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GUT DELIVERY OF BUDESONIDE, A LOCALLY ACTIVE CORTICOSTEROID, FROM PLAIN AND CONTROLLED-RELEASE CAPSULES

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  • Sarah Krein
    GUT DELIVERY OF BUDESONIDE, A LOCALLY ACTIVE CORTICOSTEROID, FROM PLAIN AND CONTROLLED-RELEASE CAPSULES Objective To compare the pharmacokinetics and site of
    Message 1 of 1 , Jan 4, 2003
      GUT DELIVERY OF BUDESONIDE, A LOCALLY ACTIVE CORTICOSTEROID, FROM PLAIN AND
      CONTROLLED-RELEASE CAPSULES

      Objective
      To compare the pharmacokinetics and site of uptake of budesonide from a
      controlled-release formulation and a deuterium-labelled standard formulation
      given before and after a meal.
      Methods
      Six healthy volunteers were randomized into an open, crossover study. They
      received 4.5 mg controlled-release budesonide (mixed with 111In pellets to
      trace gastrointestinal transit) and 4.8 mg 2H8-budesonide simultaneously at
      each of two visits: one visit before a standardized breakfast and the other
      after breakfast. Plasma concentrations of budesonide were followed over 24 h
      The transit of the 111In pellets through the gastrointestinal tract was
      followed for 36 h. Data on the site of absorption were calculated from
      transit times and absorption curves.
      Results
      The time to peak plasma concentration was significantly increased with
      controlled-release budesonide when compared with the deuterium-labelled
      standard formulation (before breakfast, 4.5 h vs 1.8 h; after breakfast, 5.2
      h vs 2.9 h). When given after breakfast, the controlled-release formulation
      was associated with a mean residence time 1.6 h longer than that seen with
      the standard formulation. However, the areas under the plasma concentration
      curves were similar with the two formulations, regardless of when the
      treatments were given (before breakfast, 18.0 � 3.8 nmol/l vs 18.0 � 6.0
      nmol/l; after breakfast, 16.9 � 7.0 nmol/l vs 18.5 � 9.0 nmol/l). Over 60%
      of the total budesonide absorbed from controlled-release capsules was
      delivered and absorbed in the ileum and colon. The corresponding proportion
      for the standard formulation was approximately 33%.
      Conclusions
      Controlled-release budesonide effectively delivers most of the budesonide dose to the ileum and colon, the regions that are most often affected by inflammatory bowel disease. In addition, the time of food intake has little effect on the site of absorption or the bioavailability of the controlled-release formulation. Delivery to the colon and ileum was independent of whether the drug was given before or after breakfast.
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