Roxithromycin Penetration into Gingiva and Alveolar Bone of Odontoiatric Patients

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The concentrations of the new macrolide antibiotic roxithromycin in plasma, saliva, gingiva, and alveolar bone were studied in 24 odontoiatric patients treated with a first dose of 300 mg p.o. followed by three maintenance doses of 150 mg p.o., 12-hourly. Samples of blood, saliva, gingiva, and bone were collected at various time points up to 24 h after the last dosing, and the roxithromycin concentration was measured microbiologically, using Bacillus subtilis ATCC 6633 as the reference organism. Pharmacokinetic analysis was performed according to a two-compartment open model with first-order absorption. The plasma, gingiva, and alveolar bone peak concentrations were 6.12 +/- 1.94 mg/l, 6.55 +/- 2.54 mg/kg, and 5.09 +/- 1.60 mg/kg, respectively. Low levels of roxithromycin were detected in saliva (0.67 +/- 0.12 mg/l at the 3rd h). The values of the area under the concentration-time curve for plasma, gingiva, and bone were 59.47 mg/l.h, 51.88 mg/kg.h and 46.80 mg/kg.h, respectively; the half-life values were 7.52 h for plasma and 6.36 and 5.20 h for gingiva and bone, respectively. These results indicate that roxithromycin reaches high levels in periodontal tissues.

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