Abstract
Reports in the literature indicate that hot-melt extrusion (HME) processing techniques could alter the mechanical properties of the pharmaceutical physical blend, which may alter successful processing during tableting. The aim of this study was to evaluate whether HME processing conditions have an impact on the tabletability of Atorvastatin calcium trihydrate (ATR) in the presence of Neusilin® US2 (NUS2). ATR drug load of 25% was mixed with 75% of NUS2 and extruded using two screw configurations, screw speeds, and feed rates. Solid-state thermal analysis showed that ATR transformed to an amorphous form which led to improved solubility. ATR tabletability was affected positively by screw configuration that had no shearing and mixing force. SEM analysis indicated that a conveying screw configuration preserved the spherical nature of NUS2, thus improving ATR tabletability. This novel study demonstrates the significance of changing and monitoring the HME process parameters, which impact the materials' mechanical properties and may prevent adverse outcomes during tableting.
Keywords:
Adsorbent; Atorvastatin; Hot-melt extrusion; Neusilin US2; Tabletability.