Margarit F, Moreno-Dalmau J, Obach R, Peraire C, Plá-Delfina J M
Department of Pharmacy, University of Barcelona, Spain.
Eur J Drug Metab Pharmacokinet. 1991;Spec No 3:102-7.
Intestinal absorption rate constants of amoxicillin, ampicillin, epicillin, cyclacillin and azidocillin, by means of a static in situ intestinal perfusion method has been estimated. Luminal remaining antibiotic concentrations were determined using a standard microbiological technique. In order to establish statistically better absorption kinetics, five dose levels were used, ranging from 10 to 1000 micrograms/ml, and first order, Michaelis-Menten and combined first-order and Michaelis-Menten differential model equations were fitted to experimental data found for each antibiotic. According to the AIC test, the best equation for absorption kinetics was selected. Amoxicillin and ampicillin absorption mechanisms were better described by combined kinetics, while for cyclacillin and epicillin the most probable kinetics was that of Michaelis-Menten. For azidocillin, the only non-aminopenicillin component of this series, first order kinetics should be statistically selected.
采用静态原位肠灌注法估算了阿莫西林、氨苄西林、依匹西林、环青霉素和叠氮西林的肠道吸收速率常数。使用标准微生物技术测定肠腔中残留的抗生素浓度。为了在统计学上建立更好的吸收动力学,使用了5个剂量水平,范围从10至1000微克/毫升,并将一级、米氏和一级与米氏组合微分模型方程拟合到每种抗生素的实验数据中。根据AIC检验,选择了最佳的吸收动力学方程。阿莫西林和氨苄西林的吸收机制用组合动力学能更好地描述,而环青霉素和依匹西林最可能的动力学是米氏动力学。对于该系列中唯一的非氨基青霉素成分叠氮西林,应在统计学上选择一级动力学。