Stable Liquid Pantoprazole Formulation Without Lyophilization
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Solution Overview
Problem
Existing pantoprazole formulations face challenges with hydrolysis and thermal instability, requiring complex and costly lyophilization processes, and necessitate time-consuming reconstitution steps, limiting their stability and usability.
Innovation Solution
A stable, non-aqueous composition of pantoprazole with polyethylene glycol and a stabilizer, such as sodium hydroxide, allowing for a ready-to-use, directly injectable formulation that can be stored at room temperature and easily administered without reconstitution.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Stability of the object's composition
If freeze-dried/lyophilized formulations are used to ensure stability, then storage stability is improved, but device complexity and manufacturing cost increase
Solution Approach 1:
The patent changes the physical state parameter from solid (freeze-dried powder) to liquid (aqueous solution), and adjusts concentration parameters to create a stable liquid formulation that does not require lyophilization. This resolves the contradiction by achieving stability through parameter optimization rather than complex formulation processes.
2Stability of the object's composition
If freeze-dried/lyophilized formulations are used to ensure stability, then storage stability is improved, but manufacturing cost increases
Solution Approach 1:
The patent optimizes concentration and composition parameters to create a stable liquid formulation that eliminates the need for expensive lyophilization equipment and multi-step drying processes, thereby reducing manufacturing cost while maintaining stability.
3Stability of the object's composition
If reconstitution steps are required for administration, then formulation stability is maintained, but loss of time increases
Solution Approach 1:
The patent performs the dissolution and mixing actions in advance during manufacturing, creating a ready-to-use liquid formulation. This eliminates the need for reconstitution at the time of administration, thereby reducing administration time while maintaining formulation stability through proper preservative design.
4Stability of the object's composition
If multiple dilution steps are required for infusion, then formulation stability is maintained, but device complexity increases
Solution Approach 1:
The patent pre-dilutes and prepares the formulation in the correct concentration during manufacturing, creating a ready-to-administer solution. This eliminates the need for multiple dilution steps at the point of use, thereby reducing administration complexity while maintaining stability through controlled formulation design.
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 provides long-term stability, enabling fast and convenient administration, suitable for self-administration at home, and reduces the complexity and cost associated with traditional lyophilized formulations.
Implementation Method 1
a concentrated, storage stable, non-aqueous composition of pantoprazole comprising: 20-80 mg of a pharmaceutically acceptable salt of pantoprazole (API), expressed in amount of pantoprazole, polyethylene glycol in a quantity for the dissolution of the API
Implementation Method 2
optionally a stabilizer, preferably an alkali metal hydroxide, more preferably sodium hydroxide
Data Source
AI summary
The present invention provides a concentrated, storage stable, liquid composition of pantoprazole or a pharmaceutically acceptable salt thereof. The invention further provides uses for the composition, and packaging containers comprising the composition. In particular, the present invention relates to stable pantoprazole sodium formulations with controlled room temperature as storage condition, in the form of a ready-to-use liquid solution or in the form of a ready-to-dilute formulation, for dilution with infusion solution, processes for their preparation and use.