G. Frieri et al., Rectal and colonic mesalazine concentration in ulcerative colitis: oral vs. oral plus topical treatment, ALIM PHARM, 13(11), 1999, pp. 1413-1417
Aim: To measure mucosal concentrations of mesalazine in ulcerative colitis
patients treated with oral mesalazine alone, compared to patients treated w
ith both topical and oral mesalazine.
Methods: Twenty-two patients with mild to moderate ulcerative colitis were
randomized to receive 2.4 g/day of oral mesalazine (11 patients) or 2.4 g/d
ay oral plus 4 g/day of topical mesalazine (11 patients). After 2 weeks of
treatment, endoscopic biopsies specimens were taken from the rectum and in
descending colon just distal of the splenic flexure and stored to -80 degre
es C for later assay (HPLC). Wilcoxon's rank sum test for unpaired data was
used for the statistical analysis.
Results: Mucosal levels of mesalazine in the rectum were significantly high
er in patients who received oral plus topical treatment than in those who h
ad oral treatment alone (52.1 ng/mg, range: 13.6-122.1 vs. 0.2 ng/mg, range
: 0.2-9.7, respectively; P < 0.0001). Similarly, in the descending colon, t
he mucosal concentrations of mesalazine were significantly higher in patien
ts who had oral plus topical treatment than in those receiving oral treatme
nt alone (46.6 ng/mg, range: 6-112.6 vs. 15.9 ng/mg, range: 2.3-42.4, respe
ctively; P = 0.01).
Conclusions: Topical treatment of mesalazine significantly increases mucosa
l concentrations of mesalazine up to the splenic flexure, supporting the ra
tionale to treat left-sided ulcerative colitis with topical formulations of
mesalazine.