Anhydrous Pharmaceutical Base for Anesthetic Bioavailability
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Solution Overview
Problem
Existing anesthetic compositions using lidocaine and tetracaine face challenges in bioavailability due to the use of hydrophilic bases that hinder the absorption of these anesthetic substances into deeper skin layers where nerve cells are located.
Innovation Solution
A pharmaceutical base is developed containing a solvating aprotic solvent like dimethyl sulfoxide, carbonic acid amide such as urea, animal fat with unsaturated fatty acids, propylene glycol, isopropyl alcohol, and oleic acid, which enhances the bioavailability of lidocaine and tetracaine by facilitating their absorption into the epidermal and dermal layers.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Ease of operation
If hydrophilic bases (emulsions, creams, gels) are used to formulate anesthetic compositions, then the composition can be easily applied and spread on skin, but the absorption of anesthetic substances into deeper skin layers is hindered
Solution Approach 1:
The patent changes the physical-chemical parameters of the base by using a lipophilic anhydrous system instead of hydrophilic emulsions or gels. This parameter change enables the anesthetic substances to be dissolved in the lipophilic phase and effectively absorbed into the deeper skin layers where nerve endings are located, thereby improving bioavailability while maintaining ease of application.
Solution Approach 2:
The patent employs a composite base system combining anhydrous petrolatum with specific lipophilic solvents (isopropyl myristate, isopropyl palmitate) and emulsifiers (sorbates). This composite material structure creates an optimal lipophilic environment that enhances the penetration and absorption of anesthetic substances into the skin while maintaining the desired consistency and spreadability.
2Reliability
If water-insoluble forms (lidocaine and tetracaine bases) are used in lipophilic bases, then absorption into deeper layers is improved, but the substances become soluble in the dissipative fat phase remaining on skin surface
Solution Approach 1:
The patent applies local quality by creating different micro-environments within the formulation. The anesthetic substances are dissolved in the lipophilic phase that can penetrate into the skin, while the dissipative fat phase remains on the surface. This spatial differentiation ensures that the active substances are delivered to the target site (deeper layers) rather than remaining on the surface.
Solution Approach 2:
The patent uses specific emulsifiers (monopalmitic sorbate or monostearate sorbate) as intermediaries at the interface between the lipophilic phase and the dissipative fat phase. These emulsifiers facilitate the controlled transfer of anesthetic substances from the base into the skin, reducing the amount that remains on the surface while ensuring adequate absorption.
3Stability of the object's composition
If strong adsorbing substances like carboxymethylcellulose are used to prepare cream/gel formulations, then the composition has good stability and consistency, but the adsorption properties hinder the release and absorption of active substances
Solution Approach 1:
The patent extracts or removes the strong adsorbing substances (carboxymethylcellulose, guar gum) from the formulation. By eliminating these substances that would otherwise bind and retain the anesthetic molecules, the patent ensures that the active substances remain available for release and absorption into the skin, while stability is maintained through the lipophilic base system and appropriate emulsifiers.
4Reliability
If high doses of anesthetic substances are used to ensure sufficient effect, then the anesthetic effect is maintained, but the risk of side effects and toxicity increases
Solution Approach 1:
The patent changes the delivery parameters of the anesthetic substances by using a lipophilic base system that enhances penetration and bioavailability. This parameter change in the formulation system allows for reduced dosing while maintaining the desired anesthetic effect, thereby reducing the risk of side effects and toxicity associated with high doses.
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 new composition achieves higher bioavailability of lidocaine and tetracaine, allowing for reduced doses while maintaining or increasing the anesthetic effect, and it forms a semi-solid mass with high homogeneity and low contamination levels.
Implementation Method 1
A pharmaceutical base is developed containing a solvating aprotic solvent like dimethyl sulfoxide, carbonic acid amide such as urea
Implementation Method 2
facilitating their absorption into the epidermal and dermal layers
Implementation Method 3
animal fat with unsaturated fatty acids, propylene glycol, isopropyl alcohol, and oleic acid, which enhances the bioavailability of lidocaine and tetracaine by facilitating their absorption into the epidermal and dermal layers
Data Source
AI summary
The invention relates to a pharmaceutical composition for the delivery of anaesthetic active substances. The pharmaceutical composition contains an anaesthetic active substance, an animal fat, and an anhydrous pharmaceutical ointment base. The anhydrous pharmaceutical ointment base can contain a sulfoxide, a carbonic acid amide, a dihydric alcohol, an aliphatic alcohol, and an omega-9 monounsaturated fatty acid.