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
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.