Formulation and pharmacokinetics of colon-specific double-compression coated mini-tablets: Chronopharmaceutical delivery of ketorolac tromethamine

Formulation, preparation and in vitro - in vivo evaluation of compression-coated tablets for the colonic-specific release of ketoprofen

“…The MRT value for CR-tablets was 7.07 ± 1.35 h, which was 2.8 times longer than that for IR-tablets (2.51 ± 0.61 h). The value of MRT ratio between CR-tablets and IR-tablets was similar to the MRT ratio obtained in other studies: 2.8 for colon-specific double-compression coated mini-tablets (Vemula, 2015).…”

“…This means that the lag time corresponds to the transit time of the stomach and the small intestine and that the release of ketoprofen started in the last part of the ileum or in the colon, the majority of drug release happening in the colon. Other studies, which worked on establishing an in vitro-in vivo correlation, established the relationship between in vitro and in vivo parameters through a correlation coefficient r 2 (Vemula, 2015). However, of all the data obtained in this study, it can be observed that the developed colonic system using time-dependent and pH-dependent techniques managed to prevent release of ketoprofen in the stomach and small intestine and allowed releasing a significant amount in the colon.…”

“…Compression-coated tablets as colonic release systems are usually obtained by coating the drug cores by compression-coating (Fukui, Miyamura, Kobayashi, 2001a, 2001bFukui et al, 2001). Very few works were found to prepared colon delivery systems by doublecompression coating (Vemula, 2015) or by compressioncoating combined with film-coating (Fukui et al, 2000). The polymers in the coating layers are usually soluble or insoluble matrix-forming polymers, capable of controling drug release by matrix dissolution or erosion (Biswas et al, 2015), polysaccharides which control drug release through their enzymatic degradation by the colonic microflora (Sinha et al, 2004) or enteric polymers, which are insoluble in acidic media, but dissolve in slightly acid to neutral pH environments (Fukui et al, 2000).…”

Physical characterization of multiparticulate systems

“…Controlled-release (Almeida et al, 2011;Grassi et al, 2003;Phaechamud, Thongpin, Choncheewa, 2012;Sharma, Amin, 2013;Tran et al, 2011;Verhoeven, Vervaet, Remon, 2006);  Gastro-retentive/floating systems (Malode, Paradkar, Devarajan, 2015);  High drug loading in immediate-release systems (Cai et al, 2013);  Combination of different delivery systems (Dierickx et al, 2012;Dierickx, Remon, Vervaet, 2013);  Obtention of immediate-release systems, with a focus on masking drug flavor (Gryczke et al, 2011;Issa et al, 2012b);  Improvement in dissolution of poorly soluble drugs (Deng et al, 2012;Kalidova, Fischbach, Kleinebudde, 2012 Controlled-release (Aleksovski et al, 2015;Lopes et al, 2006;Tomuta, Leucuta, 2007);  Combination of different delivery systems (Souza, Goebel, Andreazza, 2013);  Colonic release (Vemula, 2015);  Ocular bio-adhesives (Bozdag et al, 2010;Weyenberg et al, 2003;Weyenberg et al, 2006);  Gastro-retentive/floating systems (Goole et al, 2008;Hauptstein et al, 2013;Katakam et al, 2014);  Obtention of immediate-release systems, with a focus on masking drug flavor (Eckert, Pein, Breitkreutz, 2014);…”

Desenvolvimento de sistemas multiparticulados de liberação imediata e modificada para associação de fármacos anti-hipertensivos

“…Dentre os sistemas multiparticulados, os minicomprimidos, que podem ser obtidos por processos bastante simples e com reduzida variabilidade, representam uma opção vantajosa para o desenvolvimento de formulações com diferentes cinéticas de dissolução, trazendo assim, oportunidades para o fabricante e benefícios aos pacientes (GABER; NAFEE; ABDALLAH, 2015;VEMULA, 2015).…”