Investigating the Use of Hot-melt Extrusion as a Surrogate To Conventional Techniques as the Principal Manufacturing Technique for the Preparation of Lornoxicam Tablets
摘要
The use of Hot-Melt Extrusion (HME) as an alternative to conventional manufacturing techniques leveraging its reproducibility and scalability.
MethodsA blend of lornoxicam (LORX), filler, disintegrant And Poloxamer 188 was used for the preparation of the solid mixture via HME. Varying concentrations of lactose monohydrate from 10% w/w to 60% w/w as An intragranular filler were incorporated into the solid mixtures along with different levels of croscarmellose sodium as a disintegrant between 2.5% And 7.5% w/w. The extrudates were milled and further compressed into tablets. The dissolution properties of the tablets were compared with those of the Xefo product and physical mixture (PM) tablets. Furthermore, it was evaluated for tablets prepared using other intragranular fillers including mannitol or calcium hydrogen phosphate at 60% w/w with 2.5% w/w of croscarmellose sodium. Solid state characterization of LORX was conducted using Differential Scanning Calorimetry (DSC) and polarized light microscopy (PLM) techniques.
ResultsFindings indicate variations in disintegrant levels had little effect whereas the type And concentration of fillers played a pivotal role in the dissolution profiles. All lactose-based formulations exhibited dissolution profiles aligned with Xefo while optimal enhancement was at higher filler concentrations of 60%w/w. Mannitol-based formulation also demonstrated enhanced performance whereas the incorporation of calcium hydrogen phosphate significantly slowed the drug release rate. DSC and PLM analysis confirmed that the drug maintained its crystalline form throughout processing.
ConclusionResults confirm HME as a promising approach that proves its feasibility in replacing conventional methods for developing pharmaceutical products that mimic commercial products.
Graphical Abstract