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An Eudragit‐coated prednisolone preparation for ulcerative colitis: pharmacokinetics and preliminary therapeutic use
Author(s) -
FORD G. A.,
OLIVER P. S.,
SHEPHERD N. A.,
WILKINSON S. P.
Publication year - 1992
Publication title -
alimentary pharmacology and therapeutics
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 3.308
H-Index - 177
eISSN - 1365-2036
pISSN - 0269-2813
DOI - 10.1111/j.1365-2036.1992.tb00542.x
Subject(s) - medicine , ulcerative colitis , pharmacokinetics , prednisolone , pharmacology , colitis , disease
SUMMARY Prednisolone metasulphabenzoate, a steroid with poor colonic absorption, was coated with the pH‐dependent acrylic resin Eudragit S, as a means of delivering an orally administered preparation to the proximal colon. The therapeutic potential of delivering this steroid with potentially less systemic side‐effects to the proximal colon was assessed in extensive ulcerative colitis. Plasma and urine prednisolone profiles in 6 healthy volunteers confirmed minimal absorption from Eudragit S‐coated prednisolone metasulphabenzoate compared to prednisolone acetate: peak plasma prednisolone concentrations 29 ± 21 ng/ml vs. 570 ± 185 ng/ml ( P < 0.01), area under curve measurements 204 ± 214 vs. 2724 ± 1236 ng.h/ml ( P < 0.01). Prednisolone metasulphabenzoate coated with Eudragit S (30–60 mg daily) was then administered for 12 weeks to 12 patients with colonoscopically proven extensive ulcerative colitis in relapse. Symptoms, sigmoidoscopic appearances and rectal histological abnormalities all improved during therapy. Complete clinical remission occurred in 7 patients, a partial response in 2 patients and no response in 3 patients. Cortisol responses to tetracosactrin demonstrated no significant adrenal suppression following treatment. Eudragit S‐coated prednisolone metasulphabenzoate may be a useful treatment for extensive ulcerative colitis, without risk of systemic steroid side‐effects.