White C A, Toothaker R D
J Antimicrob Chemother. 1985 Jan;15 Suppl A:257-60. doi: 10.1093/jac/15.suppl_a.257.
Escherichia coli ATCC 12407 was exposed in an in-vitro kinetic model to multiple dose ampicillin regimens differing in simulated drug elimination half-life but with equal dosage intervals and similar dose levels. Bacterial sensitivity was monitored during drug exposure. Greater bactericidal effect was observed with long half-life regimens. The development of rapid low-level resistance was not influenced by the half-life. Results suggest that in-vivo drug activity may be improved by increasing the drug elimination half-life.
将大肠杆菌ATCC 12407置于体外动力学模型中,使其暴露于模拟药物消除半衰期不同但给药间隔相同且剂量水平相似的多次剂量氨苄西林给药方案下。在药物暴露期间监测细菌敏感性。半衰期长的给药方案显示出更大的杀菌效果。快速低水平耐药性的产生不受半衰期的影响。结果表明,增加药物消除半衰期可能会提高体内药物活性。