BASIC AND CLINICAL STUDIES ON BMY-28100

• Published in: CHEMOTHERAPY Vol. 37; no. Supplement3; pp. 855 - 876
• Main Authors: TOMITA, FUMISADA, OHTA, YOSHIHIDE, SHIIKI, KAZUO, GOTO, JUN, MORIHANA, TAKEFUMI, SASAKI, JIRO, UEMATSU, MASATAKA, KANEKO, AKIHIRO, SAKAMOTO, HARUO, YAMANE, NOBUO, YAMAMOTO, TADASHI, MORISHIMA, TAKASHI
• Format: Journal Article
• Language: English; Japanese
• Published: Japanese Society of Chemotherapy 1989; 公益社団法人 日本化学療法学会
• Subjects: BMY-28100; 口腔外科領域感染症
• ISSN: 0009-3165; 1884-5894
• DOI: 10.11250/chemotherapy1953.37.Supplement3_855

We conducted basic and clinical studies on BMY-28100. 1) The distribution of BMY-28100 was measured in NZW rabbits after oral administration at a dose of 33mg/kg. On the basis of the data obtained, pharmacokinetic analysis was performed by the use of Imoto's one-compartment model. A personal computer (NEC-9801) was used in draw simulated curves. The Tmax and Cmax of serum levels of BMY-28100 were 1.11h and 3.98μg/ml and the transfer of the drug to tissue was: Tmax 1.41h and Cmax 1.88μg/g in the tongue; Tmax 2.09h and Cmax 1.84μg/g in the parotid gland; Tmax 0.92h and Cmax 2.65μg/g in the cervical lymph node; Tmax 1.17h and Cmax 0.98μg/g in the mandibule bone; Tmax 1.86h and Cmax 1.10μg/g in the submandibular gland; and Tmax 1.87h and Cmax 2.17μg/g in the gingiva. 2) To examine the blood concentration at the wound site after exodontia, 250mg of BMY-28100 was given to 122 subjects and the blood after extraction was sampled for measurement. Considerable difference was observed, but when the target was set at 0.39μg/ml, 80% of the cases showed levels exceeding the target level (0.39μg/ml). 3) The result of administering BMY-28100 to 100 patients with odontogenic infection was an efficacy rate of 81.4%. Gastrointestinal disturbance (3 cases) and headache (1) were observed in 4 cases (4%), but no severe adverse effect was seen in 96 cases. Laboratory tests revealed a slight increase in GOT and GPT in 5 cases and slightly eosinophilia in 1 case. 4) Culture of clinical samples resulted in isolation of 77 strains of causative bacteria from 56 patients. Studies on the sensitivity of those isolates showed that the MIC80 of BMY-28100 was 0.39μg/ml for Oral Streptococci and 1.56μg/ml for all isolated organisms.