Karba R, Mrhar A, Kozjek F, Bremsak F
Int J Clin Pharmacol Biopharm. 1979 Dec;17(12):482-5.
Clinically used dosage regimen of nitroxoline, three times 100 mg daily, was proved to be inappropriate because the successfulness of medical treatment was rarely sufficient. Nitroxoline, used as urinary antiseptic, exhibits its antibacterial activity in concentrations higher than 6 mg/l, as demonstrated in many "in vitro" experiments. This work deals with the most appropriate nitroxoline dosage form as well as with the optimal dosage regimen design. The data were obtained by the aid of the suitable pharmacokinetic model and multiple dosing simulation on analog-hybrid computer EAI 580. From the several studied alternatives two usable dosage forms with the necessary dose and corresponding dosage interval were selected.
临床上使用的硝呋妥因给药方案为每日3次，每次100毫克，但事实证明该方案并不合适，因为治疗效果很少能达到预期。正如许多“体外”实验所表明的，硝呋妥因作为尿路抗菌剂，在浓度高于6毫克/升时才会发挥抗菌活性。这项工作涉及最合适的硝呋妥因剂型以及最佳给药方案设计。数据是借助合适的药代动力学模型以及在模拟混合计算机EAI 580上进行的多次给药模拟获得的。从几个研究方案中，选择了两种可用的剂型以及必要的剂量和相应的给药间隔。
