Moxifloxacin penetration into human gastrointestinal tissues.
OBJECTIVE
Moxifloxacin is a recently developed fourth-generation methoxyquinolone with a broad spectrum of activity against both Gram-positive and Gram-negative aerobic bacteria and anaerobes. The aim of the present study was to assess the penetration of moxifloxacin into gastrointestinal (GI) mucosal tissues to evaluate its potential role as an antimicrobial drug in bacterial infections of the GI tract.


METHODS
Twenty-eight patients undergoing GI-tract surgery received 400 mg of moxifloxacin twice pre-operatively [eight patients orally (po) and 20 patients intravenously (iv)], of whom 22 completed the study. Mucosal tissues (three stomach, three small bowel and 16 colon) and serum samples were collected and moxifloxacin concentrations were measured by HPLC.


RESULTS
The highest tissue concentrations were detected in the mucosa of the stomach (10.9 +/- 5.1 mg/kg), followed by colon mucosa (7.8 +/- 7.1 mg/kg after iv; 6.6 +/- 3.6 mg/kg after po) and small bowel mucosa (5.4 +/- 0.5 mg/kg). The tissue-to-serum ratio of moxifloxacin was 2.0 +/- 1.6 in the small bowel mucosa, 5.8 +/- 3.4 and 6.8 +/- 3.9 in the colon mucosa after po and iv administration, respectively, and 9.7 +/- 5.7 in the stomach mucosa.


CONCLUSIONS
Moxifloxacin penetrates into and accumulates in the mucosa of the stomach, small bowel and colon. The clinical applicability of moxifloxacin administration for bacterial GI-tract infections should be investigated in controlled trials.
Wirtz
Martin
M
Department of General Surgery, University of Heidelberg, Im Neuenheimer Feld 110, D-69120 Heidelberg, Germany.
Kleeff
Jörg
J
Swoboda
Stefanie
S
Halaceli
Irfan
I
Geiss
Heiko K
HK
Hoppe-Tichy
Torsten
T
Büchler
Markus W
MW
Friess
Helmut
H
D000328:Adult; D000890:Anti-Infective Agents / Q000008:administration & dosage / Q000097:blood / Q000493:pharmacokinetics*; D001372:Aza Compounds / Q000008:administration & dosage / Q000097:blood / Q000493:pharmacokinetics*; D003106:Colon / Q000378:metabolism; D004064:Digestive System / Q000378:metabolism*; D005260:Female; D024841:Fluoroquinolones; D005753:Gastric Mucosa / Q000378:metabolism; D006801:Humans; D007275:Injections, Intravenous; D007421:Intestine, Small / Q000378:metabolism; D008297:Male; D008875:Middle Aged; D000077266:Moxifloxacin; D011804:Quinolines / Q000008:administration & dosage / Q000097:blood / Q000493:pharmacokinetics*; D013050:Spectrometry, Fluorescence
D000890:Anti-Infective Agents; D001372:Aza Compounds; D024841:Fluoroquinolones; D011804:Quinolines; D000077266:Moxifloxacin