Silicic Acid Extrudate for Stable Bioavailable Formulations
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Solution Overview
Problem
Formulating a bioavailable, solid galenic formulation of silicic acid is challenging due to the rapid conversion of orthosilicic acid into non-bioavailable gels and precipitates, especially when using stabilizing agents like choline chloride, which are hygroscopic and cause capsule deformation and leakage.
Innovation Solution
A method involving the hydrolysis of silicon compounds into orthosilicic acid or oligomers in the presence of quaternary ammonium compounds or amino acids, followed by mixing with a carrier and extrusion to form a stable silicic acid extrudate, which maintains bioavailability and prevents gel formation.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If orthosilicic acid is stabilized with quaternary ammonium compounds to improve bioavailability, then bioavailability is improved, but the stabilizing agent becomes hygroscopic and causes capsule deformation and leakage
Solution Approach 1:
The patent introduces a non-hygroscopic carrier substance as an intermediary medium to carry the hygroscopic stabilized silicic acid. This carrier acts as a buffer that prevents direct contact between the hygroscopic stabilizing agent and the capsule, thereby preventing capsule deformation while maintaining the bioavailability benefits of the stabilized silicic acid formulation.
Solution Approach 2:
The patent changes the physical state and composition parameters of the formulation by incorporating a non-hygroscopic carrier substance. This parameter change reduces the overall hygroscopicity of the formulation, allowing the capsule to maintain its structural integrity while still delivering the bioavailable stabilized silicic acid.
2Stability of the object's composition
If solid excipients are added to stabilize orthosilicic acid, then stability is improved, but polymerization or gelformation occurs and bioavailability decreases
Solution Approach 1:
The patent changes the chemical and physical parameters of the formulation by using a non-hygroscopic carrier substance with specific properties. This parameter change prevents the polymerization and gelformation that occur with traditional solid excipients, while maintaining the stability and bioavailability of the stabilized silicic acid.
Solution Approach 2:
The patent creates a composite formulation combining stabilized silicic acid with a non-hygroscopic carrier substance. This composite material approach allows the formulation to maintain stability without undergoing polymerization or gelformation, thereby preserving bioavailability.
3Stability of the object's composition
If choline chloride is used as a stabilizing agent to prevent gel formation, then gel formation is prevented, but the agent is extremely hygroscopic and attracts water causing capsule deformation
Solution Approach 1:
The patent uses a non-hygroscopic carrier substance as an intermediary that separates the hygroscopic choline chloride stabilizing agent from the capsule structure. This intermediary carrier maintains the gel-preventing benefits of choline chloride while preventing it from directly deforming the capsule through hygroscopic water attraction.
Solution Approach 2:
The patent changes the hygroscopicity parameter of the overall formulation by incorporating a non-hygroscopic carrier. This parameter change allows choline chloride to function as a gel-preventing stabilizing agent without causing capsule deformation through excessive water attraction.
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 resulting extrudate is bioavailable, stable, and suitable for various applications, including pharmaceutical and cosmetic uses, with enhanced absorption and prevention of capsule deformation, as demonstrated by comparable bioavailability to liquid forms and increased bone mineral density in osteopenia patients.
Implementation Method 1
forming of stabilized silicic acid, by hydrolyzing a silicon compound into orthosilicic acid and/or oligomers thereof
Data Source
AI summary
The invention relates to a method for the preparation of a silicic acid comprising extrudate, comprising the steps of: i) forming of stabilized silicic acid, by hydrolysing a silicon compound into orthosilicic acid and/or oligomers thereof in the presence of a stabilizing agent, which is a quaternary ammonium compound, or an amino-acid, or an amino acid source or combinations thereof; ii) mixing of the stabilized silicic acid with a carrier in an amount upto the loading capacity of the carrier for silicic acid; and iii) extruding the resulting mixture thereby forming the extrudate, to extrudates obtainable with the method, to an extrudate for use in the production of animal feed, feed supplement, human food and/or food supplement and of a pharmaceutical or cosmetic preparation, and for the treatment of infections, nails, hair, skin, teeth, collagen, connective tissue, bones, osteopenia, cell generation and degenerative (ageing) processes, and to a pharmaceutical composition comprising an extrudate.