Adapalene Cyclodextrin Complex via Supercritical CO2 Diffusion
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Solution Overview
Problem
Many new pharmaceutical molecules have low water solubility, which hinders their bioavailability, and existing methods for forming molecular complexes under pressure primarily focus on adsorption rather than improving solubility.
Innovation Solution
A method involving molecular diffusion using a dense fluid under pressure in static mode, without subsequent washing, to enhance the inclusion of active substances like Adapalene within cyclodextrins, improving solubility by promoting strong interactions between the active substance and host molecules.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Ease of manufacture
If a physical mixture of adapalene and cyclodextrins is prepared, then the preparation is simple, but the solubility of adapalene in aqueous medium remains low
Solution Approach 1:
The invention changes the physical and chemical parameters by using supercritical CO2 as a solvent and adding diffusion agents (alcohols, ketones, ethers, esters, or water) to facilitate molecular diffusion. This transforms the simple mixing process into a controlled diffusion process that creates true molecular complexes rather than physical mixtures, thereby achieving both ease of manufacture and improved solubility
Solution Approach 2:
The invention introduces supercritical CO2 as an intermediary medium and diffusion agents as mediators to facilitate the interaction between adapalene and cyclodextrins. These intermediaries enable molecular diffusion and complex formation without requiring complex equipment or multiple processing steps, resolving the contradiction between simplicity and effectiveness
2Device complexity
If molecular diffusion step is carried out without diffusion agents, then the process is simpler, but the degree of inclusion of active substance is insufficient
Solution Approach 1:
The invention applies partial action by introducing diffusion agents in controlled amounts (1-25% by weight) rather than using complex multi-step processes. This partial addition of agents is sufficient to dramatically improve the degree of inclusion without requiring excessive process complexity, achieving optimal balance between simplicity and effectiveness
3Reliability
If washing step with supercritical fluid is included, then the complexation process is more complete, but the process time and complexity increase
Solution Approach 1:
The invention extracts the washing step from the traditional process and replaces it with a direct molecular diffusion approach using supercritical CO2 with diffusion agents. This eliminates the need for a separate washing step while maintaining or improving complexation completeness, thereby reducing process time and complexity
Solution Approach 2:
The invention performs preliminary action by ensuring that the molecular diffusion step with diffusion agents directly produces complete complexation without requiring subsequent washing. The diffusion agents prepare the system in advance to achieve complete complexation in a single step, eliminating the need for additional washing steps
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 significantly increases the solubility of Adapalene in an aqueous medium, multiplying dissolution by approximately 100, and is suitable for various therapeutic applications, including dermatological conditions.
Implementation Method 1
carrying out a step of molecular diffusion by bringing a dense fluid under pressure into contact, in static mode, with the mixture obtained in step (a)
Implementation Method 2
this method makes it possible to obtain a molecular complex comprising Adapalene and cyclodextrins, the solubility of which is greatly improved
Data Source
AI summary
A method for preparing molecular complexes between Adapalene and cyclodextrins using the technology of dense fluids under pressure, especially that of CO2 is described.