The dynamics of clindamycin-2-phosphate in vivo and its transfer to tissues

Studies were conducted on clindamycin-2-phosphate, a preparation of clindamycin CLDM developed for injection, and the following results were obtained. 1) The concentration of CLDM phosphate and lincomycin (LCM) in sera were measured in rabbits following continuous intravenous infusion of 20 mg/kg over a 60 minute period, and the results were compared in a crossover test. 2) The concentration of CLDM phosphate in the oral tissues of rabbits following continuous intravenous drip infusion of 20 mg/kg over a 60 minute period was found to be a maximum in the submaxillary gland (21.1 microgram/g), followed by the liver, submaxillary lymph nodes, sera and tongue. The concentration of LCM was found to be the highest in the submaxillary gland (20.2 microgram/g), followed by the submaxillary lymph nodes, tongue, sera and liver. 3) The metabolism of CLDM phosphate in vivo was investigated using TCL. CLDM phosphate was found to metabolize to CLDM N-demethyl CLDM in vivo. 4) The peak concentration of CLDM phosphate in human sera following intravenous drip infusion of 600 mg over a 60 minute period averaged 11.9 microgram/ml, while the average concentration of LCM in sera under identical circumstances was approximately twice that of CLDM phosphate.