Lyophilized Calpain Probe Preparation for Solubility and Stability
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Solution Overview
Problem
The probe used for detecting calpain activity has low water solubility and stability issues, making it difficult to provide an administration liquid at a desired concentration for clinical use.
Innovation Solution
A lyophilized preparation containing a compound represented by a specific general formula, optionally with a solubilizing agent, antioxidant, and other additives, which improves solubility and stability of the probe.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Ease of operation
If the probe is used in aqueous solution form, then it can be administered to patients, but the probe has low water solubility and cannot be instantly dissolved, making it difficult to provide administration liquid at desired concentration
Solution Approach 1:
The patent changes the physical state of the probe from liquid to solid lyophilized form, which fundamentally alters its dissolution behavior. The lyophilized probe can be instantly dissolved in water to achieve desired concentrations, resolving the contradiction between ease of operation (dissolution speed) and quantity of substance (water solubility).
Solution Approach 2:
The probe is pre-processed into lyophilized form before administration, which prepares it in advance for rapid dissolution. This preliminary action of lyophilization enables the probe to be instantly dissolved when needed, solving the dissolution speed issue without compromising its ability to achieve desired concentration.
2Ease of operation
If the probe is stored as aqueous solution, then it is ready for use, but the purity and stability of the probe deteriorate over time
Solution Approach 1:
The patent utilizes phase transition by converting the probe from liquid aqueous solution to solid lyophilized form for storage. This phase change dramatically improves stability and purity maintenance during storage, while the solid form can be easily converted back to liquid form when needed, maintaining readiness for use.
Solution Approach 2:
The probe is pre-prepared in lyophilized form with stabilizing agents before storage, which prevents degradation during storage. This preliminary preparation ensures the probe maintains high purity and stability, yet can be quickly reconstituted when needed for administration.
3Reliability
If the probe concentration is increased for practical administration, then clinical effectiveness improves, but the low water solubility prevents achieving desired concentration
Solution Approach 1:
The patent changes the physical form of the probe to lyophilized powder, which enables high concentration achievement upon reconstitution. This parameter change from liquid to solid form allows the probe to be administered at clinically effective concentrations that would be unattainable with the original aqueous solution form.
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 lyophilized preparation enhances the water solubility and stability of the probe, allowing for the preparation of an administration liquid with a practical concentration.
Implementation Method 1
A calpain inhibitor compound (I) or a salt thereof may be subjected to lyophilization
Data Source
Figure 1
AI summary
The present invention provides: a lyophilized preparation including a compound represented by the following general formula (I) or a salt thereof; a lyophilization solution including a compound represented by the following general formula (I) or a salt thereof, a solubilizing agent, and water; methods of producing the same; and a liquid preparation obtained by reconstituting the above-mentioned lyophilized preparation.