Comparative pharmacokinetics of dirithromycin and erythromycin in normal volunteers with special regard to accumulation in polymorphonuclear leukocytes and in saliva
| Autor: | K. Wettich, B. Goetschi, Hartmut Lode, Margot Rau, Peter Koeppe, Klaus Borner, H. F. Geerdes-Fenge |
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| Rok vydání: | 1997 |
| Předmět: |
Adult
Male Saliva Dirithromycin Neutrophils Administration Oral Erythromycin Granulocyte Biology Pharmacokinetics medicine Humans Distribution (pharmacology) Pharmacology (medical) Chromatography High Pressure Liquid Active metabolite Antibacterial agent Pharmacology Cross-Over Studies General Medicine Anti-Bacterial Agents medicine.anatomical_structure Area Under Curve Immunology Female Macrolides Half-Life medicine.drug |
| Zdroj: | European Journal of Clinical Pharmacology. 53:127-133 |
| ISSN: | 1432-1041 0031-6970 |
| DOI: | 10.1007/s002280050350 |
| Popis: | 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.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.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). |
| Databáze: | OpenAIRE |
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