Morpholino Microemulsion for Oral Substantivity
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Solution Overview
Problem
Delmopinol, used in oral formulations for gingivitis and dental plaque prevention, has high water solubility, leading to short duration of action and high required concentrations, increasing costs and reducing efficacy.
Innovation Solution
A microemulsion composition comprising a morpholino compound and its salt in a water-in-oil-in-water (L2/L1) microemulsion with a specific ratio of compound to salt, providing improved substantivity and stability, allowing longer duration of action at lower concentrations.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Duration of action of moving object
If delmopinol HCl is used in oral formulations, then it provides efficacy in preventing gingivitis and dental plaque, but it is rapidly removed from oral surfaces by saliva flow resulting in short duration of action
Solution Approach 1:
The patent changes the physical-chemical parameters of delmopinol by converting it from a water-soluble hydrochloride salt form to a lipophilic free base form that can be incorporated into microemulsion droplets. This parameter change transforms the compound's solubility characteristics, allowing it to partition into the lipid phase of the microemulsion and adhere to oral surfaces, thereby extending duration of action and improving substantivity against saliva flow removal
2Reliability
If high concentration of delmopinol (0.2%) is used to achieve efficacy, then it provides sufficient therapeutic effect, but it significantly increases the cost of oral formulations
Solution Approach 1:
The patent introduces a microemulsion system as an intermediary carrier between the delmopinol compound and the oral surfaces. This microemulsion mediator enhances the compound's substantivity and retention time on oral surfaces, allowing lower concentrations of delmopinol to achieve the same therapeutic effect by maximizing the time and contact duration of the active ingredient at the site of action
3Stability of the object's composition
If delmopinol is used in conventional formulations, then it is highly soluble in water, but this high water solubility causes it to be rapidly washed away by saliva flow
Solution Approach 1:
The patent fundamentally changes the solubility parameter of delmopinol by transitioning from the water-soluble hydrochloride salt form to the lipophilic free base form. This parameter change enables the compound to partition into the lipid phase of microemulsion droplets rather than remaining in the aqueous phase, thereby protecting it from saliva flow and extending its retention time on oral surfaces
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 microemulsion composition enhances the substantivity and stability of delmopinol, allowing it to remain effective for longer periods at lower concentrations, reducing costs and improving oral health outcomes.
Implementation Method 1
a microemulsion of an L2-phase in an L1-phase of a compound of formula I, a salt of a compound of formula I and water is, surprisingly, kinetically very stable and has improved substantivity
Data Source
AI summary
An L2/L1 microemulsion composition comprising water, a compound of formula (I) wherein R1 is a straight or branched alkyl group containing 8 to 16 carbon atoms at the 2- or 3-position of the morpholino ring, and R2 is a straight or branched alkyl group containing 2 to 10 carbon atoms, substituted with a hydroxy group except in the alpha-position, and a salt of a compound of formula (I).