Influence of active pharmaceutical ingredient structures on Hansen solubility parameters

In drug development, preformulation is the key step, where compatibility between active pharmaceutical ingredient (API) and excipients is the crucial parameter. To simplify this process, reliable and suitable prediction models are needed. In this case, Hansen solubility parameters (HSPs) can be used. Moreover, HSPs can also describe and characterize the surface properties of the measured substances. Precisely, the surface properties of APIs and excipients affect the compatibility of the resulting dosage form. In this work, HSPs of six selected APIs of different chemical nature were determined (tadalafil, vardenafil-hydrochloride trihydrate, mefenamic acid, bisoprolol hemi-fumarate, meloxicam and indomethacin) using inverse gas chromatography (IGC) according to Snyder and Karger adsorption model. This study aimed to investigate the influence of APIs structure on HSPs and to prove the sensitivity of this method to different chemical nature of measured substances. Our results showed the influence of selected APIs chemical nature on HSPs. These results can provide a better understanding of API behaviour during the drug development process.

Automated summary

Preformulation is a crucial step in drug development, where the compatibility between API and excipients is determined by Hansen solubility parameters (HSPs) which can also describe the surface properties of substances. In this study, the HSPs of six selected APIs with different chemical nature were determined using inverse gas chromatography (IGC), revealing the influence of API structure on HSPs and the sensitivity of the method to different chemical substances. This provides valuable insights into API behavior during drug development.