Carbetocin Formulation pH Optimization for Room Temperature Stability
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Solution Overview
Problem
Current uterotonic drugs for preventing postpartum hemorrhage, such as oxytocin and Syntometrine, have limitations including short half-life, side effects, and contraindications, while carbetocin offers a long-acting solution but requires refrigeration, limiting its stability and usability in tropical regions.
Innovation Solution
A liquid pharmaceutical composition of carbetocin with a pH range of 5.4 to 5.65 and a concentration of 0.05 to 0.5 mg/mL, which is room temperature stable for up to two years, allowing for use in ambulances and tropical regions without refrigeration.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Duration of action of moving object
If carbetocin is formulated for long-acting uterotonic effect, then duration of action is improved, but stability at room temperature deteriorates
Solution Approach 1:
The patent changes the pH parameter of the formulation to a specific range (5.0-6.0, preferably 5.2-5.6) to achieve both long-acting effect and room temperature stability. This parameter optimization allows the carbetocin formulation to maintain stability without refrigeration while preserving its extended duration of action compared to conventional oxytocin formulations
2Stability of the object's composition
If carbetocin requires refrigeration for stability, then stability is improved, but ease of operation deteriorates
Solution Approach 1:
By optimizing the pH to 5.0-6.0 and selecting appropriate excipients, the formulation achieves stability at room temperature (25°C) for at least 24 months, eliminating the need for refrigeration. This parameter change transforms the storage requirements, making the drug easy to operate and distribute in resource-limited settings without cold chain infrastructure
3Adaptability or versatility
If carbetocin is used in tropical regions, then adaptability is improved, but stability deteriorates due to heat and humidity
Solution Approach 1:
The formulation is specifically designed with pH 5.0-6.0 and stabilized with appropriate excipients to withstand tropical conditions (high temperature and humidity). Stability studies confirm the formulation maintains integrity under these challenging environmental conditions, enabling deployment in tropical and developing regions where refrigeration is unavailable
Data Source
Figure 1
Figure 1a
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AI summary
The present invention relates to pharmaceutical compositions having improved stability.