title: Compacted Multiparticulate Systems for Colon-Specific Delivery of Ketoprofen.
abstract: Pellet-containing tablets for colon-specific drug delivery present higher targeting efficiency and lower costs when compared with monolithic tablets and pellet-filled capsules, respectively. In this study, pellets containing ketoprofen were coated with different acrylic polymers and submitted to compaction. The influence of formulation and process factors on film integrity was then evaluated. Pellets were prepared via extrusion-spheronization and coated using two acrylic polymers (Eudragit® FS 30 D and Opadry® 94 k28327, PMMA and PMA, respectively). The resulting pellets were mixed with placebo granules and compressed in a hydraulic press. Multiple regression showed that ketoprofen release from pellet-containing tablets is predominantly influenced by pellet content, hardness, friability, and disintegration time. PMA-containing tablets prepared under low compaction force or with low pellet content showed rapid disintegration (<1 min) and ketoprofen release similar to those of uncompressed coated pellets (∼30% at 360 min of experiment). On the other hand, PMMA-containing tablets showed a higher rupture level, and those prepared with higher pellet content gave rise to a non-disintegrating matrix. Coated pellets were shown to be able to target ketoprofen to the colonic region. Targeting capacity was dependent on the physicochemical characteristics of the tablets.
authors.affiliation: Laboratory of Pharmaceutical Tecnology, School of Pharmacy, Universidade Federal de Goiás (UFG), Rua 240, Setor Leste Universitário, 74 605-170, Goiânia, GO, Brazil.
authors.forename: Rodrigo Gomes
authors.initials: RG
authors.lastname: de Alencar
authors.affiliation: Laboratory of Pharmaceutical Tecnology, School of Pharmacy, Universidade Federal de Goiás (UFG), Rua 240, Setor Leste Universitário, 74 605-170, Goiânia, GO, Brazil.
authors.forename: Aline Carlos
authors.initials: AC
authors.lastname: de Oliveira
authors.affiliation: Laboratory of Pharmaceutical Tecnology, School of Pharmacy, Universidade Federal de Goiás (UFG), Rua 240, Setor Leste Universitário, 74 605-170, Goiânia, GO, Brazil.
authors.forename: Eliana Martins
authors.initials: EM
authors.lastname: Lima
authors.affiliation: Laboratory of Food, Drug and Cosmetics (LTMAC), Universidade de Brasilia (UnB), Campus Universitário Darcy Ribeiro, Asa Norte, 70 910-900, Brasília, DF, Brazil.
authors.forename: Marcílio Sérgio Soares
authors.initials: MSS
authors.lastname: da Cunha-Filho
authors.affiliation: Laboratory of Pharmaceutical Tecnology, School of Pharmacy, Universidade Federal de Goiás (UFG), Rua 240, Setor Leste Universitário, 74 605-170, Goiânia, GO, Brazil.
authors.forename: Stephânia Fleury
authors.initials: SF
authors.lastname: Taveira
authors.affiliation: Laboratory of Pharmaceutical Tecnology, School of Pharmacy, Universidade Federal de Goiás (UFG), Rua 240, Setor Leste Universitário, 74 605-170, Goiânia, GO, Brazil. ricardomarreto@ufg.br.
authors.forename: Ricardo Neves
authors.initials: RN
authors.lastname: Marreto
mesh_terms: D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000008:administration & dosage*; D003106:Colon / Q000187:drug effects*; D016503:Drug Delivery Systems; D006801:Humans; D007660:Ketoprofen / Q000008:administration & dosage* / Q000737:chemistry; D011108:Polymers / Q000737:chemistry; D013607:Tablets
chemical_list: D000894:Anti-Inflammatory Agents, Non-Steroidal; D011108:Polymers; D013607:Tablets; D007660:Ketoprofen
keywords: acrylic polymers; coated pellets; multiparticulate tablets; pellet compaction; site-specific drug delivery