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A pharmacokinetic study of sulphasalazine and two new formulations of mesalazine
Author(s) -
SWIFT G. L.,
MILLS C. M.,
RHODES J.,
EVANS B. K.,
BENNETT A.,
TAVARES I. A.
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.tb00269.x
Subject(s) - medicine , mesalazine , pharmacokinetics , sulfasalazine , pharmacology , ulcerative colitis , disease
SUMMARY We have examined the pharmacokinetics of enteric coated sulphasalazine compared with two new formulations of mesalazine. These consisted of microgranules of mesalazine coated with Eudragit S in a concentration of either 20 or 25% dry lacquer substance; these in turn were enclosed in capsules coated with Eudragit L. In‐vitro dissolution studies of coated microgranules showed that drug release was pH dependent. Studies in 7 normal volunteers showed median peak concentrations of 5‐amino‐salicylic acid and N ‐acetyl‐5‐amino‐salicylic acid occurred at about 6 hours with both microgranular preparations, compared with sulphasalazine at 15 h. The microgranule formulation coated with 20% Eudragit S gave serum levels and overall systemic absorption similar to values with sulphasalazine. This new formulation may be of value for delivering mesalazine and other therapeutic agents to the colon.