Ding G, Naora K, Nagasako S, Hirano H, Iwamoto K
Department of Pharmacy, Shimane Medical University Hospital, 89-1 Enya-cho, Izumo, Shimane 693-8501, Japan.
J Pharmacol Exp Ther. 1998 Oct;287(1):31-6.
To clarify effects of renal failure on salivary distribution of ofloxacin (OFLX), a quinolone antibiotics, blood, parotid and mandibular saliva were collected from the single-step 5/6th-nephrectomized and sham-operated (control) rats after bolus i. v. administration of OFLX (5 mg/kg). The concentrations of OFLX in these samples were determined by high-performance liquid chromatography. Renal failure induced by the partial nephrectomy significantly elevated plasma levels and cumulative salivary excretion of OFLX when compared to control rats. Total body clearance was significantly decreased by the renal failure, although salivary clearance of the partially nephrectomized rats was about three times larger than that of the control. At the terminal phase, the saliva/plasma concentration ratios of OFLX for parotid and mandibular saliva in control rats was 0.249 +/- 0.180 and 0.136 +/- 0.024, respectively, and there was a significant difference between both salivary glands. The saliva/plasma concentration ratios in the rats with renal failure were significantly greater than those in the control group in both parotid (about 3.2 times) and mandibular (about 2.5 times) saliva. The results of this study suggest that the salivary excretion of OFLX is significantly increased by renal failure and a glandular difference in the salivary excretion of OFLX exists in both rats with normal and impaired renal function.
为阐明肾衰竭对喹诺酮类抗生素氧氟沙星（OFLX）唾液分布的影响，在单次静脉注射OFLX（5mg/kg）后，从单侧5/6肾切除大鼠和假手术（对照）大鼠中采集血液、腮腺唾液和下颌下唾液。通过高效液相色谱法测定这些样本中OFLX的浓度。与对照大鼠相比，部分肾切除诱导的肾衰竭显著提高了OFLX的血浆水平和唾液累积排泄量。肾衰竭使总体清除率显著降低，尽管部分肾切除大鼠的唾液清除率比对照大鼠约大三倍。在终末期，对照大鼠腮腺唾液和下颌下唾液中OFLX的唾液/血浆浓度比分别为0.249±0.180和0.136±0.024，且两个唾液腺之间存在显著差异。肾衰竭大鼠腮腺（约3.2倍）和下颌下（约2.5倍）唾液中的唾液/血浆浓度比均显著高于对照组。本研究结果表明，肾衰竭显著增加了OFLX的唾液排泄，且在肾功能正常和受损的大鼠中，OFLX的唾液排泄均存在腺性差异。
