title: Suitability of κ-carrageenan pellets for the formulation of multiparticulate tablets with modified release.
abstract: κ-Carrageenan is a novel pelletisation aid with high formulation robustness and quick disintegration leading to fast drug release unlike the matrix-like release from non-disintegrating microcrystalline cellulose pellets. Compression of pellets into tablets is cost effective. The feasibility of formulating multiparticulate tablets with coated κ-carrageenan pellets was investigated. Pellets containing a highly soluble drug in acid, namely bisacodyl and κ-carrageenan or MCC as pelletisation aid were prepared, enteric coated with a mixture of Kollicoat(®) MAE 30 DP and Eudragit(®) NE 30 D and compressed using silicified microcrystalline cellulose as embedding powder. The effect of coating level, type of pellet core, compression force and punch configurations on drug release were studied. A sufficient coating thickness for κ-carrageenan pellets was necessary to obtain multiparticulate tablets with adequate resistance in the acid stage regardless of the compression pressure used. While κ-carrageenan pellets and their tablets released over 80% of the drug during the neutral stage only about 20-24% was released from MCC pellets and their tablets. The type of punches used (oblong or round) did not significantly influence the drug release from the prepared tablets. Moreover, sufficient prolonged release properties were obtained with κ-carrageenan pellets containing theophylline as a model drug and coated with Kollicoat(®) SR 30 D using Kollicoat(®) IR as pore former. A lower coating level and higher amount of pore former were needed in case of theophylline pellets formulated with MCC as pelletisation aid. The sustained release properties of both coated pellet formulations were maintained after compression at different compression pressures.
authors.affiliation: Institute of Pharmaceutics and Biopharmaceutics, Heinrich-Heine-University, Universitaetsstr. 1, 40225 Duesseldorf, Germany.
authors.forename: Dima
authors.initials: D
authors.lastname: Ghanam
authors.forename: Peter
authors.initials: P
authors.lastname: Kleinebudde
mesh_terms: D001726:Bisacodyl / Q000008:administration & dosage* / Q000737:chemistry; D002351:Carrageenan / Q000737:chemistry*; D002482:Cellulose / Q000737:chemistry; D003692:Delayed-Action Preparations; D005079:Excipients / Q000737:chemistry*; D005240:Feasibility Studies; D008689:Methacrylates / Q000737:chemistry; D011108:Polymers / Q000737:chemistry; D011109:Polymethacrylic Acids / Q000737:chemistry; D011145:Polyvinyls / Q000737:chemistry; D011312:Pressure; D012995:Solubility; D013607:Tablets; D013806:Theophylline / Q000008:administration & dosage* / Q000737:chemistry
chemical_list: D003692:Delayed-Action Preparations; C477853:Eudragit NE 30-D; D005079:Excipients; C519734:Kollicoat IR; D008689:Methacrylates; D011108:Polymers; D011109:Polymethacrylic Acids; D011145:Polyvinyls; D013607:Tablets; C117135:kollicoat MAE 30 D; D001726:Bisacodyl; C013215:polyvinyl acetate; D002351:Carrageenan; D002482:Cellulose; D013806:Theophylline; C109691:microcrystalline cellulose