Tigecycline Liquid Formulation Stability
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Solution Overview
Problem
The existing formulations of tigecycline for injection require reconstitution, making them costly, inconvenient, and not in a ready-to-use form, which complicates manufacturing, distribution, and administration.
Innovation Solution
A stable, ready-to-use liquid parenteral formulation of tigecycline in infusion bags or vials, incorporating pharmaceutically acceptable excipients such as calcium chloride, sodium chloride, and sodium bisulfite, which eliminates the need for reconstitution and ensures stability and safety.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Stability of the object's composition
If tigecycline is supplied as a lyophilized powder for reconstitution, then storage stability is improved, but ease of operation deteriorates due to the additional reconstitution step required
Solution Approach 1:
The patent changes the physical state parameter from solid lyophilized powder to liquid solution, and adjusts the pH parameter to 3.0-5.0 range to achieve both stability and ready-to-use convenience. This parameter transformation resolves the contradiction by allowing the drug to be stored as a stable liquid formulation without requiring reconstitution.
Solution Approach 2:
The reconstitution process is performed in advance during manufacturing to create a ready-to-use liquid formulation. This preliminary action eliminates the need for reconstitution at the point of administration, resolving the contradiction between storage stability and ease of operation.
2Ease of manufacture
If tigecycline is supplied as a lyophilized powder, then manufacturing cost is reduced, but productivity deteriorates due to the additional reconstitution step at pharmacy
Solution Approach 1:
The reconstitution step is moved from the pharmacy setting to the manufacturing process. By performing reconstitution in advance during drug production, the patent eliminates the time-consuming pharmacy操作步骤, thereby improving productivity while maintaining manufacturing efficiency.
3Ease of operation
If tigecycline is formulated as a ready-to-use liquid solution, then ease of operation is improved, but stability deteriorates due to potential degradation in liquid form
Solution Approach 1:
The patent applies parameter changes by adjusting the pH to the 3.0-5.0 range and selecting specific excipients to enhance the stability of the liquid formulation. This resolves the contradiction by demonstrating that liquid solutions can be both ready-to-use and stable through proper formulation parameters.
Solution Approach 2:
Excipients such as buffers and antioxidants are introduced as intermediary substances to protect tigecycline from degradation in liquid form. These intermediaries maintain solution stability while allowing the formulation to remain ready-to-use without reconstitution.
4Stability of the object's composition
If complex excipients are added to ensure stability, then stability is improved, but device complexity deteriorates due to multiple ingredients
Solution Approach 1:
The patent uses parameter changes (pH 3.0-5.0) as the primary stability mechanism rather than relying on multiple complex excipients. This approach achieves formulation stability with minimal ingredients, resolving the contradiction between stability and formulation 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 high purity and stability for extended periods, reducing manufacturing and pharmacy costs, and simplifies administration by providing a clear, ready-to-use solution suitable for various bacterial infections.
Implementation Method 1
the formulation includes a pharmaceutically acceptable antioxidant. In at least one embodiment, the antioxidant comprises sodium bisulfite.
Implementation Method 2
the formulation includes a pharmaceutically acceptable complex forming agent. In at least one embodiment, the complex forming agent comprises at least one of calcium chloride and sodium chloride.
Data Source
AI summary
Liquid parenteral formulations are provided that include tigecycline and at least one or more pharmaceutically acceptable excipient or adjuvant, where the formulation is ready to use without additional steps for reconstitution at the time of administration.