LXR Modulator Salt Formulation Stability
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Solution Overview
Problem
There is a need for formulations of Liver X Receptor (LXR) modulators with improved stability, as existing formulations may not adequately maintain the efficacy and bioavailability of these compounds over time.
Innovation Solution
The development of a pharmaceutically acceptable salt of a specific formula, which includes a fatty acid carboxylate and various alkyl, cycloalkyl, aryl, and Het moieties, along with a lipophilic vehicle containing a lipid excipient and a surfactant, to enhance the stability and bioavailability of LXR modulators.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Stability of the object's composition
If conventional formulations of LXR modulators are used, then the compounds can be administered to treat diseases, but the stability and bioavailability of the compounds deteriorate over time
Solution Approach 1:
The patent changes the chemical parameters of the LXR modulator by forming pharmaceutically acceptable salts with specific counterions (fatty acid carboxylates, amino acid carboxylates, or nucleotide carboxylates). This parameter change improves stability and bioavailability while maintaining therapeutic activity, directly addressing the contradiction between stability and duration of action.
Solution Approach 2:
The invention creates composite molecular structures by combining LXR modulator cations with specific anionic counterions to form salt formulations. These composite materials exhibit improved stability and extended duration of action compared to the parent compounds alone, resolving the technical contradiction.
2Stability of the object's composition
If LXR modulators are formulated to improve stability, then degradation is reduced, but the complexity of formulation increases
Solution Approach 1:
The patent simplifies formulation complexity by focusing on parameter changes in the molecular structure itself—specifically, forming salts with naturally occurring counterions. This approach improves stability without requiring complex formulation systems, as the stability enhancement is achieved at the molecular level rather than through complex formulation engineering.
3Reliability
If existing formulations are used, then LXR modulators can be administered, but bioavailability is insufficient
Solution Approach 1:
The invention changes the chemical parameters of the LXR modulator by forming salts with specific counterions that enhance bioavailability. This parameter change leads to improved absorption and increased amount of active compound reaching the target, directly addressing the contradiction between reliability and quantity absorbed.
Data Source
AI summary
Formulations containing pharmaceutically active compounds with improved stability.