Sustained-Release 25-Hydroxyvitamin D2/D3 for Stable Blood Levels
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Solution Overview
Problem
Current Vitamin D supplements cause surges in blood levels, leading to undesirable storage, catabolism, and aberrations in calcium and phosphorus metabolism, and are ineffective in maintaining optimal 25-hydroxyvitamin D levels.
Innovation Solution
A sustained release formulation of 25-hydroxyvitamin D2 and/or 25-hydroxyvitamin D3 dispersed in a wax matrix with an enteric coating, designed for controlled release in the ileum, avoiding first-pass effects and supraphysiologic surges.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Quantity of substance
If high doses of Vitamin D supplements are administered to treat deficiency, then blood levels of 25-hydroxyvitamin D increase rapidly, but this causes supraphysiologic surges leading to excessive hormone production, catabolism, and aberrations in calcium and phosphorus metabolism
Solution Approach 1:
The patent applies dynamics by transitioning from static high-dose supplementation to a dynamic controlled-release system that adjusts the release rate of 25-hydroxyvitamin D to maintain physiological levels. The formulation releases the prohormone gradually over time, preventing supraphysiologic surges while ensuring adequate blood levels are maintained for effective treatment of Vitamin D deficiency.
Solution Approach 2:
The patent employs preliminary action by pre-formulating 25-hydroxyvitamin D in a controlled-release delivery system before administration. The formulation is designed in advance to release the prohormone at a controlled rate, preventing the need for high initial doses that would cause harmful surges. This preliminary structuring of the dosage form ensures safe and effective delivery from the start of treatment.
2Stability of the object's composition
If sustained release formulation is used to maintain stable blood levels, then supraphysiologic surges are avoided, but the formulation complexity increases with wax matrix and enteric coating
Solution Approach 1:
The patent applies parameter changes by modifying the physical and chemical properties of the 25-hydroxyvitamin D formulation. The wax matrix and enteric coating alter the release parameters of the prohormone, transforming it from immediate-release to controlled-release. These parameter changes in the formulation structure enable stable blood levels to be maintained while avoiding the complexities of complex delivery systems.
3Ease of operation
If immediate release Vitamin D supplements are used, then the formulation is simple and easy to administer, but they cause marked surges in blood 25-hydroxyvitamin D levels leading to toxicity risk
Solution Approach 1:
The patent employs an intermediary approach by introducing a controlled-release formulation as a mediator between the administered 25-hydroxyvitamin D and the bloodstream. This intermediary delivery system, using wax matrix and enteric coating, modulates the release rate to prevent marked surges while maintaining ease of oral administration. The formulation acts as a buffer that safely delivers the prohormone over time.
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 effectively maintains stable blood levels of 25-hydroxyvitamin D above 30 ng/mL, reducing the risk of toxicity and promoting optimal Vitamin D metabolism.
Implementation Method 1
the 25-hydroxyvitamin D2, the 25-hydroxyvitamin D3, or the combination of 25-hydroxyvitamin D2 and 25-hydroxyvitamin D3 is dispersed within a wax matrix and encased with an enteric coating material
Implementation Method 2
A sustained release formulation of 25-hydroxyvitamin D2 and/or 25-hydroxyvitamin D3 dispersed in a wax matrix with an enteric coating, designed for controlled release in the ileum
Data Source
AI summary
Methods and compositions for treating 25-hydroxyvitamin D insufficiency or deficiency in a patient are described herein. The method includes orally administering to the patient a sustained release formulation of 25-hydroxyvitamin D2, 25-hydroxyvitamin D3, or a combination of 25-hydroxyvitamin D2 and 25-hydroxyvitamin D3. The 25-hydroxyvitamin D is administered in combination with one or more agents selected from: one or more calcium salts, bisphosphonates, calcimimetics, nicotinic acid, iron, phosphate binders, glycemic control agents, hypertension control agents, and antineoplastic agents.