Bagger-Sjöbäck D, Lundman L, Nilsson-Ehle I
Department of Otolaryngology, Karolinska Institute, Karolinska Hosital, Stockholm, Sweden.
ORL J Otorhinolaryngol Relat Spec. 1992;54(1):5-9. doi: 10.1159/000278933.
This study was conducted in order to evaluate ototoxic potential and passage through the round window membrane of ciprofloxacin, a newly developed antimicrobial drug with an antibacterial spectrum well suited for the treatment of suppurative otitis media. Ciprofloxacin was injected intraperitoneally in 40 guinea pigs in doses ranging from 25 to 150 mg/kg body weight for 14 consecutive days. Sixteen inner ears of chinchillas were exposed to ciprofloxacin at a concentration of 0.1 mg/ml applied directly to the intact round window membrane. Despite severe deterioration of the animals injected with the highest doses, no behavioral or definite morphological evidence of inner ear or vestibular damage could be seen. Ciprofloxacin concentrations in the perilymph were determined with high-performance liquid chromatography. Direct passage of ciprofloxacin, presumably via the round window membrane, was demonstrated. After 1 h and 15 min, an arithmetic mean concentration of 0.165 micrograms/ml (95% confidence interval +/- 0.053) could be demonstrated in the perilymph. It can be concluded that ciprofloxacin has no ototoxic effect when administered systemically. Furthermore, when locally applied into the middle ear, it has the capacity to pass into the inner ear.
本研究旨在评估环丙沙星的耳毒性潜力及其透过圆窗膜的情况。环丙沙星是一种新开发的抗菌药物，其抗菌谱非常适合治疗化脓性中耳炎。将40只豚鼠连续14天腹腔注射环丙沙星，剂量范围为25至150毫克/千克体重。将16只龙猫的内耳暴露于浓度为0.1毫克/毫升的环丙沙星中，直接应用于完整的圆窗膜。尽管注射最高剂量的动物出现了严重恶化，但未观察到内耳或前庭损伤的行为学或明确的形态学证据。用高效液相色谱法测定外淋巴中环丙沙星的浓度。证实环丙沙星可能通过圆窗膜直接进入外淋巴。1小时15分钟后，外淋巴中的算术平均浓度为0.165微克/毫升（95%置信区间±0.053）。可以得出结论，环丙沙星全身给药时无耳毒性作用。此外，当局部应用于中耳时，它有进入内耳的能力。
