title: Absorption of various erythromycin esters and salts in mice after intragastric intubation.
abstract: Erythromycin base and its different salts and esters were given intragastrically to mice. Serum concentrations of erythromycin and its 2'-esters were determined by the bacterial growth inhibition method. Acetyl and propionyl erythromycin were the best absorbed 2'-esters, and differed significantly from butyryl erythromycin and erythromycin base. Erythromycin estolate yielded a larger area under the concentration curve than acistrate or stearate. Among the syrup preparations, erythromycin acistrate was significantly better absorbed than 2'-ethylsuccinyl erythromycin. Absorption of 2'-esters decreased with increasing number of esterified carbon atoms and increasing hydrophobicity and increasing log P value (the logarithm of octanol-water partition coefficient). In addition to sufficient lipophilicity, the optimum absorption of erythromycin esters seems to require a high hydrophilicity.
authors.affiliation: Department of Pharmacology and Toxicology, University of Helsinki, Finland.
authors.forename: P J
authors.initials: PJ
authors.lastname: Vainio
authors.forename: M
authors.initials: M
authors.lastname: Viluksela
authors.forename: P T
authors.initials: PT
authors.lastname: Männistö
mesh_terms: D000818:Animals; D055598:Chemical Phenomena; D002627:Chemistry, Physical; D004917:Erythromycin / Q000008:administration & dosage / Q000031:analogs & derivatives / Q000493:pharmacokinetics*; D007408:Intestinal Absorption; D007441:Intubation, Gastrointestinal; D008297:Male; D051379:Mice; D012995:Solubility
chemical_list: D004917:Erythromycin