单剂量静脉注射的药物动力学、安全性和耐受性(ZTI-01)和在健康志愿者口服磷霉素。

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温茨E, Ellis-Grosse EJ, Rodvold KA

单剂量静脉注射的药物动力学、安全性和耐受性(ZTI-01)和在健康志愿者口服磷霉素。

Antimicrob代理Chemother。2017年8月24日,61 (9)。pii: AAC.00775-17。doi: 10.1128 / AAC.00775-17。打印2017年9月。

PubMed ID

28630194 (在PubMed

]

文摘

静脉注射的药物动力学,安全性和耐受性(注射)磷霉素钠(ZTI-01)和口服磷霉素氨丁三醇进行评估后在28个健康的成年受试者单剂量。受试者接受一个1小时输液1 g和8 g磷霉素钠盐和注入一剂口服磷霉素氨丁三醇3 g在第一阶段,随机、非盲、三交叉研究。连续血液和尿液样本收集前和给药后48 h。平均磷霉素的药代动力学参数+ / -标准差在等离子体1 g和8 g注射。分别是以下:最大间隙的药物血清(Cmax) 44.3 + / - 7.6和370 + / - 61.9杯/毫升;时间最大的药物浓度血清(达峰时间),1.1 + / - 0.05和1.08 + / - 0.01 h;的体积分布(V), 29.7 + / - 5.7和31.5 + / - 10.4升;间隙(CL) 8.7 + / - 1.7和7.8 + / - 1.4升/小时;肾清除率(CLR) 6.6 + / - 1.9和6.3 + / - 1.6升/小时;曲线下的面积从0到无穷大(AUC0-infinity) 120 + / - 28.5和1060 + / - 192 mug.h /毫升; and half-life (t1/2), 2.4 +/- 0.4 and 2.8 +/- 0.6 h. After oral administration, the parameters were the following: Cmax, 26.8 +/- 6.4 mug/ml; Tmax, 2.25 +/- 0.4 h; V/F, 204 +/- 70.7 liters; CL/F, 17 +/- 4.7 liters/h; CLR, 6.5 +/- 1.8 liters/h; AUC0-infinity, 191 +/- 57.6 mug . h/ml; and t1/2, 9.04 +/- 4.5 h. The percent relative bioavailability of orally administered fosfomycin was 52.8% in relation to the 1-g i.v. dose. Approximately 74% and 80% of the 1-g and 8-g i.v. doses were excreted unchanged in the urine by 48 h compared to 37% after oral administration, with the majority of this excretion occurring by 12 h regardless of dosage form. No new safety concerns were identified during this study. The results of this study support further investigation of i.v. fosfomycin in the target patient population, including patients with complicated urinary tract infections and pyelonephritis.

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药物

磷霉素