Liquid Picosulfate Formulation Stabilized for Immediate Dosing
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Solution Overview
Problem
Existing formulations of picosulfate, particularly those combined with magnesium oxide and citric acid, do not dissolve immediately and require stirring, risking incomplete dosing if not stirred properly, and picosulfate formulations are unstable when stored or allowed to stand.
Innovation Solution
Development of stable liquid formulations containing picosulfate with an antioxidant, such as sodium metabisulfite, to maintain stability for extended periods, allowing for immediate use without stirring.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If picosulfate is formulated as a solid preparation requiring dissolution, then the formulation can be stored stably, but the patient must stir for 2-3 minutes to ensure complete dissolving, risking incomplete dosing
Solution Approach 1:
The patent changes the physical state parameter from solid to liquid formulation. The liquid formulation contains picosulfate, magnesium citrate, and antioxidant already dissolved in water, eliminating the need for patient stirring while ensuring complete dosing. This parameter change directly resolves the contradiction between dosing completeness and operation simplicity.
2Ease of operation
If liquid formulation containing picosulfate is prepared immediately for use, then immediate administration is possible, but the formulation is unstable and degrades when stored
Solution Approach 1:
The patent introduces an antioxidant (such as sodium metabisulfite, ascorbic acid, or other reducing agents) as an intermediary substance that protects picosulfate from oxidation and degradation. This intermediary stabilizes the liquid formulation during storage while maintaining its immediate use capability, resolving the contradiction between stability and immediate use.
Solution Approach 2:
The patent changes the chemical stability parameter by adjusting pH (maintaining between 4.0-6.5) and adding antioxidants. These parameter changes enable the liquid formulation to remain stable during storage while still allowing immediate administration without degradation.
3Stability of the object's composition
If solid picosulfate preparation is used, then storage stability is maintained, but the formulation does not dissolve immediately and requires patient stirring
Solution Approach 1:
The patent changes the physical state from solid to liquid and pre-dissolves all components (picosulfate, magnesium citrate, and antioxidants) during manufacturing. This parameter change achieves immediate dissolution upon administration while maintaining formulation stability through controlled storage conditions and antioxidant protection.
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 formulations remain stable for at least 10 days to 2 years, maintaining effectiveness and ensuring complete dosing by preventing degradation and precipitation.
Implementation Method 1
formulations containing picosulfate, e.g., sodium picosulfate, are unstable when stored or allowed to stand
Implementation Method 2
the products include citric acid, magnesium oxide, and sodium picosulfate, as active ingredients
Data Source
AI summary
Stable liquid formulations containing picosulfate and magnesium citrate are provided. The formulations are useful to treat constipation or for the clearance of the bowel prior to X-ray examination, endoscopy or surgery.