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口服磷霉素制剂与饲料或饮用水之间的潜在相互作用:对仔猪生物利用度的影响。

Potential interactions between an oral fosfomycin formulation and feed or drinking water: Impact on bioavailability in piglets.

机构信息

Área Toxicología, Departamento de Fisiopatología, Facultad de Ciencias Veterinarias, Universidad Nacional del Centro de la Provincia de Buenos Aires, Tandil, Argentina.

Facultad de Ciencias Veterinarias, Centro de Investigación Veterinaria de Tandil (CIVETAN, UNCPBA-CICPBA-CONICET, Tandil, Argentina.

出版信息

J Vet Pharmacol Ther. 2021 Sep;44(5):783-792. doi: 10.1111/jvp.12966. Epub 2021 Mar 15.

Abstract

Feed and drinking water are the most frequently used vehicles for administration of antibiotics in intensive pig production. Interactions of drugs with feed and water components may affect dissolution and bioavailability. Therefore, antibiotic formulations should be tested in order to assure their suitability for oral use. In this study, an oral fosfomycin (FOS) formulation was evaluated considering dissolution in water (soft and hard), release kinetics from feed in simulated gastrointestinal fluids and bioavailability after oral administration blended into feed or dissolved in water (soft and hard), to fed and fasted piglets. FOS reached immediate dissolution in soft and hard water. The presence of feed significantly decreased antibiotic dissolution in simulated intestinal medium. Bioavailability was lower when feed was used as a vehicle for FOS administration than when the drug was dissolved in water (soft or hard). The fed or fasted condition of piglets did not affect bioavailability. Probably, FOS interactions with feed components alter its dissolution in the gastrointestinal tract, and only a fraction of the dose would be available for absorption. This information must be considered to support decisions on eligibility of antibiotic pharmaceutical formulations and the vehicle for their administration in order to pursue a responsible use of antibiotics.

摘要

在集约化养猪生产中,饲料和饮用水是最常被用作投药途径的媒介,用于投予抗生素。药物与饲料和水分成分之间的相互作用可能会影响药物的溶解和生物利用度。因此,应测试抗生素制剂,以确保其适合口服使用。在这项研究中,评估了一种口服磷霉素(FOS)制剂,考虑了其在水(软、硬)中的溶解情况、在模拟胃肠道液中的释放动力学以及在口服投予(混入饲料或溶于水软、硬)后在禁食和进食仔猪体内的生物利用度。FOS 可立即溶于软、硬水。饲料的存在显著降低了抗生素在模拟肠液中的溶解。与将药物溶于水(软或硬)相比,当饲料用作 FOS 投药途径时,生物利用度较低。仔猪的进食或禁食状态并不影响生物利用度。可能是 FOS 与饲料成分相互作用改变了其在胃肠道中的溶解,只有一部分剂量可被吸收。在决定抗生素药物制剂的适用性和投药途径时,必须考虑这些信息,以负责任地使用抗生素。

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