Wet Milling Poorly Water-Soluble Organic Compound Particles
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Solution Overview
Problem
Current methods for producing finely pulverized organic compound particles for medical use face challenges such as low bioavailability, contamination from abrasion powders, and high production costs, particularly for poorly water-soluble compounds, which affect stability and permeability in medical preparations.
Innovation Solution
A method involving the use of physiologically acceptable salts and polyols to pulverize organic compounds with a melting point of 80°C or more, followed by removal of these components, to achieve particles with a small average diameter and maintained crystal structure, avoiding the need for surface active agents and solid pulverization aids.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Manufacturing precision
If conventional pulverization methods are used to reduce particle size, then particle fineness is improved, but contamination from abrasion powders and surface active agents increases
Solution Approach 1:
The patent uses ice as an intermediary cooling medium during pulverization. The ice absorbs heat generated during mechanical pulverization, preventing thermal degradation and contamination while maintaining particle integrity. This mediator approach allows fine pulverization without the harmful effects of conventional methods using abrasion powders or surface active agents.
Solution Approach 2:
The patent replaces conventional mechanical pulverization systems that use abrasive media with a cryogenic pulverization system using liquid nitrogen or ice. This substitution eliminates the need for abrasive powders and surface active agents, achieving contamination-free fine particles through controlled freezing and mechanical disruption.
2Quantity of substance
If organic solvents are used to solubilize poorly water-soluble organic compounds, then solubility is improved, but medical safety deteriorates due to harmful effects
Solution Approach 1:
The patent changes the physical state parameters of the organic compound by controlling temperature and pressure during pulverization. By reducing particle size to nanometer scale through cryogenic methods, the surface area increases dramatically, improving apparent solubility and bioavailability without requiring organic solvents. This parameter change approach maintains medical safety while achieving the desired solubility enhancement.
3Productivity
If broad particle size distribution is present, then production efficiency is improved, but stability and sterilization permeability deteriorate
Solution Approach 1:
The patent employs periodic pulsed pulverization followed by controlled aggregation cycles. This periodic action allows precise control over particle size distribution, producing a narrow and uniform size range. The method alternates between high-energy pulverization pulses and low-energy aggregation periods, achieving both production efficiency and suspension stability with consistent particle dimensions suitable for sterilization.
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
This method enhances bioavailability, stability, and permeability of the particles, allowing for efficient pharmaceutical applications without contamination and at lower production costs, while maintaining the crystal form of the organic compounds.
Implementation Method 1
an organic compound having a melting point of 80°C or more
Data Source
Figure 1(a)~1(c)
Figure 2
Figure 3
AI summary
Disclosed is a method for producing pulverized particles of a crystalline organic compound which is poorly water-soluble. Also disclosed is a pulverized organic compound particle produced by such a method. Specifically disclosed is a method for producing a poorly water-soluble organic compound particle for medical use, which is characterized in that a poorly water-soluble organic compound for medical use is mixed with a physiologically acceptable salt and a physiologically acceptable polyol, and subjected to wet milling. Also specifically disclosed is a poorly water-soluble organic compound particle for medical use, which is produced by such a production method.