A pharmacokinetic study of sulphasalazine and two new formulations of mesalazine.
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.
Department of Gastroenterology, University Hospital of Wales, Heath Park, Cardiff.
G L
GL
Swift
C M
CM
Mills
J
J
Rhodes
B K
BK
Evans
A
A
Bennett
I A
IA
Tavares
D000328:Adult; D000636:Aminosalicylic Acids / Q000097:blood / Q000493:pharmacokinetics* / Q000652:urine; D002626:Chemistry, Pharmaceutical; D003692:Delayed-Action Preparations; D006801:Humans; D008297:Male; D019804:Mesalamine; D008875:Middle Aged; D011108:Polymers; D012460:Sulfasalazine / Q000493:pharmacokinetics*; D013608:Tablets, Enteric-Coated
D000636:Aminosalicylic Acids; D003692:Delayed-Action Preparations; D011108:Polymers; D013608:Tablets, Enteric-Coated; D012460:Sulfasalazine; D019804:Mesalamine; C028836:N-acetyl-5-aminosalicylic acid