-acetic acid at specific pH ranges), stabilizer concentrations (sugars, amino acids, polyols), and surfactant types to enable stable storage of high-concentration (125-155 mg/mL) IL-17A antibody formulations, resolving the contradiction between concentration and stability
Solution Approach 2:
The patent introduces formulation excipients as intermediary substances that protect the IL-17A antibody from degradation. These include buffers that maintain pH stability, stabilizers that prevent aggregation and hydrolysis, and surfactants that reduce surface tension and prevent adsorption, thereby enabling high-concentration formulations to remain stable
2Productivity
If the antibody concentration is increased to 125-155 mg/mL, then the medication effectiveness is improved, but the complexity of formulation development increases due to multiple physical and chemical reactions
Solution Approach 1:
The patent divides the formulation into distinct functional components: buffer system (pH control), stabilizers (aggregation and hydrolysis prevention), surfactants (adsorption prevention), and antioxidants (oxidation prevention). This segmentation allows systematic optimization of each component's concentration and type to manage formulation complexity while achieving high stability
3Productivity
If the antibody concentration is increased, then the frequency of medication is reduced, but the safety of clinical medication is compromised due to by-product formation from aggregation, hydrolysis, and oxidation
Solution Approach 1:
The patent applies preliminary protective measures by incorporating stabilizers, surfactants, and antioxidants into the formulation before storage and administration. These agents preemptively prevent aggregation, hydrolysis, and oxidation reactions that would otherwise generate harmful by-products, thereby ensuring safety even at high concentrations and reduced administration frequencies
Data Source
Figure 1~2
AI summary
The present application relates to a pharmaceutical composition of an anti-human IL-17A monoclonal antibody and use thereof. The pharmaceutical composition comprises: (a) an anti-human IL-17A monoclonal antibody; and (b) a pharmaceutically acceptable carrier. The pharmaceutical composition described in the present application can improve the stability of the anti-human IL-17A monoclonal antibody, thus reducing the administration frequency, and improving the safety and effectiveness of clinical use.