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目的 :研究肾功能障碍时氧氟沙星 (OFLX)在唾液中分布的变化规律。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。OFLX( 10mg·kg-1)静脉注射后 ,经时采血及腮腺 (Pr)、颌下腺 (M )唾液。采用HPLC法测定各样品中的OFLX浓度。结果 :肾功能障碍使大鼠OFLX血浆浓度显著增高 ,全身清除率下降约 4 0 %。肾障碍组Pr唾液中浓度明显增高 ,而M唾液中浓度与对照组之间差异无显著性。在肾功能障碍组及对照组 ,消失相的OFLX唾液中浓度及唾液 /血浆浓度比 (S/P比 ) ,在Pr唾液均比M唾液高约 2和 3倍。肾功能正常大鼠的S/P比与Pr唾液中药物浓度之间呈良好正相关。结论 :OFLX在大鼠唾液中的分布存在腺差。肾功能低下 ,导致了OFLX向Pr唾液中的移行性增大 ,但对M唾液的影响不明显。而OFLX向Pr唾液中分布的量与该唾液中药物浓度有关。
Objective: To investigate the distribution of OFLX in saliva during renal dysfunction. Methods: Rat renal dysfunction model was made by 5/6 nephrectomy. The simulated operation was used as the control. OFLX (10mg · kg-1) after intravenous injection, blood and Parotid (Pr), submandibular gland (M) saliva. The OFLX concentration in each sample was determined by HPLC. RESULTS: Renal dysfunction significantly increased plasma levels of OFLX in rats, and systemic clearance rate decreased by about 40%. The concentrations of Pr in saliva of renal failure group were significantly higher than those in control group. In the renal dysfunction group and the control group, the concentrations of OFLX in the disappeared phase and the salivary / plasma concentration ratio (S / P ratio) were both about 2 and 3 times higher in Saliva than in M Saliva. There was a positive correlation between the S / P ratio in normal renal function and the drug concentration in Pr saliva. Conclusion: The distribution of OFLX in rat saliva has poor glandularity. Renal dysfunction led to an increased migration of OFLX into Pr saliva, but its effect on M saliva was not significant. The amount of OFLX distributed to Pr saliva is related to the drug concentration in the saliva.