Self-Emulsifying Liquid Concentrate for Poorly Soluble Drug Injection
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Solution Overview
Problem
Current methods for administering poorly soluble drugs via injection face challenges such as solubility issues, high costs, complex production processes, stability problems, and adverse effects, particularly with emulsions, liposomes, micelles, and nanosuspensions, which limit their clinical application and stability.
Innovation Solution
A liquid concentrate comprising a poorly soluble drug, a composite emulsifier of phospholipid and non-phospholipid emulsifier, medium chain triglyceride as oil, and absolute ethanol as co-emulsifier, which forms a stable and transparent oily solution that can be easily diluted into an emulsion for intravenous administration, reducing the number of excipients and simplifying the preparation process.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Ease of operation
If drug-loaded emulsions are used to solubilize poorly soluble drugs for injection, then the drugs can be administered by injection, but the formulation has poor stability (layering, reduced drug content, increased impurities) and requires cold chain storage
Solution Approach 1:
The patent changes the physical state parameter of the drug from solid to liquid by converting it into a eutectic mixture with a carrier substance. This parameter change allows the drug to be formulated into a stable emulsion that can be administered by injection without requiring cold chain storage, resolving the contradiction between injectability and stability.
Solution Approach 2:
The patent uses a composite emulsion system comprising oil-in-water emulsion containing a eutectic mixture of the poorly soluble drug and a carrier substance. This composite material approach combines the benefits of eutectic mixtures (enhanced solubility and stability) with emulsion technology (injectability), thereby resolving the stability issue while maintaining ease of administration.
2Ease of operation
If existing drug-loaded emulsions are formulated to achieve injection administration, then poorly soluble drugs can be delivered, but the formula, process, equipment and formulation system have extremely high requirements that only a few manufacturers can master
Solution Approach 1:
The patent extracts the complex formulation requirements by simplifying the approach: instead of using complicated emulsion formulations with multiple components and strict process controls, the invention uses a eutectic mixture of the drug with a carrier substance. This extraction of complexity allows any manufacturer to produce stable injectable formulations without mastering sophisticated formulation technologies.
Solution Approach 2:
By changing the physical state of the drug through eutectic mixture formation, the patent eliminates the need for complex emulsion stabilization techniques, sophisticated equipment, and stringent process controls. This parameter change simplifies the entire formulation system while maintaining injectability.
3Ease of operation
If drug-loaded emulsions are prepared for injection, then poorly soluble drugs can be administered, but the cost is high due to cold chain requirements and complex manufacturing
Solution Approach 1:
The patent removes the costly cold chain requirement by extracting the instability issue through eutectic mixture formation. The resulting formulation is inherently stable at room temperature, eliminating the need for expensive cold chain infrastructure and reducing manufacturing complexity, thereby improving both reliability and cost-effectiveness while maintaining injectability.
4Ease of operation
If emulsions are formulated to achieve high drug load, then injection administration is possible, but the emulsions are not resistant to elevated temperature sterilization and freezing-thawing
Solution Approach 1:
The patent changes the physical and chemical parameters of the drug formulation by creating a eutectic mixture, which fundamentally alters the thermal behavior of the system. This parameter change makes the formulation resistant to elevated temperature sterilization and freezing-thawing cycles, thereby resolving the contradiction between injectability and temperature resistance.
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 solution provides a stable and cost-effective composition suitable for a wide range of poorly soluble drugs, ensuring excellent stability and safety, with the emulsion maintaining stability and efficacy for intravenous injection, reducing adverse effects and simplifying clinical administration.
Implementation Method 1
A liquid concentrate comprising a poorly soluble drug, a self-emulsifying carrier consisting of: (1) a composite emulsifier consisting of phospholipid and a non-phospholipid emulsifier; (2) an oil, which is medium chain triglyceride; and (3) a co-emulsifier, which is absolute ethanol
Implementation Method 2
a composite emulsifier consisting of phospholipid and a non-phospholipid emulsifier; an oil, which is medium chain triglyceride; and a co-emulsifier, which is absolute ethanol
Data Source
AI summary
A concentrate, characterized in that the concentrate contains a poorly soluble drug and a self-emulsifying carrier. The selfemulsifying carrier consists of the following substances: a composite emulsifier, which consists of phospholipid and nonphospholipid emulsifiers; an oil, which is medium chain triglyceride; and a co-emulsifier, which is anhydrous ethanol. The phospholipid is selected from soybean phospholipid, egg yolk lecithin, and a mixture thereof. The concentrate can be used to prepare an intravenous injection emulsion.