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Provedor de dados:  60
País:  Brazil
Título:  Formulation, preparation and in vitro - in vivo evaluation of compression-coated tablets for the colonic-specific release of ketoprofen
Autores:  Hales,Dana
Dumitrașcu,Dan Lucian
Tomuță,Ioan
Briciu,Corina
Muntean,Dana-Maria
Tefas,Lucia Ruxandra
Iurian,Sonia
Iovanov,Rareș Iuliu
Achim,Marcela
Vlase,Laurian
Data:  2017-01-01
Ano:  2017
Palavras-chave:  Colonic delivery
Compression-coated tablets
PH-Dependent release
Time-dependent release
In vitro-in vivo comparison
Resumo:  ABSTRACT The aim of this study was to formulate and prepare compression-coated tablets for colonic release (CR-tablets), and to evaluate the bioavailability of ketoprofen following the administration of a single dose from mini-tablets with immediate release (IR-tablets) compared to CR-tablets. CR-tablets were prepared based on time-controlled hydroxypropylmethylcellulose K100M inner compression-coating and pH-sensitive Eudragit® L 30D-55 outer film-coating. The clinical bioavailability study consisted of two periods, in which two formulations were administered to 6 volunteers, according to a randomized cross-over design. The apparent cumulative absorption amount of ketoprofen was estimated by plasma profile deconvolution. CR-tablets were able to delay ketoprofen’s release. Compared to IR-tablets used as reference, for the CR-tablets the maximum plasma concentration (Cmax) was lower (4920.33±1626.71 ng/mL vs. 9549.50±2156.12 ng/mL for IR-tablets) and the time needed to reach Cmax (tmax) was 5.33±1.63 h for CR-tablets vs. 1.33±0.88 h for IR-tablets. In vitro-in vivo comparison of the apparent cumulative absorption amount of ketoprofen showed similar values for the two formulations. Therefore, the obtained pharmacokinetic parameters and the in vitro-in vivo comparison demonstrated the reliability of the developed pharmaceutical system and the fact that it is able to avoid the release of ketoprofen in the first part of the digestive tract.
Tipo:  Info:eu-repo/semantics/article
Idioma:  Inglês
Identificador:  http://www.scielo.br/scielo.php?script=sci_arttext&pid=S1984-82502017000400609
Editor:  Universidade de São Paulo, Faculdade de Ciências Farmacêuticas
Relação:  10.1590/s2175-97902017000400266
Formato:  text/html
Fonte:  Brazilian Journal of Pharmaceutical Sciences v.53 n.4 2017
Direitos:  info:eu-repo/semantics/openAccess
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