Gerstner G J, Dalhoff A, Weuta H
Department for Obstetrics and Gynecology, Stockerau-Hospital.
Infection. 1988;16 Suppl 1:S24-8. doi: 10.1007/BF01650503.
In a prospective pharmacokinetic study the serum and tissue concentrations of ciprofloxacin (Bay O9867), a new carboxyquinolone antimicrobial agent were studied. 22 patients were given 300 mg ciprofloxacin i. v. before the operation (group A), and 19 patients were premedicated with 500 mg ciprofloxacin orally twice daily for three days followed by 300 mg i. v. preoperatively. Tissue samples weighing approximately 2 g were taken from the fallopian tubes, the ovaries, the fundus myometrium and the cervix. Ciprofloxacin concentrations were measured biologically by the cup plate agar diffusion method. Ciprofloxacin concentrations in serum and gynecological tissues were within the same range in both groups. Maximal serum concentrations of 6 and 4 mg/l, respectively, were recorded immediately after infusion. After 2 h serum concentrations ranged from 0.6 to 1.3 mg/l in both groups. At the same time, the tissue concentrations ranged from 0.62 to 3.3 mg/kg, indicating that tissue levels exceed corresponding serum concentrations. On average ciprofloxacin is concentrated in the extravascular space two-fold, as compared to the corresponding serum concentrations. There is no drug accumulation. The tissue concentrations obtained provide a full antibacterial coverage for gynecological infections, since the MIC for the most pathogenic bacteria is less than 1 mg/l.
在一项前瞻性药代动力学研究中，对一种新型羧基喹诺酮类抗菌剂环丙沙星（拜耳O9867）的血清和组织浓度进行了研究。22例患者在手术前静脉注射300mg环丙沙星（A组），19例患者术前三天每天口服两次500mg环丙沙星进行预处理，然后术前静脉注射300mg。从输卵管、卵巢、子宫底肌层和宫颈采集约2g的组织样本。采用杯碟琼脂扩散法生物测定环丙沙星浓度。两组血清和妇科组织中环丙沙星浓度在同一范围内。输注后立即分别记录到最大血清浓度为6mg/l和4mg/l。2小时后，两组血清浓度范围为0.6至1.3mg/l。与此同时，组织浓度范围为0.62至3.3mg/kg，表明组织水平超过相应的血清浓度。与相应血清浓度相比，环丙沙星平均在血管外间隙中的浓度高出两倍。没有药物蓄积。所获得的组织浓度为妇科感染提供了充分的抗菌覆盖，因为大多数病原菌的最低抑菌浓度小于1mg/l。
