Alternate Solid Forms for Modulating Physicochemical Properties of BCS Class Ii and IV Drug Substances

Abstract

Low solubility and dissolution rate (physicochemical properties) of BCS class newlineII and class IV active pharmaceutical ingredients (API molecules) is a biggest problem for newlineoral solid dosage forms in the market and pipeline. Approximately 70% of the pipeline newlinedrug substances (APIs) are suffering from low solubility issue. To address this kind of newlineissues many scientists have come up with alternate solid form approach. Namely, cocrystal newlineformation of API with pharmaceutically acceptable co-formers, alternate newlinepolymorph formation, pseudopolymorph (solvates/hydrates) formation, and co-amorphous newlinepreparation with pharmaceutically acceptable co-formers, complexation with newlinecyclodextrins, amorphous solid dispersions with inactive polymers, surfactant approach, newlineco-solvent approach and lipid based system formation. In our current research, we have newlineslected 4 low solubility class molecules (BCS class II and class IV) to modulate the newlinephysicochemical properties. The selected molecules are Apalutamide (BCS class II), newlineDasatinib (BCS class II), Lesinurad ((BCS class II) and (BCS class IV) respectively. By newlineadopting co-crystallization, pseudopolymorph (solvate) and amorphonization approaches newlineprepared alternate solid forms which consist of novel forms of the selected molecules newline