抄録
In the application of a drug to clinical use, it is essential to define its pharmacokinetics. Usually, a pharmacokinetic study is performed in healthy animals in the stage of in vivo studies. In the case of antibiotics, however, it is desirable to study the transfer of the drug using an infected model. We prepared an experimental infected model in rabbits using the Satoh and Heimdahl method which we had used for several years, and orally administrered to these rabbits cefuroxime axetil : CXM-AX, a new cephalosporin antibiotic, to study tissue transfer of the drug in them with that in healthy rabbits. In this study, transfer especially into soft tissues or the oral and maxillofacial region : tongue, gingiva, submandibular gland, parotid gland and submandibular lymphonodi, and into serum were examined, and use of the drug to tissues with dental infections and subsequent symptoms was discussed.
Results
1) In the infected animal group, peaks of the drug levels in the examined tissues were attained 4-42 minutes later than that of serum level, and the peak levels in tissues were about 43-88% of that in serum. Pus level got to the peak 23 minutes later than serum level, and the peak level in pus was about 31% of that in serum. In the healthy animal group, peaks of the drug levels in various tissues appeared 4-18 minutes after that of serum level, and peak levels in tissues were about 27-71% of that in serum. High concentrations of CXM were noted in the gingiva and the submandibular gland, both in the infected and in the healthy animal group.
2) CXM levels in tissues and serum were obout 1.2-2 times higher in the infected animal group than in the healthy animal group.
3) Comparatively good transfer of CXM into pus was observed in experimental lesion, althogh it was not as good as that into serum, and T1/2 was long. The above results demonstrated in vivo that CXM-AX exerts satisfactory effects at the lesion for inflammatory disorders.
