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Comparative Study
. 2013 Sep 14;19(34):5665-70.
doi: 10.3748/wjg.v19.i34.5665.

5-ASA colonic mucosal concentrations resulting from different pharmaceutical formulations in ulcerative colitis

Renata D'Incà  1 , Martina Paccagnella, Romilda Cardin, Surajit Pathak, Vincenzo Baldo, Maria Cecilia Giron, Giacomo Carlo Sturniolo
Affiliations
Comparative Study

5-ASA colonic mucosal concentrations resulting from different pharmaceutical formulations in ulcerative colitis

Renata D'Incà et al. World J Gastroenterol. .

Abstract

Aim: To compare the mucosal concentrations of 5-aminosalicylic acid (5-ASA) resulting from different pharmaceutical formulations and analyse the influence of inflammation on the mucosal concentrations.

Methods: The study included 130 inflammatory bowel disease (IBD) patients receiving 5-ASA as pH-dependent-release formulations (73 patients), time-dependent-release formulations (11 patients), or pro-drugs (18 patients). In addition, 28 patients were receiving topical treatment (2-4 g/d) with pH-dependent-release formulations. Endoscopic biopsies were obtained from the sigmoid region during the colonoscopy. The 5-ASA concentrations (ng/mg) were measured in tissue homogenates using high-pressure liquid chromatography with electrochemical detection. The t test and Mann-Whitney test, when appropriate, were used for statistical analysis.

Results: Patients receiving pH-dependent-release formulations showed significantly higher mucosal concentrations of 5-ASA (51.75 ± 5.72 ng/mg) compared with patients receiving pro-drugs (33.35 ± 5.78 ng/mg, P = 0.01) or time-dependent-release formulations (38.24 ± 5.53 ng/mg, P = 0.04). Patients with endoscopic remission had significantly higher mucosal concentrations of 5-ASA than patients with active disease (60.14 ± 7.95 ng/mg vs 35.66 ± 5.68 ng/mg, P = 0.02). Similar results were obtained when we compared patients with the histological appearance of remission and patients with active histological inflammation (67.53 ± 9.22 ng/mg vs 35.53 ± 5.63 ng/mg, P < 0.001). Significantly higher mucosal concentrations of 5-ASA were detected in patients treated with both oral and topical treatments in combination compared with patients who received oral treatment with pH-dependent-release formulations alone (72.33 ± 11.23 ng/mg vs 51.75 ± 5.72 ng/mg, P = 0.03).

Conclusion: IBD patients showed significant variability in mucosal 5-ASA concentrations depending on the type of formulation, and the highest mean concentration was achieved using pH-dependent-release formulations.

Keywords: 5-aminosalicylic acid; Inflammatory bowel diseases; Mucosal concentration.

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Figures

Figure 1
Figure 1
Distribution of 5-aminosalicylic acid mucosal concentrations in the sigmoid colon in patients receiving oral 5-aminosalicylic acid either pH-dependent release formulations, time-dependent release formulations or prodrugs. 5-ASA: 5-aminosalicylic acid.
Figure 2
Figure 2
5-aminosalicylic acid mucosal concentrations in the sigmoid colon. A: In patients receiving oral 5-aminosalicylic acid (5-ASA) pH-dependent release formulations according to endoscopic and histological grading of disease; B: In patients receiving 5-ASA pH-dependent release formulations on oral plus topical treatment or oral therapy alone.
See this image and copyright information in PMC

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