环丙沙星在肾功能障碍大鼠唾液中的排泄

丁国华 直良浩司 平野荣作 岩本喜久生 猪爪信夫

中国药学杂志 ›› 2000, Vol. 35 ›› Issue (12) : 827-829.

中国药学杂志 ›› 2000, Vol. 35 ›› Issue (12) : 827-829.
临床药学

环丙沙星在肾功能障碍大鼠唾液中的排泄

  • 丁国华,直良浩司,平野荣作,岩本喜久生,猪爪信夫
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Excretion of ciprofloxacin into saliva in rats with renal failure

  • DING Guo-hua, NAORA Kohji, HIRANO Hidenari, IWAMOTO Kikuo,INOTSUME Nobuo
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摘要

目的 研究肾功能障碍时环丙沙星(CPFX)向唾液中排泄的变化规律。方法 通过5/6肾摘除术,制成大鼠肾功能障碍模型,以模拟手术为对照,CPFX(10 mg·kg〈sup〉-1〈/sup〉)静脉注射后,经时采血及腮腺、颌下腺唾液。采用HPLC测定各样品中的CPFX浓度。结果 肾功能障碍大鼠与对照组相比,CPFX血浆浓度显著增高,全身清除率降至对照组的约40%。肾功能障碍使大鼠唾液中CPFX浓度也明显升高,其唾液/血浆浓度比(S/P比)呈增大倾向。结论 肾功能障碍虽使CPFX血浆和唾液中浓度明显升高,但S/P比无显著变化,说明在肾功能低下时仍可以利用唾液对该药物进行体内动态监测。

Abstract

OBJECTIVE To study the pharmacokinetics of excretion of ciprofloxacin (CPFX) into saliva in rats with renal failure. METHODS Blood, parotid and mandibular saliva were collected from the single-step 5/6th-nephrectomized and sham-operated (control) rats after bolus iv administration of CPFX (10 mg·kg-1).The concentrations of CPFX in these samples were determined by high-performance liquid chromatography. RESULTS In the nephrectomized rats, significantly higher plasma and saliva CPFX levels were observed when compared to the control rats.Total body clearance was decreased to about 40% by the renal failure.The saliva/plasma concentration ratios (S/P ratio) in the rats with renal failure showed a tendency towards greater than those in the control group. CONCLUSION The results of this study suggested that the plasma and saliva concentrations of CPFX was significantly elevated by renal failure but the S/P ratios were no significantly difference between the rats with renal failure or with normal renal function, and it is possible to use the saliva for the therapeutic drug monitoring in patients with renal failure.

关键词

环丙沙星 / 肾功能 / 唾液 / 排泄 / 唾液/血浆浓度比

Key words

ciprofloxacin(CPFX) / renal function / saliva / excretion / saliva-to-plasma concentration ratio

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丁国华 直良浩司 平野荣作 岩本喜久生 猪爪信夫. 环丙沙星在肾功能障碍大鼠唾液中的排泄[J]. 中国药学杂志, 2000, 35(12): 827-829
DING Guo-hu;NOR Kohji;HIRNO Hidenri;IWMOTO Kikuo;INOTSUME Nouo. Excretion of ciprofloxacin into saliva in rats with renal failure[J]. Chinese Pharmaceutical Journal, 2000, 35(12): 827-829

参考文献

[1]Gasser TC,Ebert SC,Graversen PH,et al.Ciprofloxacin pharmacokinetics in patients with normal and impaired renal function[J].Antimicrob Agents Chemother,1987,31(5):709-712. [2]Naora KJ,Katagiri YH,Ichikawa NH,et al.A possible reduction in the renal clearance of ciprofloxacin by fenbufen in rats[J].J Pharm Pharmacol,1990,42(4):704-707. [3]Shiiki KZ.Penetration of new quinolones into saliva[J].Chemotherapy,1989,37(5):604-609. [4]Ding GH,Naora KJ,Nagasako SA,et al.Excretion of ofloxacin into saliva in rats with renal failure[J].J Pharmaco Exp Ther,1998,287(1):31-36. [5]Watanabe J,Nakase Y,Urasaki Y,et al.Protein binding effects on salivary excretion of phenobarbital in dogs[J].J Pharmacobiodyn,1981,4(10):968-977.

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