Colonic spread and serum pharmacokinetics of budesonide foam in patients with mildly to moderately active ulcerative colitis.
BACKGROUND
Local treatment with foams in patients suffering from ulcerative proctitis or proctosigmoiditis is considered a rational treatment option.


OBJECTIVE
To investigate colonic spread, safety, tolerability and acceptance of a newly developed budesonide foam formulation.


METHODS
Twelve patients (four females, eight males) with acute proctosigmoiditis or left-sided ulcerative colitis were rectally administered a single dose of [99Tcm]-labelled budesonide foam (Budenofalk; Dr Falk Pharma GmbH, Freiburg, Germany) containing 2 mg budesonide in 20 mL foam after diagnostic colonoscopy. Thereafter, the colonic spread was assessed by means of gamma-scintigraphy for 6 h. Serum samples were taken simultaneously.


RESULTS
Budesonide foam spread with a maximum between 11 and 40 cm, thus reaching the sigmoid colon in all patients. In some patients, the foam even extended into the distal third and the middle of the descending colon with maximum radioactivity at 4 h. Systemic budesonide absorption was rapid and pharmacokinetic data were comparable with published data on marketed budesonide enemas, with mean serum C(max) and AUC(0-8 h) values of 0.8 +/- 0.5 ng/mL and 3.7 +/- 1.9 ng h/mL, respectively. The new formulation was well accepted by all patients, who could retain the foam for at least 4 h.


CONCLUSIONS
In the majority of patients, budesonide foam effectively spread up to the left-sided colon and thus qualifies for the local treatment of proctosigmoiditis.
Brunner
M
M
Department of Clinical Pharmacology, Division of Clinical Pharmacokinetics, Medical University of Vienna, Vienna, Austria. martin.brunner@meduniwien.ac.at
Vogelsang
H
H
Greinwald
R
R
Kletter
K
K
Kvaternik
H
H
Schrolnberger
C
C
Eichler
H-G
HG
Brunner
H
H
Dudczak
R
R
Müller
M
M
D000285:Administration, Rectal; D000893:Anti-Inflammatory Agents / Q000008:administration & dosage / Q000493:pharmacokinetics*; D019819:Budesonide / Q000008:administration & dosage / Q000493:pharmacokinetics*; D003093:Colitis, Ulcerative / Q000000981:diagnostic imaging / Q000188:drug therapy*; D003106:Colon / Q000000981:diagnostic imaging / Q000378:metabolism*; D005260:Female; D015902:Gamma Cameras; D006801:Humans; D008297:Male; D011350:Proctocolitis / Q000188:drug therapy*; D011446:Prospective Studies; D011877:Radionuclide Imaging; D013667:Technetium
D000893:Anti-Inflammatory Agents; D019819:Budesonide; D013667:Technetium