Deep Eutectic Pharmaceutical Solvents for Water-Sensitive Drug Delivery
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Solution Overview
Problem
Eutectic compositions have not been widely utilized in medical applications, particularly for delivering pharmaceutical agents and other beneficial substances, and there is a need for compositions that can maintain pharmaceutical agents in a liquid state at ambient temperatures without water, especially for sensitive compounds.
Innovation Solution
Development of eutectic compositions comprising at least 20 mol% choline chloride and acetaminophen, or other hydrogen bond donor and acceptor pairs, forming a deep eutectic solvent that maintains pharmaceutical agents in a liquid state at ambient temperatures, suitable for inhalation or other administration methods.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If water is used as a solvent to deliver pharmaceutical agents, then the agents can be dissolved and transported, but water-sensitive pharmaceutical agents deteriorate or become ineffective
Solution Approach 1:
The patent uses a eutectic solvent system as an intermediary medium between the pharmaceutical agent and the administration route. This eutectic solvent acts as a protective carrier that prevents direct contact between water-sensitive drugs and water, while still enabling delivery to the target site through inhalation or other non-aqueous routes.
Solution Approach 2:
The patent changes the physical-chemical parameters of the solvent system by creating a eutectic mixture with specific composition ratios (e.g., choline chloride:acetaminophen in 1:1 molar ratio). This parameter change results in a solvent system with lowered melting point and altered solubility characteristics that protect water-sensitive pharmaceutical agents while maintaining deliverability.
2Temperature
If conventional solvents are used to maintain pharmaceutical agents in liquid state, then the agents remain stable, but the compositions require water which compromises sensitive compounds
Solution Approach 1:
The patent exploits phase transition properties of eutectic mixtures, specifically the depression of melting point, to maintain pharmaceutical agents in a liquid state at ambient temperatures without requiring water. The eutectic solvent system undergoes phase change at lower temperatures, creating a liquid medium that stabilizes temperature-sensitive drugs while avoiding water exposure.
3Object-affected harmful factors
If eutectic compositions are used to avoid water, then water-sensitive pharmaceutical agents are protected, but the compositions are not commonly used in medical applications
Solution Approach 1:
The patent performs preliminary formulation work by pre-mixing eutectic solvent systems with pharmaceutical agents in specific ratios before administration. This preliminary action ensures that the water-sensitive drugs are already protected within the eutectic matrix when delivered to the target site, eliminating the need for complex in-situ protection mechanisms.
Solution Approach 2:
The eutectic solvent system provides self-service protection for water-sensitive pharmaceutical agents through its inherent chemical properties. The eutectic mixture automatically creates a protective microenvironment around the drug molecules, preventing water interaction without requiring additional protective agents or complex delivery mechanisms.
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 eutectic compositions enable effective delivery of pharmaceutical agents and beneficial substances that are sensitive to water, allowing high concentrations of these agents to be administered without significant water exposure, enhancing delivery efficacy.
Implementation Method 1
A eutectic is generally a mixture of substances that melts or solidifies at a single temperature that is lower than the melting point of either of the constituents
Implementation Method 2
at least mol % of the eutectic comprises choline chloride and a pharmaceutical agent comprising a hydrogen bond donor
Data Source
AI summary
The present invention generally relates to eutectic compositions comprising pharmaceutical agents and other beneficial substances, and in particular, to eutectic compositions where the pharmaceutical agent and beneficial substance forms a part of the eutectic composition. In one aspect, the pharmaceutical agent and beneficial substance defines part of the eutectic composition, i.e., rather than just being present within the eutectic composition. In one set of embodiments, at least about 20 mol % of the eutectic composition may comprise a hydrogen bond donor and a hydrogen bond acceptor, for example, acetaminophen and choline chloride, respectively. However, in other embodiments, the pharmaceutical agent can be either donor or acceptor, and the other agent either donor or acceptor. Other aspects are generally directed to methods of making such compositions, methods of using such compositions, kits including such compositions, etc.