EFFECT OF A SINGLE ORAL DOSE OF 2 ERYTHROMYCIN ETHYLSUCCINATE FORMULATIONS ON GASTRIC-EMPTYING IN HEALTHY-VOLUNTEERS - A SCINTIGRAPHIC STUDY

Citation
F. Delatour et al., EFFECT OF A SINGLE ORAL DOSE OF 2 ERYTHROMYCIN ETHYLSUCCINATE FORMULATIONS ON GASTRIC-EMPTYING IN HEALTHY-VOLUNTEERS - A SCINTIGRAPHIC STUDY, Fundamental and clinical pharmacology, 12(3), 1998, pp. 292-297
Citations number
33
Categorie Soggetti
Pharmacology & Pharmacy
ISSN journal
07673981
Volume
12
Issue
3
Year of publication
1998
Pages
292 - 297
Database
ISI
SICI code
0767-3981(1998)12:3<292:EOASOD>2.0.ZU;2-1
Abstract
Macrolides are potential gastrokinetic agents. The purpose of this stu dy was to assess the effect of a single oral dose of two erythromycin formulations on gastric emptying of the solid and liquid phases in twe lve healthy volunteers and to seek a correlation between pharmacokinet ic parameters and changes in gastric emptying. The gastric emptying ti mes of liquids and solids were measured simultaneously by means of a s cintigraphic technique after a single oral administration of amorphous erythromycin ethylsuccinate (500 mg), crystalline erythromycin ethyls uccinate (1000 mg) or a placebo, in a double-blind crossover study in three separate weeks. Blood samples were obtained for erythromycin ass ay. The two oral formulations induced a similar acceleration of gastri c emptying. When compared to the placebo, both erythromycin preparatio ns significantly shortened the gastric transit time of solids and liqu ids (respectively 30% and 20% on average, p < 0.01). The incidence of gastrointestinal side-effects was similar with the two erythromycin fo rms and the placebo. No correlation was found between the peak serum e rythromycin concentrations and the solid or Liquid gastric half-lives. With the amorphous formulation, the area under the plasma time-concen tration curves was small and solid and liquid gastric emptying were st rongly accelerated, pointing to a direct effect on the gastrointestina l smooth muscle. (C) 1998 Elsevier, Paris.