A simple blending with α-glycosylated naringin produces enhanced solubility and absorption of pranlukast hemihydrate.

The possibility of newly developed α-glycosylated naringin (Naringin-G) as a solubilizing agent was investigated against pranlukast hemihydrate (PLH), a model drug with extremely low water solubility. The physical mixtures (PMs) of PLH/Naringin-G increased the solubility of PLH compared with PLH crystals and PMs with other additives, such as α-glycosylated rutin (Rutin-G) and sodium dodecyl sulfate (SDS). Naringin-G did not decrease the surface tension, whereas SDS showed a surface-active property and critical micelle concentration. The apparent solubility of PLH increased in proportion to the concentration of Naringin-G, and similarly for SDS, indicating that constant amounts of Naringin-G molecules interacted with PLH molecules. There was no change in the Caco-2 cell viability following contact with a high concentration of Naringin-G solution (10% (w/v)). The oral absorption of PLH in a rat animal model was improved when administrated with Naringin-G. The value for the area under plasma concentration-time curve from PMs of PLH/Naringin-G was 2.2 times higher than that from PLH crystals alone. Together, these results suggested that newly synthesized Naringin-G would be a promising solubilizing agent as an alternative to surfactants.