Sakai A, Iwasaki M, Suzuki T, Morishita M, Muranishi S
Department of Pharmaceutics, Kyoto College of Pharmacy.
Jpn J Antibiot. 1988 Jul;41(7):797-808.
14C-Rokitamycin (RKM) at the dose of 200 mg/kg was administered orally to fasted infant rats to study the absorption, distribution, metabolism and excretion in infant animals. The mean blood level of 14C-RKM reached its peak of 20.25 micrograms/ml in 30 minutes. The mean area under the curve was 93.23 micrograms.hr/ml. In vivo plasma protein binding rates of 14C-RKM were about 30% in both infant and adult rats. 14C-RKM was distributed at high concentrations into liver, kidney, lung, spleen, pancreas, bone marrow, submaxillary gland and some other tissues. Major metabolites detected in plasma, urine and bile were 10"-OH-RKM, leucomycin A7, leucomycin V and 14-OH-leucomycin V. In excretion studies, about 97% of the administered radioactivity was recovered in urine and feces within 144 hours. After intraduodenal administration to rats with cannulated bile ducts, 7.42% and 25.66% of the radioactivity were excreted within 24 hours in the urine and bile, respectively.
以200mg/kg的剂量给禁食的幼龄大鼠口服14C-罗他霉素（RKM），以研究其在幼龄动物体内的吸收、分布、代谢和排泄情况。14C-RKM的平均血药浓度在30分钟时达到峰值20.25微克/毫升。曲线下平均面积为93.23微克·小时/毫升。在幼龄大鼠和成年大鼠体内，14C-RKM的血浆蛋白结合率均约为30%。14C-RKM在肝脏、肾脏、肺、脾脏、胰腺、骨髓、下颌下腺和其他一些组织中高浓度分布。在血浆、尿液和胆汁中检测到的主要代谢产物为10"-OH-RKM、柱晶白霉素A7、柱晶白霉素V和14-OH-柱晶白霉素V。在排泄研究中，给药后144小时内约97%的放射性在尿液和粪便中回收。对胆管插管的大鼠进行十二指肠内给药后，24小时内尿液和胆汁中放射性排泄率分别为7.42%和25.66%。
