Sincalide Formulations Without Buffers
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Solution Overview
Problem
Current formulations of sincalide, such as KINEVAC®, face stability issues and shortages, requiring additional stable solid formulations and ready-to-use liquid formulations to reduce drug preparation errors and improve storage stability.
Innovation Solution
Development of storage stable solid and liquid sincalide compositions without buffers or surfactants/solubilizers, which maintain high purity and activity over extended periods, including at least 18 months for solid compositions and 6 months for liquid compositions, using excipients like pentetic acid, arginine hydrochloride, lysine hydrochloride, and mannitol.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Stability of the object's composition
If traditional formulations with buffers and surfactants are used, then stability is improved, but formulation complexity and risk of preparation errors increase
Solution Approach 1:
The patent removes buffers and surfactants from the sincalide formulation, retaining only essential excipients (mannitol, amino acids, chelating agents). This extraction of non-essential components simplifies the formulation while maintaining stability through the remaining critical ingredients.
Solution Approach 2:
The patent changes the formulation parameters by eliminating buffer systems and surfactant components, transitioning from a complex multi-component formulation to a simplified formulation with fewer ingredients that maintains stability through optimized concentrations of essential excipients.
2Stability of the object's composition
If traditional formulations with multiple excipients are used, then stability is improved, but manufacturing complexity and cost increase
Solution Approach 1:
The patent extracts and removes non-essential excipients (buffers, surfactants) from the formulation, reducing the number of components that need to be sourced, handled, and controlled during manufacturing, thereby simplifying the manufacturing process.
Solution Approach 2:
The remaining excipients in the simplified formulation perform multiple functions: mannitol provides bulking and tonicity, amino acids stabilize the peptide, and chelating agents prevent metal-catalyzed degradation. This multi-functionality reduces the need for multiple specialized excipients.
3Duration of action of stationary object
If traditional formulations are used, then initial stability is maintained, but shelf life is limited to 18-24 months
Solution Approach 1:
The patent changes the formulation parameters by optimizing the concentrations and combinations of essential excipients, creating a formulation that maintains stability over extended periods. The simplified formulation with focused use of stabilizing agents extends shelf life beyond traditional limits.
Solution Approach 2:
The formulation includes chelating agents and amino acid stabilizers that proactively prevent degradation mechanisms before they occur, extending the functional shelf life by preemptively addressing potential stability issues during storage.
Data Source
AI summary
Disclosed herein are solid compositions that comprise sincalide and are storage stable and which lack a buffer, and optionally, also lack a surfactant/solubilizer, wherein such compositions are storage stable. Also disclosed herein are liquid compositions that comprise sincalide, wherein such compositions are storage stable, and may lack buffer and/or surfactant/solubilizer. Also provided are methods of making and administering the solid or liquid storage stable compositions to a patient in need of, e.g., for the treatment, prevention, and/or diagnosis of gall bladder- and/or pancreatic disorders; or other diagnostic imaging.