Determination of excipient based solubility increases using the CheqSol method.

Area of Science:

• Pharmaceutical Science
• Drug Development
• Physical Chemistry

Background:

• Aqueous solubility is critical for drug-likeness, but many drug candidates exhibit poor solubility.
• Developing effective methods to enhance drug solubility is essential in pharmaceutical research.

Purpose of the Study:

• To evaluate the CheqSol method's capability in quantifying solubility enhancements of four model drugs.
• To assess the impact of non-ionic excipients (hydroxypropyl-β-cyclodextrin, poloxamers 407 and 188) on drug solubility using CheqSol.

Main Methods:

• CheqSol assays were conducted on ibuprofen, gliclazide, atenolol, and propranolol, both alone and with varying concentrations of non-ionic excipients.
• The study compared CheqSol results with standard equilibrium-based solubility techniques.

Main Results:

• The CheqSol method accurately reflected increased aqueous solubility for all four drugs in an excipient concentration-dependent manner.
• Results were consistent with existing literature, validating the CheqSol method's efficacy.
• The method demonstrated comparability to traditional equilibrium-based solubility determination techniques.

Conclusions:

• The CheqSol method is a viable tool for determining solubility increases induced by non-ionic excipients.
• Its automated nature and minimal sample requirement make it a valuable screening tool for solubility and formulation development.
• CheqSol offers more detailed physicochemical insights compared to simpler visual screening systems.