title: Absorption of erythromycin acistrate and erythromycin base in the fasting and non-fasting state.
abstract: Absorption of erythromycin acistrate (EA) and two erythromycin base (EB) preparations (enterotablet A and B) taken after an overnight fast or immediately before a standard breakfast was studied in 29 healthy volunteers in three separate studies, in a cross-over, randomized design. In Study I, the absorption of a single dose (400 mg) of EA was similar in the fasting and non-fasting state. There was, however, more interindividual variation and in two subjects absorption was markedly impaired in the presence of food. Cimetidine given at two doses (400 + 800 mg) had no effect on the pharmacokinetics of erythromycin acistrate. In Study II, the effect of food on the bioavailability of the two EB preparations was studied after a single dose of 500 mg (2 x 250 mg enterocoated tablets) and after multiple dosing (2 x 250 mg tid). When given with a standard breakfast, erythromycin base was significantly better absorbed from enterotablet A than from enterotablet B, whether given as a single dose or in repeated doses. Study III followed the same design as Study II except that the tablet size of both enterotablets A and B was now 500 mg. Even in this study the absorption of enterotablet A was significantly better than that of enterotablet B. EA is adequately absorbed when taken before a meal. Cimetidine does not interfere with its elimination. Concomitant food intake produced considerably dissimilar absorption of two commercially available enterocoated EB preparations. Although at steady-state this was less prominent than after a single dose, it may have some clinical significance.
authors.affiliation: Research Unit of Neurobiology, University of Helsinki, Finland.
authors.forename: R K
authors.initials: RK
authors.lastname: Tuominen
authors.forename: P T
authors.initials: PT
authors.lastname: Männistö
authors.forename: P
authors.initials: P
authors.lastname: Pohto
authors.forename: A
authors.initials: A
authors.lastname: Solkinen
authors.forename: A
authors.initials: A
authors.lastname: Vuorela
mesh_terms: D000328:Adult; D002927:Cimetidine / Q000494:pharmacology; D004347:Drug Interactions; D004917:Erythromycin / Q000031:analogs & derivatives* / Q000493:pharmacokinetics*; D005215:Fasting; D005260:Female; D005502:Food; D006801:Humans; D007408:Intestinal Absorption / Q000187:drug effects; D008297:Male; D011897:Random Allocation; D013607:Tablets; D013608:Tablets, Enteric-Coated
chemical_list: D013607:Tablets; D013608:Tablets, Enteric-Coated; D004917:Erythromycin; D002927:Cimetidine; C056625:erythromycin 2'-acetate