Ketoprofen is a NSAID readily absorbed from the gastrointestinal tract and peak plasma concentrations occur about 0.5–2 h after a dose, but it causes a certain irritation in the gastrointestinal mucous membrane and possesses a bitter taste and aftertaste. The short half-life (about 2–3 h) and the low single administration dose make ketoprofen a very good candidate for the formulation of controlled release dosage forms and considerable efforts have been performed in this direction. At the same time, great attention has been devoted on the possibility to prepare ketoprofen microspheres or microcapsules in order to formulate oral gastroresistant systems, to protect the gastric mucous membrane from drug irritation or to mask its unpleasant taste. Some pharmaceutical microparticulate systems are based on the pH-depentent solubility of Eudragit® S and L, anionic copolymers of methacrylic acid and methyl methacrylate soluble respectively over pH 6 and 7. This study concerns the use of these copolymers and stearic acid to prepare modified release microcapsules containing cores of ketoprofen solubilized in different oils and mint essence.
Gastroresistant microcapsules. New approaches for colon-specific delivery of ketoprofen
BIGUCCI, FEDERICA;LUPPI, BARBARA;CERCHIARA, TERESA;ZECCHI, VITTORIO
2005
Abstract
Ketoprofen is a NSAID readily absorbed from the gastrointestinal tract and peak plasma concentrations occur about 0.5–2 h after a dose, but it causes a certain irritation in the gastrointestinal mucous membrane and possesses a bitter taste and aftertaste. The short half-life (about 2–3 h) and the low single administration dose make ketoprofen a very good candidate for the formulation of controlled release dosage forms and considerable efforts have been performed in this direction. At the same time, great attention has been devoted on the possibility to prepare ketoprofen microspheres or microcapsules in order to formulate oral gastroresistant systems, to protect the gastric mucous membrane from drug irritation or to mask its unpleasant taste. Some pharmaceutical microparticulate systems are based on the pH-depentent solubility of Eudragit® S and L, anionic copolymers of methacrylic acid and methyl methacrylate soluble respectively over pH 6 and 7. This study concerns the use of these copolymers and stearic acid to prepare modified release microcapsules containing cores of ketoprofen solubilized in different oils and mint essence.I documenti in IRIS sono protetti da copyright e tutti i diritti sono riservati, salvo diversa indicazione.
