Plasma and salivary concentrations of erythromycin after administration of three different formulations

Abstract

In a 6-volunteer cross-over study the pharmacokinetics of 3 erythromycin preparations were compared. A single oral dose of 500 mg of each preparation was administered at each occasion and the levels measured in timed samples of plasma and saliva. Markedly higher blood concentrations of the estolate and propionate were obtained compared to the stearate. Comparison of serum and plasma concentration of the drugs from each split sample showed no significant differences. Plasma concentrations always exceeded those in saliva but for any one preparation a similar ratio was obtained at different times. This may be useful to ascertain compliance and to measure concentration of the compounds where direct measurement in plasma is not practicable.

Comparative pharmacokinetics of macrolide antibiotics and concentrations achieved in polymorphonuclear leukocytes and saliva

“…Since ER is characterized by poor water solubility and rapid inactivation, by gastric acid, the bioavailability of this compound is unpredictable. In the literature C max values after dosing with 500 mg ER stearate have been given as 1.23 [10], 0.5 and 2.9 mg/L [19]. Concentrations of ER in PMNs exceeded those in serum, with a peak level of 6.58 mg/L 3 h after application at steady state, corresponding to an accumulation factor of 6.2.…”

“…Touminen found an accumulation factor for saliva between 0.12 and 0.20 compared with serum levels after administration of 500 mg ER acistrate [23]. In another study 0.71 mg/L ER was measured in saliva 2 h after administration of 500 mg ER propionate [10]. In contrast Stephen et al could not detect ER in saliva after administration of 2×250 mg ER estolate [11].…”

“…Antibiotics accumulated in salivary gland tissue are excreted in saliva, which is easily collected. The levels of these substances in saliva reflect concentrations in the gland tissue [10–12].…”

Erythromycin versus neomycin in the treatment of hepatic encephalopathy in cirrhosis: a randomized double-blind study

“…Hence, this drug could be used to decrease the ammonia production not only in the colon but also in the small intestine, where ammonia production can occur more rapidly than in the colon in experimental studies [13]. Erythromycin estolate seems to present some advantages over the other forms [14-16] and was already evaluated in cirrhotic patients, but only at the dosage of 500 mg QID, showing no deleterious effects [17]. Minor dosages have been used as a prokinetic drug for many years, and the risk of inducing bacterial resistance is still not proven [18].…”

Φαρμακοκινητικη Μελετη Της Συγκεντρωσεως Στο Σιελο Των Νεωτερων Χημειοθεραπευτικων Κεφοξιτινης, Κεφοταξιμης, Μοξαλακταμης Και Αζτρεοναμης

“…Οι συγκεντρώσεις των διαφόρων μορφών της ερυθρομυκίνης στα πτύελα και το σίελο έχει βρεθεί σε ασθενείς με χρόνια βρογχίτιδα καί υγιείς εθελοντές, περίπου σε επίπεδα ίσα με το 10% των αντιστοί χων επιπέδων του ορού (Henry et al 1980, Marlin et al 1980. Ο ουνδιαομός της τριμεθοπρίμης και της σουλφαμεθοξαζόλης δίνει καλές συγκεντρώσεις στο σίελο, που είναι ανάλογες με τις συγκεντρώ-οεις στο αίμα και η οχέοη πυκνότητας του σιέλου προς ,τη συγκέντρω ση πλάσματος βρέθηκε 0,087 για την σουλφαμεθοξαζόλη και 0,839 για την τριμεθοπρίμη (Sardi et al 1981).…”