Penetration of moxifloxacin into rat mandibular bone and soft tissue.

OBJECTIVE: Based on its in vitro activity and spectrum of activity, the new 8-methoxyquinolone antibiotic moxifloxacin (MXF) seems suited for the antibiotic therapy of odontogenic infections. Penetration into the relevant tissue is another prerequisite for clinical efficacy. For this reason, the levels of MXF in plasma, soft tissue, and mandibular bone were determined in an animal model with Wistar rats. MATERIAL AND METHODS: Samples of 49 rats were analyzed. Tissue samples were homogenized and proteins were precipitated. The pharmacokinetic evaluation was conducted based on non-compartmental analysis. RESULTS: The concentration-time courses of tissues show a more plateau-shaped curve compared to plasma. Calculated AUC (area under the curve) ratios tissue:plasma were M. masseter:plasma = 2.64 and mandibles:plasma = 1.13. CONCLUSIONS: Administration of antibiotics is considered an important part of therapy during and/or after surgical procedures in the maxillofacial area. Because of the good penetration into bone and muscle tissues demonstrated in Wistar rats, MXF might be an option for clinical application in this indication.

Metabolites of orally active NO-independent pyrazolopyridine stimulators of soluble guanylate cyclase.

The pyrazolopyridine stimulators of soluble guanylate cyclase BAY 41-2272 and 41-8543 were oxidised in rats and dogs at their 5-pyrimidinyl-cyclopropyl and -morpholino residue. These metabolites activate the soluble guanylate cyclase, induce vasoelaxation and thereby may contribute to the in vivo activity of BAY 41-2272 and BAY 41-8543.