Alkali Metal Salt Formulation for AMPK Drug Bioavailability
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Solution Overview
Problem
There is a need to improve the bioavailability of 4-chloro-N-[2-[(4-chlorophenyl)methyl]-3-oxo-1,2,4-thiadiazol-5-yl]benzamide to enhance its effectiveness in medical treatments, particularly for conditions targeted by AMPK activation.
Innovation Solution
The use of alkali metal salts, such as sodium or potassium salts, of 4-chloro-N-[2-[(4-chlorophenyl)methyl]-3-oxo-1,2,4-thiadiazol-5-yl]benzamide, combined with milling to reduce particle size, enhances bioavailability by increasing systemic exposure.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If the free acid form of the compound is used, then the compound shows desired AMPK activation activity, but the compound has poor solubility and cannot be formulated for administration
Solution Approach 1:
The patent applies parameter changes by converting the compound from its free acid form to salt forms (such as sodium salt, potassium salt, etc.), thereby changing the chemical parameter of the compound to improve solubility while maintaining AMPK activation activity. This allows the compound to be formulated for administration.
Solution Approach 2:
The patent creates composite material forms by combining the active compound with suitable base materials to form pharmaceutical compositions. These formulations integrate the salt form of the compound with excipients and other components to achieve both solubility and desired therapeutic effect.
2Reliability
If conventional pharmaceutical formulations are used, then the formulations are stable and safe, but they cannot effectively deliver compounds with poor solubility
Solution Approach 1:
The patent changes the physical and chemical parameters of the compound by using salt forms instead of the free acid form. This parameter change enables the compound to be incorporated into conventional pharmaceutical formulations while maintaining both formulation stability and adequate solubility for effective delivery.
3Quantity of substance
If the compound is administered in high doses to overcome solubility issues, then sufficient drug delivery may be achieved, but toxicity increases
Solution Approach 1:
The patent changes the chemical parameter of the compound to its salt form, which improves solubility. This allows the administration of lower doses to achieve the same therapeutic effect, thereby reducing toxicity while maintaining adequate drug delivery.
Data Source
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AI summary
There is provided an alkali metal salt of 4-chloro-N-[2-[(4-chlorophenyl)methyl]-3-oxo-1,2,4-thiadiazol-5-yl]benzamide and formulations thereof. This salt finds particular utility in the treatment or prevention of a disorder or condition ameliorated by the activation of AMPK.