25-Hydroxy Vitamin D3 Cyclodextrin Inclusion Complex
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Solution Overview
Problem
Current formulations of 25-Hydroxy Vitamin D3 are prone to degradation due to unsaturated double bonds and have low bioavailability due to being dissolved in oil, leading to short shelf-life and poor absorption in animals.
Innovation Solution
A complex is formed between 25-Hydroxy Vitamin D3 and β-cyclodextrin, where each 25-Hydroxy Vitamin D3 molecule is enclosed within two β-cyclodextrin molecules, enhancing stability and bioavailability through improved water solubility and protection from oxidation.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Ease of manufacture
If 25-Hydroxy Vitamin D3 is dissolved in vegetable oil with antioxidant, then the formulation can be manufactured, but the product has short shelf-life and is prone to oxidation degradation
Solution Approach 1:
β-cyclodextrin serves as an intermediary substance that forms an inclusion complex with 25-Hydroxy Vitamin D3. The cyclodextrin cavity encapsulates the vitamin molecule, protecting it from oxidation while the outer surface provides water solubility. This mediator resolves the contradiction by enabling stable formulation without oil-based antioxidants.
Solution Approach 2:
The invention creates a composite material system where 25-Hydroxy Vitamin D3 is complexed with β-cyclodextrin in a specific ratio (6:1 to 12:1 mass ratio). This composite structure combines the protective cavity of cyclodextrin with the active vitamin, achieving both stability and bioavailability that neither component provides alone.
2Ease of manufacture
If 25-Hydroxy Vitamin D3 is dissolved in oil phase, then the product can be formulated, but the bioavailability is low due to poor water solubility and slow absorption
Solution Approach 1:
The invention changes the physical-chemical parameters of 25-Hydroxy Vitamin D3 by forming an inclusion complex with β-cyclodextrin. This transformation converts the oil-soluble vitamin into a water-soluble complex, fundamentally altering its solubility parameter and enabling rapid dissolution and absorption in the gastrointestinal tract while maintaining manufacturability.
3Ease of operation
If the unsaturated double bonds are exposed to air, then the vitamin D3 can be accessed by the body, but oxidation degradation occurs rapidly
Solution Approach 1:
The β-cyclodextrin molecule forms a nested structure with the 25-Hydroxy Vitamin D3 molecule inside its cavity. This nesting protects the vulnerable unsaturated double bonds from atmospheric oxygen while still allowing the complex to be recognized and absorbed by the body, effectively shielding the sensitive regions from harmful oxidation.
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 complex exhibits improved stability, bioavailability, and absorption efficiency, with minimal degradation and increased vitamin D3 levels in animal blood, outperforming existing products in thermal stability and bioefficiency tests.
Implementation Method 1
by forming a complex between 25-Hydroxy Vitamin D3 and β-cyclodextrin, each 25-Hydroxy Vitamin D3 molecule was enclosed into β-cyclodextrin's cavity
Implementation Method 2
Adding β-cyclodextrin into deionized (DI) water, heating it to 45∼65 °C while stirring, until dissolved
Implementation Method 3
Dissolving the 25-Hydroxy Vitamin D3 crystals into an ethanol solution, stirring until dissolved
Implementation Method 4
Taking the solution from step 2, adding it into the solution from step 1, slowly and keeping stirring while adding, forming white particles which precipitate out of the solution
Data Source
AI summary
This invention provides a 25-OH Vitamin D3 complex, this complex is made of β-cycledextrin and/or its derivatives and 25-Hydroxy Vitamin D3. This invention also relates to a method of manufacturing this complex of β-cycledextrin and 25-Hydroxy Vitamin D3, as well as its applications. Due to there being many hydroxy groups at the outside of β-cycledextrin and/or its derivatives, the complex increases the solubility of entrapped 25-HO Vitamin D3, thus increasing its bioavailability greatly. In addition, the ring structure of β-cycledextrin protects the unstable unsaturated double bonds of 25-HO Vitamin D3, shield it from oxygen and other harmful chemicals and make it much more stable.