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单剂量口服环丙沙星在持续非卧床腹膜透析患者中的药代动力学

Pharmacokinetics of single-dose oral ciprofloxacin in patients undergoing chronic ambulatory peritoneal dialysis.

作者信息

Shalit I, Greenwood R B, Marks M I, Pederson J A, Frederick D L

出版信息

Antimicrob Agents Chemother. 1986 Jul;30(1):152-6. doi: 10.1128/AAC.30.1.152.

Abstract

The prevention and treatment of peritonitis in patients undergoing peritoneal dialysis is often complicated by several factors, including nephrotoxicity, requirement for hospitalization, parenteral antibiotic therapy, and infection caused by resistant microorganisms. Ciprofloxacin, a new carboxyquinolone derivative, may offer the advantages of oral administration, a broad spectrum of antibacterial activity, and safety for the management of these patients. The pharmacokinetics of ciprofloxacin in serum and peritoneal fluid of eight adult patients undergoing chronic ambulatory peritoneal dialysis (CAPD) were investigated. Each patient ingested a single 750-mg dose of ciprofloxacin, and drug concentrations were measured by high-pressure liquid chromatography in serum and peritoneal fluid for 48 h after the dose. Serum concentrations reached a mean peak of 3.6 micrograms/ml 1 to 2 h after the oral dose. The mean terminal serum half-life was 16.8 h, and the mean peritoneal fluid/serum concentration ratio was 0.64. The mean peak ciprofloxacin concentration in peritoneal fluid was 1.3 micrograms/ml, and the bioactivity of the drug in peritoneal fluid was confirmed. These data indicated that therapeutic concentrations of ciprofloxacin against bacterial pathogens commonly associated with peritonitis in CAPD patients may be achievable in the peritoneal fluid after oral administration to patients undergoing CAPD. In addition, the pharmacokinetic data provide guidelines for further clinical studies of oral ciprofloxacin in CAPD patients.

摘要

腹膜透析患者腹膜炎的防治常因多种因素而复杂化,这些因素包括肾毒性、住院需求、胃肠外抗生素治疗以及耐药微生物引起的感染。环丙沙星,一种新的羧基喹诺酮衍生物,在治疗这些患者时可能具有口服给药、抗菌谱广和安全性等优点。对8例接受持续性非卧床腹膜透析(CAPD)的成年患者血清和腹膜液中环丙沙星的药代动力学进行了研究。每位患者口服单次750毫克剂量的环丙沙星,并在给药后48小时通过高压液相色谱法测定血清和腹膜液中的药物浓度。口服给药后1至2小时血清浓度达到平均峰值3.6微克/毫升。平均终末血清半衰期为16.8小时,平均腹膜液/血清浓度比为0.64。腹膜液中环丙沙星的平均峰值浓度为1.3微克/毫升,且该药物在腹膜液中的生物活性得到证实。这些数据表明,对于接受CAPD的患者口服给药后,腹膜液中可能达到治疗浓度的环丙沙星以对抗CAPD患者腹膜炎常见相关的细菌病原体。此外,药代动力学数据为环丙沙星在CAPD患者中的进一步临床研究提供了指导。

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