A Screening Study of Lubricants in Wet Powder Masses Suitable for Extrusion-Spheronization

Abstract

Fourteen different substances were evaluated for their usefulness in reducing surf ace defects , heat due to friction and energy consumption in an instrumented extruder.The materials include several common lubricants and glidants, surface active agents, humectants, polyethylene glycol and a binder in a simple binary system with high drug loading. The substances under study were evaluated at two concentrations in a matrix composed of acetaminophen, Avicel PH-101 (70:30) and water. Maximum screen temperature, peak amperage draw, surface morphology of the extrudate, resistance to 944 MESIHA AND VALLES applied force, resistance to abrasion, surface morphology of the spheres, sphericity and size analysis were determined for each substance/concentration combination. High HLB surfactants, particularly SLS, performed best at levels as low as 0.125%, keeping heat and amperage draw to a minimum and greatly reducing surface defects.

Masking of Unpleasant Gustatory Sensation by Cross-Linking of Dehydrated Paracetamol Alginate Pellets Produced by Extrusion-Spheronization

“…Friability of pellets is influenced by spheronization residence time, speed (Erkoboni, 2003), calcium cross-linking treatment time, and calcium concentration (Mukhopadhyay et al, 2005). The optimized formulation showed lower friability values than those that have been reported abundantly in the literature (Bianchini, Bruni, Gazzaniga, & Vecchio, 1992;Howard et al, 2006;Malinowski & Smith, 1975;Mesiha & Valles, 1993;O'Connor & Schwartz, 1985;Zhang, Schwartz, Schnaare, Wigent, & Sugita, 1991) and which may also be attributed to the presence of Avicel ® RC 591 having strong binding property.…”

“…Avicel ® PH 101 was used as a spheronizing aid. A mixture of purified water and polysorbate 80 (as a lubricant for extrusion) (Mesiha & Valles, 1993) (99.8:0.2) was added as the wet massing fluid (0.4 mL/g) to form wetted mass for extrusion. The wetted mass was further mixed for 1 minute and then passed through axial single screw extruder (Naomi Enterprise, Mumbai, India) equipped with 0.8-mm aperture diameter screen with L/R ratio of 1.7, where L is thickness of screen and R is radius of screen aperture (Vervaet et al, 1995).…”

Functionality of Cross-Linked Polyvinylpyrrolidone as a Spheronization Aid: A Promising Alternative to Microcrystalline Cellulose

“…The unsurpassed efficiency of MCC in extrusionYspheronization has been attributed to its high internal porosity and large surface area, enabling the moistened mass to retain a large amount of usable moisture for lubrication during extrusion (2). This moisture then plasticizes the surface of the extrudates for remodeling their shape into pellets during spheronization (3). In addition, the ability of MCC to bind together the components of the wetted powder mass is critical to its performance during extrusionYspheronization.…”

Physicomechanical Properties of Naproxen-Loaded Microparticles Prepared from Eudragit L100

“…Since its gastrointestinal intolerance is not only related to the inhibition of the prostaglandin synthesis, but also to acute local contact of the drug with the gastric mucosa (3), the development of an enteric multiparticulate drug delivery system might reduce or even avoid the mucosal irritation. This objective could be achieved by formulating naproxen-loaded enteric microparticles which offer several additional advantages including good reproducibility of transport through the GIT and minimization of local damage to the GIT mucosal membrane because of their wide distribution over a large area, compared with larger monolithic dosage forms (4,5).…”