Laboratory of Medical Biochemistry and Clinical Analysis, Faculty of Pharmaceutical Sciences, Ghent University, Harelbekestraat 72, B-9000 Gent, Belgium.
J Antimicrob Chemother. 2012 Jan;67(1):226-9. doi: 10.1093/jac/dkr436. Epub 2011 Oct 10.
Roux-en-Y gastric bypass surgery is the most commonly performed procedure for the treatment of morbid obesity. This anatomical alteration may affect the absorption and consequently the bioavailability of oral drugs. This study aims to investigate the oral bioavailability of moxifloxacin in 12 healthy volunteers who underwent gastric bypass surgery.
In this randomized crossover study, each subject received two single standard doses of 400 mg of moxifloxacin orally or intravenously administered on two occasions separated by a washout period of 1 week. Serial venous blood samples were drawn up to 72 h after dosing and moxifloxacin plasma levels were measured by a validated HPLC method with fluorescence detection. [clinicaltrials.gov database (identifier: NCT01130922).]
After oral dosing, moxifloxacin plasma concentrations reached a maximum (C(max)) of 3.38 ± 1.41 mg/L after 1.75 h (0.75-4.00). After intravenous dosing, C(max) and T(max) were 4.53 ± 1.43 mg/L and 1.03 h (0.75-2.50), respectively. The mean areas under the plasma concentration time curve extrapolated to infinity (AUC(∞)) were 46.2 ± 1.4 mg · h/L after oral dosing and 52.3 ± 1.3 mg · h/L after intravenous dosing, resulting in a mean oral bioavailability of 88.32% [90% confidence interval (CI) 85.64%-91.08%].
This study confirms that exposure to moxifloxacin is equivalent for oral and intravenous administration of 400 mg dosages in healthy volunteers who underwent gastric bypass surgery. But these exposures were more than 50% higher than those described for subjects without gastric bypass. This may suggest a higher enterohepatic recirculation of moxifloxacin after gastric bypass.
Roux-en-Y 胃旁路手术是治疗病态肥胖最常用的方法。这种解剖结构的改变可能会影响口服药物的吸收，进而影响其生物利用度。本研究旨在调查 12 例接受胃旁路手术的健康志愿者中莫西沙星的口服生物利用度。
在这项随机交叉研究中，每位受试者在两次间隔 1 周的洗脱期内，两次分别接受 400mg 莫西沙星的单次标准口服或静脉给药剂量。在给药后 72 小时内采集系列静脉血样，并采用经验证的 HPLC 法（荧光检测）测定莫西沙星的血浆水平。[临床试验.gov 数据库（标识符：NCT01130922）。]
口服给药后，莫西沙星的血浆浓度在 1.75 小时后达到最大值（C(max)）3.38±1.41mg/L（0.75-4.00）。静脉给药后，C(max)和 T(max)分别为 4.53±1.43mg/L 和 1.03 小时（0.75-2.50）。口服给药后，血浆浓度时间曲线下面积外推至无穷大（AUC(∞)）为 46.2±1.4mg·h/L，静脉给药后为 52.3±1.3mg·h/L，口服生物利用度平均为 88.32%[90%置信区间（CI）85.64%-91.08%]。
本研究证实，在接受胃旁路手术的健康志愿者中，莫西沙星的暴露量相当于口服和静脉给予 400mg 剂量。但这些暴露量比未接受胃旁路手术的受试者高 50%以上。这可能表明胃旁路手术后莫西沙星的肠肝循环更高。
