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

  • Dana Hales University of Medicine and Pharmacy “Iuliu Hațieganu”; Faculty of Pharmacy; Department of Pharmaceutical Technology and Biopharmacy
  • Dan Lucian Dumitrașcu University of Medicine and Pharmacy “Iuliu Hațieganu”; Faculty of Medicine
  • Ioan Tomuță University of Medicine and Pharmacy “Iuliu Hațieganu”; Faculty of Pharmacy; Department of Pharmaceutical Technology and Biopharmacy
  • Corina Briciu University of Medicine and Pharmacy “Iuliu Hațieganu”; Faculty of Pharmacy; Department of Clinical Pharmacy
  • Dana-Maria Muntean University of Medicine and Pharmacy “Iuliu Hațieganu”; Faculty of Pharmacy; Department of Pharmaceutical Technology and Biopharmacy
  • Lucia Ruxandra Tefas University of Medicine and Pharmacy “Iuliu Hațieganu”; Faculty of Pharmacy; Department of Pharmaceutical Technology and Biopharmacy
  • Sonia Iurian University of Medicine and Pharmacy “Iuliu Hațieganu”; Faculty of Pharmacy; Department of Pharmaceutical Technology and Biopharmacy
  • Rareș Iuliu Iovanov University of Medicine and Pharmacy “Iuliu Hațieganu”; Faculty of Pharmacy; Department of Pharmaceutical Technology and Biopharmacy
  • Marcela Achim University of Medicine and Pharmacy “Iuliu Hațieganu”; Faculty of Pharmacy; Department of Pharmaceutical Technology and Biopharmacy
  • Laurian Vlase University of Medicine and Pharmacy “Iuliu Hațieganu”; Faculty of Pharmacy; Department of Pharmaceutical Technology and Biopharmacy
Keywords: Colonic delivery, Compression-coated tablets, pH-Dependent release, Time-dependent release, In vitro-in vivo comparison

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.

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Published
2017-01-01
How to Cite
Hales, D., Dumitrașcu, D., Tomuță, I., Briciu, C., Muntean, D.-M., Tefas, L., Iurian, S., Iovanov, R., Achim, M., & Vlase, L. (2017). Formulation, preparation and in vitro - in vivo evaluation of compression-coated tablets for the colonic-specific release of ketoprofen. Brazilian Journal of Pharmaceutical Sciences (Impresso), 53(4), e00266. https://doi.org/10.1590/s2175-97902017000400266
Section
Articles