Cellulosic-Stabilized Vitamin D Release Formulation for Storage Stability
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Solution Overview
Problem
Existing controlled release formulations of 25-hydroxyvitamin D are unstable during storage, leading to variations in dissolution profiles and undesirable side effects, such as supraphysiologic surges in vitamin D levels and increased catabolism, which can be mitigated by incorporating a cellulosic compound to stabilize the formulation.
Innovation Solution
A stabilized formulation comprising 25-hydroxyvitamin D and a cellulosic compound, such as cellulose derivatives, maintains a consistent dissolution profile and bioavailability over extended periods, ensuring controlled release in the gastrointestinal tract.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If controlled release formulations of 25-hydroxyvitamin D are used, then therapeutic efficacy is improved by avoiding supraphysiologic surges and reducing catabolism, but storage stability deteriorates leading to variations in dissolution profiles
Solution Approach 1:
The patent introduces a stabilizer as an intermediary substance that mediates between the 25-hydroxyvitamin D compound and the controlled release matrix. This stabilizer prevents direct interactions that would otherwise cause degradation or instability during storage, thereby maintaining dissolution profile consistency while preserving the therapeutic benefits of controlled release
Solution Approach 2:
The patent creates a composite formulation system combining multiple components: 25-hydroxyvitamin D compound, controlled release matrix, and stabilizer. This composite structure leverages the synergistic effects of each component - the matrix provides controlled release, the stabilizer maintains composition stability, and together they achieve both improved therapeutic efficacy and storage stability
2Ease of manufacture
If immediate release formulations are used, then manufacturing simplicity is maintained, but harmful side effects increase due to supraphysiologic surges in vitamin D levels
Solution Approach 1:
The patent segments the release of 25-hydroxyvitamin D into controlled, gradual portions through the use of a controlled release matrix. This segmentation prevents the immediate, complete release that causes supraphysiologic surges, while the manufacturing process remains relatively simple by using established matrix formulation techniques
3Object-generated harmful factors
If controlled release formulations are used, then side effects are reduced by maintaining constant blood levels, but dissolution profile consistency deteriorates during storage
Solution Approach 1:
The patent applies preliminary stabilization action by incorporating the stabilizer into the formulation during manufacturing. This stabilizer proactively prevents degradation and maintains dissolution profile consistency throughout storage, ensuring that the controlled release characteristics and constant blood level maintenance remain effective throughout the product shelf life
Data Source
AI summary
A stabilized formulation for controlled release of a vitamin D compound is disclosed. The formulation can comprise one or both of 25-hydroxyvitamin D2 and 25-hydroxyvitamin D3 and a stabilizing compound. The stabilized formulations exhibit a stable dissolution profile following exposure to storage conditions and demonstrate improved pharmacokinetic parameters compared to unstabilized formulations.