Pharmaceutical Emulsion with Polydimethylsiloxane Stabilization
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Solution Overview
Problem
Current methods for administering active ingredients like procaine result in significant side effects and instability, limiting their frequent use due to absorption issues and local reactions, and existing emulsions fail to maintain effectiveness at lower doses while causing adverse effects.
Innovation Solution
An emulsion comprising emulsion spheres with diameters ≤3.5 µm, containing polydimethylsiloxanes, a complex emulsifier, biocompatible saline, dimethyl sulfoxide, and a chelating agent, which is produced through a specific homogenization process to enhance stability and bioavailability, allowing for a sustained release of the active ingredient.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If active ingredients are administered directly or in conventional adjuvants, then the active ingredient can be delivered to the patient, but side effects increase and stability decreases
Solution Approach 1:
The active ingredient is segmented into microscopic emulsion spheres with diameters ≤3.5 µm, where at least 99% of spheres meet this size criterion. This segmentation increases surface area for absorption while controlling distribution and reducing side effects through uniform micro-dosing.
Solution Approach 2:
A complex emulsifier system acts as an intermediary between the active ingredient and the biological system. The emulsifier comprises multiple components including aliphatic alcohols, sorbitol and/or glycerol fatty acid esters, and polysorbates, creating a stable interface that enhances bioavailability while reducing direct contact between the active ingredient and tissues that would cause side effects.
2Reliability
If higher doses of active ingredient are used to maintain effectiveness, then the therapeutic effect is maintained, but side effects increase
Solution Approach 1:
The invention changes the physical parameters of the active ingredient delivery system by creating emulsion spheres with controlled size distribution (≤3.5 µm for 99% of spheres). This parameter change in particle size and distribution enables sustained release and improved absorption efficiency, allowing lower doses to achieve the same therapeutic effect.
Solution Approach 2:
The invention uses a composite emulsion system combining polydimethylsiloxanes, complex emulsifiers, biocompatible saline, dimethyl sulfoxide, and chelating agents. This composite material structure provides sustained release capabilities and enhanced stability, maintaining effectiveness at lower dosages.
3Quantity of substance
If conventional emulsions are used to reduce dosage, then the required amount of active ingredient decreases, but the emulsion becomes unstable and loses effectiveness
Solution Approach 1:
The emulsion uses a composite emulsifier system comprising aliphatic alcohols with chain lengths C10 to C100, sorbitol and/or glycerol fatty acid esters, and polysorbates. This multi-component composite provides synergistic stabilization of the emulsion spheres, maintaining stability at reduced dosages.
Solution Approach 2:
The invention specifies precise parameter ranges for emulsifier HLB values (9 to 16) and emulsion sphere size (≤3.5 µm for 99% of spheres). These controlled parameters ensure optimal stability and sustained release properties, preventing emulsion breakdown that would occur with conventional formulations.
4Duration of action of moving object
If frequent administration is attempted to maintain therapeutic effect, then the therapeutic coverage is improved, but side effects accumulate
Solution Approach 1:
The emulsion spheres are pre-formulated with sustained release properties, creating a reservoir that gradually releases the active ingredient over time. This preliminary structuring eliminates the need for frequent re-administration, as the sustained release maintains therapeutic levels between doses, reducing cumulative side effects.
Solution Approach 2:
The emulsion provides continuous release of the active ingredient through the sustained release mechanism, maintaining constant therapeutic action over an extended period. This continuous delivery replaces intermittent high-dose administration with frequent dosing, thereby reducing side effect accumulation while maintaining therapeutic coverage.
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 emulsion significantly increases the effectiveness of the active ingredient, reduces side effects, and allows for more frequent use by improving distribution and reducing the required dosage, while maintaining stability over extended periods.
Implementation Method 1
The oil phase is stabilized in the water phase using a complex emulsifier that has an HLB value of 9 to 16
Implementation Method 2
The complex emulsifier is a combination of aliphatic alcohols essentially with the chain length C10 to C100 from sorbitol and/or glycerol fatty acid esters and from polysorbates
Implementation Method 3
dimethyl sulfoxide, which is distributed in both phases according to its solubility behavior... proves to be an ideal hydroxyl radical scavenger
Implementation Method 4
G. Roewer, Institute for Inorganic Chemistry, TU Bergakademie Freiberg, lecture on November 12, 2004 in Lostau, reported that Dimetikon, whose polymer molecules surround the dimethyl sulfoxide molecules in a spherical shape, is suitable as a radical scavenger for the methyl radicals formed by the decomposition of dimethyl sulfoxide
Implementation Method 5
The invention further relates to a process for producing an emulsion containing an active ingredient, the type of emulsion and its production resulting in an increase in the active ingredient
Data Source
AI summary
The invention relates to an emulsion for pharmaceutical use, said emulsion consisting of emulsion globules, at least 99 % of which each have a diameter that is greater than or equal to a value D99 < 3.5 ?m, calculated using laser diffractometry, and containing: an active ingredient in a proportion of between 0.001 % and 50 %; between 0.01 % and 30 % of polydimethylsiloxanes having a degree of polymerisation of n = 20 to 400; between 0.01 % and 15 % of a complex emulsifier with an HLB value of 9,16; between 45 % and 99 % of a biocompatible saline solution; between 0.01 % and 10 % of a dimethyl sulfoxide; and between 0 % and 1 % of a chelating agent.