Thorsteinsson S B, Bergan T, Oddsdottir S, Rohwedder R, Holm R
Chemotherapy. 1986;32(5):408-17. doi: 10.1159/000238444.
Ciprofloxacin is one of the newer 4-quinolones. It combines a high antibacterial activity and a broad spectrum with favourable pharmacokinetic properties. The present study was designed to detect the influence of urinary pH and fluid consumption on crystalluria. Six healthy volunteers aged 25-41 years, 3 of each sex, participated in the study. Single doses of 1,000 and 500 mg of ciprofloxacin were given orally. The urinary pH was varied by giving each subject three different diets: a regular diet, a diet supplemented by ammonium chloride to acidify urine, and a diet supplemented by sodium bicarbonate to obtain alkaline urine. The urine volume and pH were measured and microscopically examined at 37 degrees C immediately after voiding. After the very high dose of 1,000 mg ciprofloxacin the regular diet regimen led to crystalluria in only one subject. Even with this high dose, but with the acidifying regimen, no crystals were observed in any one of the volunteers. When bicarbonate was supplemented 5 to 6 volunteers presented crystals in 22 of the 36 urine samples. 21 of the crystalluric urine samples showed a pH greater than or equal to 7.3. After the usual 500-mg dose and regular diet no crystals were observed at all; only in 3 subjects who received bicarbonate supplement crystals have been seen. In the urine of two subjects crystals emerged 'ex vivo' after some hours of storage at both 37 degrees C and room temperature; these results show the importance of sediment observation at 37 degrees C immediately after voiding to differentiate between real and 'ex vivo' crystalluria. Results of different examinations permit the conclusion that the crystals contain mostly unchanged ciprofloxacin as major component and magnesium as characteristic element. Participation of the metabolite 2 in the crystal formation cannot be excluded. No significant change was observed in blood counts and blood chemistry of any subject. Urinalysis showed no modifications except the eventual presence of the typical drug-related crystals. Hematuria never occurred.
环丙沙星是较新的4-喹诺酮类药物之一。它具有高抗菌活性、广谱抗菌性以及良好的药代动力学特性。本研究旨在检测尿液pH值和液体摄入量对结晶尿的影响。6名年龄在25至41岁之间的健康志愿者（男女各3名）参与了该研究。口服单剂量1000毫克和500毫克的环丙沙星。通过给予每位受试者三种不同饮食来改变尿液pH值：常规饮食、补充氯化铵以酸化尿液的饮食以及补充碳酸氢钠以获得碱性尿液的饮食。排尿后立即在37摄氏度下测量尿量和pH值，并进行显微镜检查。服用1000毫克环丙沙星的极高剂量后，常规饮食方案仅导致一名受试者出现结晶尿。即使是这个高剂量，但采用酸化方案时，任何一名志愿者都未观察到结晶。补充碳酸氢钠时，5至6名志愿者在36份尿液样本中的22份中出现了结晶。21份结晶尿样本的pH值大于或等于7.3。服用常规的500毫克剂量并采用常规饮食后，根本未观察到结晶；仅在3名接受碳酸氢钠补充的受试者中发现了结晶。在两名受试者的尿液中，在37摄氏度和室温下储存数小时后出现了“体外”结晶；这些结果表明排尿后立即在37摄氏度下观察沉淀物对于区分真正的和“体外”结晶尿的重要性。不同检查的结果表明，结晶主要包含未变化的环丙沙星作为主要成分，镁作为特征元素。不能排除代谢物2参与晶体形成的可能性。任何受试者的血细胞计数和血液化学均未观察到显著变化。尿液分析除了最终可能出现典型的药物相关结晶外，未显示出任何改变。从未发生血尿。
