Ionic Liquid Formulations for Low-Solubility Drug Absorption
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Solution Overview
Problem
Existing oral preparations for drugs with low solubility and/or low permeability face challenges in achieving sufficient absorbability, leading to delayed development or discontinuation, and there is a lack of effective methods to enhance their transmucosal and gastrointestinal absorption.
Innovation Solution
Development of a pharmaceutical composition comprising a drug with low solubility and/or low permeability and an ionic liquid, where the ionic liquid includes an anion ingredient such as oleic acid or isostearic acid and a cation ingredient from a cationic lipid, specifically DODAP or DODMA, to enhance transmucosal and gastrointestinal absorption.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If conventional oral preparations are used for drugs with low solubility and/or low permeability, then the preparation formulation is simple, but the absorbability is insufficient
Solution Approach 1:
The patent introduces an ionic liquid as an intermediary substance that facilitates the absorption of drugs with low solubility and/or low permeability. The ionic liquid acts as a mediator between the drug and the biological membrane, enhancing the drug's ability to cross the membrane without requiring complex formulation systems.
Solution Approach 2:
The patent modifies the physical and chemical parameters of the drug formulation by incorporating ionic liquids with specific properties (anion and cation components). This changes the solubility and permeability parameters of the drug system, enabling better absorption while maintaining formulation simplicity.
2Reliability
If absorption enhancers such as surfactants and bile salts are used, then the absorbability of low-permeability drugs is improved, but the effectiveness is insufficient and the formulation complexity increases
Solution Approach 1:
The patent changes the chemical parameters of absorption enhancers by using ionic liquids with specific anion and cation combinations. This provides superior effectiveness compared to conventional surfactants and bile salts while simplifying the formulation development process through a more systematic approach to selecting ionic liquid components.
3Reliability
If existing absorption enhancers are used for proteins such as GLP-1, then some absorption enhancement is achieved, but the effectiveness remains insufficient for low-solubility and low-permeability drugs
Solution Approach 1:
The patent fundamentally changes the parameters of absorption enhancement by introducing ionic liquids with optimized anion and cation properties. This enables significantly greater absorption enhancement magnitude compared to existing enhancers, making it effective for difficult-to-absorb drugs with low solubility and permeability.
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 absorbability of drugs with low solubility and/or low permeability is remarkably improved, allowing for the formulation of effective oral preparations and enhancing transmucosal or gastrointestinal absorption.
Implementation Method 1
the absorbability of a drug with low solubility and/or low permeability is improved as well as a transmucosal absorption enhancer and a gastrointestinal absorption enhancer for improving the absorption of a drug with low solubility and/or low permeability to the transmucosal membranes and the gastrointestinal tract
Data Source
AI summary
The present invention provides a pharmaceutical composition comprising a drug with low solubility and/or low permeability and an ionic liquid, wherein the ionic liquid is an anion ingredient and a cation ingredient, the anion ingredient is oleic acid or isostearic acid, and the cation ingredient is selected from a cationic lipid as well as a transmucosal absorption enhancer or a gastrointestinal absorption enhancer comprising an ionic liquid, wherein the ionic liquid is an anion ingredient and a cation ingredient, the anion ingredient is oleic acid or isostearic acid, and the cation ingredient is selected from a cationic lipid.