Selecting the most appropriate formulation excipient for manufacture of amorphous solid dispersions: a case study of lumefantrine

Abstract

This work demonstrated the importance of pre-formulation studies and proposed a generalised scheme for excipient screening in the early stage of amorphous solid dispersion(ASD) system development by profiling the excipients’ capability to solubilise, amorphisise, and stabilise the chosen active pharmaceutical ingredient (API) in an effort to rank their suitability. Lumefantrine, an antimalarial active compound with both poor solubility and permeability, was used as a model API and solvent evaporation film casting was used to prepare the candidate ASD matrices in this work.

Keywords

• amorphous solid dispersion
• polymer
• pre-formulation study
• drug enabling
• amorphous solid dispersion