ISSN:
1432-1041
Keywords:
Key words Dirithromycin
;
Erythromycin; polymorphonuclear leukocytes
;
saliva
;
accumulation
Source:
Springer Online Journal Archives 1860-2000
Topics:
Chemistry and Pharmacology
,
Medicine
Notes:
Abstract Objective: In a randomized cross-over study, we assessed pharmacokinetics and intracellular concentrations in polymorphonuclear leukocytes (PMN) and saliva of erythromycin and erythromycylamine, the active metabolite of dirithromycin. Methods: Ten healthy volunteers received 1 g erythromycin b.i.d. or 500 mg dirithromycin qd for 5 days (wash out period, 35 days). Concentrations of erythromycin and erythromycylamine were measured in serum, urine, saliva, and granulocytes by bioassay and high-performance liquid chromatography (HPLC) on days 1, 3, and 5 of each study period, respectively. Results: While maximal serum concentrations (Cmax) and the area under the data (AUDtot) of erythromycin were significantly higher (Cmax 1.44 mg · l−1, AUDtot 5.66 mg · h · l−1) than those of erythromycylamine (Cmax 0.29 mg · l−1, AUDtot 1.96 mg · h · l−1), erythromycylamine had a significantly higher mean residence time (21 h) than erythromycin (5.5 h). Erythromycylamine accumulated significantly more in PMN than erythromycin;␣the accumulation factor of erythromycylamine was 100 with a maximal intracellular concentration of 13.4 mg · l−1, whereas the maximal accumulation factor of erythromycin was 4 with a maximal intracellular concentration of 6.1 mg · l−1. There were no significant differences in maximal saliva concentrations (erythromycin 0.35 mg · l−1, erythromycylamine 0.31 mg · l−1).
Type of Medium:
Electronic Resource
URL:
http://dx.doi.org/10.1007/s002280050350
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