Ludwig M, Jantos C A, Wolf S, Bergmann M, Failing K, Schiefer H G, Weidner W
Urologische Klinik, Justus-Liebig-Universität, Giessen, Germany.
Infection. 1997 May-Jun;25(3):178-84. doi: 10.1007/BF02113609.
The epididymal, testicular, and prostatic tissue penetration of sparfloxacin, a new quinolone, was assessed in a rat model of acute epididymitis. Seventy-two hours after injection of 0.1 ml (10(6) cfu/ml) of an Escherichia coli suspension into the right epididymis via the right ductus deferens, a single oral dose of sparfloxacin 50 mg/kg body weight was administered. One, 2, 4, 8, 12, and 24 h after administration the animals were sacrificed and the sparfloxacin concentrations and "areas under the curve" (AUC0-24) in both epididymides, both testes, the prostate gland and in the serum were measured by bioassay. The highest mean AUC0-24 was found in the prostate gland, followed by left epididymis, right epididymis, serum, right testis, and left testis (190, 79, 60, 28, 12, and 9 mg/kg x h, respectively). Though there was no statistically significant difference in the sparfloxacin concentration of both epididymides (p = 0.09), the mean AUC0-24 was significantly higher in the non-infected left epididymis (p < 0.0001). The AUC0-24 and sparfloxacin concentrations of the right infected epididymis were significantly higher than those observed in the serum (p < 0.0001). In both testes, the AUC0-24 and sparfloxacin concentrations were lower than in the serum (p < 0.0001), however, the concentration exceeded the MIC tenfold for approximately 20 h. It is concluded that the pharmacokinetic properties of sparfloxacin (good in vitro activity, high penetration into the prostate gland, testes, infected and non-infected epididymides) make this drug a recommendable choice for the initial treatment of acute epididymitis caused by E. coli.
在大鼠急性附睾炎模型中评估了新型喹诺酮类药物司帕沙星在附睾、睾丸和前列腺组织中的渗透情况。通过右侧输精管向右侧附睾注射0.1 ml(10⁶ cfu/ml)大肠杆菌悬液72小时后,给予单次口服剂量50 mg/kg体重的司帕沙星。给药后1、2、4、8、12和24小时处死动物,通过生物测定法测量双侧附睾、双侧睾丸、前列腺和血清中的司帕沙星浓度及“曲线下面积”(AUC₀ - ₂₄)。前列腺中的平均AUC₀ - ₂₄最高,其次是左侧附睾、右侧附睾、血清、右侧睾丸和左侧睾丸(分别为190、79、60、28、12和9 mg/kg·h)。尽管双侧附睾中司帕沙星浓度无统计学显著差异(p = 0.09),但未感染的左侧附睾中的平均AUC₀ - ₂₄显著更高(p < 0.0001)。右侧感染附睾的AUC₀ - ₂₄和司帕沙星浓度显著高于血清中的浓度(p < 0.0001)。在双侧睾丸中,AUC₀ - ₂₄和司帕沙星浓度均低于血清(p < 0.0001),然而,该浓度超过最低抑菌浓度十倍约达20小时。结论是,司帕沙星的药代动力学特性(体外活性良好、对前列腺、睾丸、感染和未感染附睾的高渗透性)使其成为大肠杆菌引起的急性附睾炎初始治疗的推荐选择。