LABORATORY AND CLINICAL STUDIES ON CS-807 IN THE FIELD OF ORAL SURGERY

• Published in: CHEMOTHERAPY Vol. 36; no. Supplement1; pp. 1118 - 1126
• Main Authors: MORISHIMA, TAKASHI, OOTA, YOSHIHIDE, UEMATSU, MASATAKA, SEKIGUCHI, TOKIKO, SAKAMOTO, HARUO, SASAKI, JIRO
• Format: Journal Article
• Language: English; Japanese
• Published: Japanese Society of Chemotherapy 1988; 公益社団法人 日本化学療法学会
• ISSN: 0009-3165; 1884-5894
• DOI: 10.11250/chemotherapy1953.36.Supplement1_1118

We carried out basic and clinical studies on CS-807, a new oral cephem antibiotic. 1) 20mg/kg of CS-807 was given orally to NZW rabbits to measure the distribution of CS-807 in to various tissues, and a pharmacodynamic analysis was carried out. Tmax and Cmax of the serum level of CS-807 were 0.88h and 13.8μg/ml, and the transfer to each tissue was: Tmax 0.92h and Cmax 11.0μg/ml in the tongue; Tmax 0.80h and Cmax 14.0μg/g in the gingiva; Tmax 0.76h and Cmax 12.2μg/g in the parotid gland; Tmax 0.72h and Cmax 7.38μg/g in the submandibular gland; Tmax 0.51h and Cmax 7.38μg/g in the cervical lymph node ; and Tmax 1.09h and Cmax 3.20μg/g in the mandibula. 2) 200mg of CS-807 was administered to 11 healthy volunteers to compare the serum level of CS-807 between fasting and non-fasting administration. With the former, the peak level appeared within 2h in 6 subjects and within 3h in 5 subjects, the mean of the serum peaks being 2.86μg/ml. After meals, the peak appeared within 3h in most cases, the mean being 2.56μg/ml. Four subjects had a higher peak with nonfasting than with fasting administration. Two subjects showed approximately the same mode of transfer. Some subjects had better serum transfer with postprandial than with fasting administration. 3) To examine blood concentration at the wound site after exodontia, 200mg of CS-807 was given to 131 subjects and the blood after extraction was sampled for measurement. Considerable individual difference was observed, when the target was set at 0.39μg/ml, however, 90% of the cases showed levels exceeding the traget level. 4) The result of administering CS-807 to 18 cases of odontogenic infection was an efficacy rate of 94.4%. Mild diarrhea was observed in one case, but no severe adverse effect was seen, or abnormal clinical test value observed. We thus consider CS-807 to be an antimicrobial useful against bacterial infection in the oro-facial field.