Tsuruta Y, Hata F, Yane K, Kashiwagi N, Fujita N, Kitaoku Y, Tanaka O, Miyahara H, Matsunaga T
Department of Otolaryngology, Nara Medical University, Japan.
Auris Nasus Larynx. 1994;21(4):232-6. doi: 10.1016/s0385-8146(12)80086-1.
The concentration of CZON was determined by HPLC in surgical patients with chronic otitis media, sinusitis, and tonsillitis. One gram of CZON was injected intravenously prior to surgery. The time course of the mean tissue CZON level was as follows: In the middle ear mucosa, 3.7 micrograms/g at 15 min, 7.2 micrograms/g at 30 min, and 2.9 micrograms/g at 1 hr (the half life: 21.3 min). In the maxillary sinus mucosa, 10.5 micrograms/g at 15 min, 11.8 micrograms/g at 30 min, and 2.8 micrograms/g at 1 hr (the half life: 17.5 min). In the tonsils, 14.9 micrograms/g at 15 min, 9.3 micrograms/g at 30 min, and 2.0 micrograms/g at 1 hr (the half life: 13.2 min). The concentration was high in the maxillary sinus mucosa and the tonsils, but was low in the middle ear mucosa. In the formers the transfer ratio reached its peak 15 to 30 min after administration, but in the latter the peak was reached 30 to 60 min after administration. The order of the transfer ratio at each region was above 25%. The tissue concentration exceeded the MIC80s of frequent isolates from these infections. CZON is considered to be a highly useful drug in the treatment of these infections.
采用高效液相色谱法测定慢性中耳炎、鼻窦炎和扁桃体炎手术患者体内的CZON浓度。手术前静脉注射1克CZON。平均组织CZON水平的时间进程如下：在中耳黏膜中，15分钟时为3.7微克/克，30分钟时为7.2微克/克，1小时时为2.9微克/克（半衰期：21.3分钟）。在上颌窦黏膜中，15分钟时为10.5微克/克，30分钟时为11.8微克/克，1小时时为2.8微克/克（半衰期：17.5分钟）。在扁桃体中，15分钟时为14.9微克/克，30分钟时为9.3微克/克，1小时时为2.0微克/克（半衰期：13.2分钟）。上颌窦黏膜和扁桃体中的浓度较高，但中耳黏膜中的浓度较低。在前两者中，给药后15至30分钟转运率达到峰值，但在后者中，给药后30至60分钟达到峰值。各区域的转运率顺序均高于25%。组织浓度超过了这些感染常见分离株的MIC80s。CZON被认为是治疗这些感染的一种非常有用的药物。
