Hot-melt extruded tablets

Fukuda, M., Peppas, N. A., and McGinity, J. W. (2006), Properties of sustained release hot-melt extruded tablets containing chitosan and xanthan gum, Int. J. Pharm., 310, 90-100. 

Table 2 Stability of polyethylene oxide (MW 1,000,000) in hot-melt extruded tablet formulations containing 6wt% chlorpheniramine maleate processed at different temperatures...

Eukuda, M. P eppas, N.A. McGinity, J.W. Floating hot-melt extruded tablets for gastroretentive controlled drug release system. J. Control. Release 2006,115(2), 121-129. 

Due to the unique mechanical properties of HPC, it is widely used in many applications such as extruded films, solid dispersions, and hot-melt extruded tablet formulations to name a few. 

M. Fukuda, N. A. Peppas, and J.W. McGinity, Floating hot-melt extruded tablets for gastro-retentive controlled drug rekcise system,/. Control. Release, 115 (2), 121-129,2006. 

LD. Bruce, N.H. Shah, A.W MaKck, M.H. Infeld, and J.W. McGinity, Properties of hot-melt extruded tablet formulations for the colonic delivery of 5-aminosalicylic acid, Eur J Pharm Biopharm, 59 (1), 85-97,2005. 

Figure 10.18 Peak intensity map of an HPMC-coated hot melt extruded tablet showing a wall defect beneath the surface.

The materials used in the production of hot-melt extruded dosage forms must meet the same levels of purity and safety as those used in traditional dosage forms. Most of the compounds used in the production of hot-melt extruded pharmaceuticals have been used in the production of other solid dosage forms such as tablets, pellets, and transdermals. The materials used in hot-melt extruded products must possess some degree of thermal stability in addition to acceptable physical and chemical stability. The thermal stability of each individual compound and the composite mixture should be sufficient to withstand the production process. 

Fig. 6 Influence of the granule particle size on the theophylline release properties of the tablets containing hot-melt extruded granules (n = 3). Tablets 20% extruded granules (Formula 3 25% theophylline, 2% PEG, and 73% PVAc), 79.5% Avicel PH200, and 0.5% magnesium stearate ( ) Less than 125 pm (i) 180-212 pm (a) 300 25 pm (O) 500-600 pm. (From Ref. l)...

Table 8 Release of acetaminophen from hot-melt extruded granules and tablets prepared from hot-melt extruded granules containing poly(ethylene glycol) 6000 as a thermal binder in 900ml of 50mM phosphate buffer (pH 5.8) at 37°C and a paddle speed of 50rpm...

Zhang, F. McGinity, J.W. Properties of hot-melt extruded theophylline tablets containing poly (vinyl acetate). Drug Dev. Ind. Pharm. 2000, 29 (6), 938-948. 

Andrews GP, Jones DS et al (2008) The manufacture and characterisation of hot-melt extruded enteric tablets. Eur J Pharm Biopharm 69(1) 264—273 Arkenau-Maric E, Bartholomaus J (2008) Process for the production of an abuse proofed dosage form, US 2008031197 Al, USPTO, pp 11. 

Zhu Y, Shah NH et al (2002) Influence of thermal processing on the properties of chlorpheniramine maleate tablets containing an acrylic polymer. Phaim Dev Technol 7(4) 481-489 ZhuY, Shi J et al (2005) Stimuli-responsive controlled dmg release from a hollow mesoporous silica sphere/polyelectrolyte multilayer core-shell structure. Angew Chem Int Ed 44 5083-5087 Zhu Y, Shah NH et al (2006) Controlled release of a poorly water-soluble drug from hot-melt extrudates containing acrylic polymers. Drug Dev Ind Pharm 32 569-583... 

McGinity J, Repka M. Hot melt extruded films. Drug Deliv Technol 2004 4(7) 40-47. Sood A, Ashokraj Y, Panchagnula R. Use of extrusion spenronization to develop controlled release dosage forms for diltiazem hydrochloride. Pharm Tech 2004 April 62-85. Jalal IM, Malinowski HJ, Smith WE. Tablet granulations composed of spherical-shaped particles. J Pharm Sci 1972 61 1466-1468. 

Figure 10.17 Peak intensity maps of an active, hot melt extruded (a) PVA-coated tablet and (b) HPMC-coated tablet demonstrating logo clarity differences.

Polyvinyl acetate is described in the literature as a matrix former in theophylline sustained-release tablets obtained by hot-melt extrusion [646]. In a similar way spray-dried PVAc/Povidone can be applied for the production of tablets and pellets using its excellent flowability. In this case the pulverization of polyvinyl acetate by cryogenic grinding can be avoided and the mixture of the active ingredient with the excipients are applied directly to the melt extruder. 

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