Pemilihan Jenis Koformer dan Metode Preparasi dalam Sistem Penghantaran Sediaan Ko-Amorf

Abstract

The co-amorphous is a solid multi-component system containing the active substance and other low molecular weight molecules (coformers) that can be pharmacologically relevant active substances or excipients. The co-amorphous formulations prepared with different methods and types of coformers can significantly differentiate in the physical and dissolution profile of co-amorphous forms. The purpose of this review article is to explore deeper information about co-amorphous systems, coamorphous classification, co-amorphous characterization, and the effect of coformer types and co-amorphous preparation methods on co-amorphous formulation. This review article was prepared using a literature search through PubMed, MDPI and Science Direct by including the keywords co-amorphous, co-amorphous formulations, co-amorphous stabilizers, co-amorphous drug formulations. This review found several types of coformers can be used for co-amorphous formulation, which can be in the form of pharmacologically relevant active substances and excipients such as amino acids, carboxylic acids, tannic acids, quercetin, saccharin and nicotinamide. The co-amorphous preparation methods can be used include ball milling, cryomilling, melt quenching/quench cooling, hot-melt extrusion, solvent evaporation, spray drying, freeze-drying to technologies such as supercritical antisolvent and microwave technique. The success of co-amorphous formation is determined among others by selecting of the type of coformer which involves various properties that need to be considered, such as Tg, hydrogen bond potential, miscibility, or crystallization behavior. In addition, the properties of active substances and excipients, such as thermal stability, melting temperature and tendency of crystallization of active substances and excipients, are factors that need to be considered in the selection of co-amorphous preparation methods.