An increasing number of compounds with high molecular weight and poor water solubility are being generated in the drug discovery process. As oral drug delivery is still the preferred mode, new methods of solubilizing these active pharmaceutical ingredients (APIs) are required. Amorphous solid dispersions have become one of the more prevalent techniques for delivery of these compounds as they enable the achievement saturation levels above their equilibrium solubility. To create these dispersions, new excipient technologies have been developed as part of the AFFINISOLTM polymer platform for utility in both spray drying and hot melt extrusion operations. This platform of materials includes both hydroxypropyl methylcellulose (HPMC) and hydroxypropyl methylcellulose acetate succinate (HPMC-AS) materials which deliver not only the desired higher level of API saturation but also in a more cost effective manner. AFFINISOLTM HPMC is a unique polymer that has been designed to have the right thermal/rheological properties to be processed in hot melt extrusion processes. At varying molecular weight levels these materials have been demonstrated to be easily extrudable and stablize APIs in their amorphous form achieving supersaturation in in-vitro dissolution studies. It can also be utilized in conventional spray dryer operations providing formulators the flexibility to cross processing platforms. To increase the productivity of spray dryer operations new high productivity AFFINISOLTM HPMC-AS materials have been developed with lower solution viscosity. This enables delivery of higher solids levels increasing the overall capacity of the unit operations while delivering equivalent levels of supersaturation.

Design of AFFINISOLTM cellulosic polymers for Inceased processing efficiency in solubilizing pharmaceutical actives

250th National Meeting (2015)

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