抗生素胞内抗菌活性及其细胞药代动力学评价的研究进展

侵入宿主细胞内的病原菌不仅逃避了体液免疫,而且逃避了抗生素的作用;同时抗生素在胞内的抗菌活性往往很差,这也是一些感染性疾病反复发作、迁延不愈的主要原因之一。现有的基于血浆药物浓度的经典药代动力学研究不足以有效地预测体内抗生素药效,因此迫切需要开展抗生素的细胞药代动力学研究。本文就近年来抗生素细胞药代动力学及胞内抗菌活性的相关研究做一综述,总结影响抗生素胞内活性的PK/PD参数,并且讨论优化其胞内活性的策略。

Research progress of intracellular activity of antibiotics and its celluar pharmacokinetics evaluation

Intracellular bacteria are protected from the attack of the immune system as well as from the action of the antibiotics present in the extracellular milieu, besides, antibiotics usually poorly act on intracellular bacteria. This is one of the main causes for recurrence and reinfection of infectious diseases. Thus, classical pharmacokinetic studies based on plasma drug concentrations may not be sufficient to predict activity of antibiotics in vivo, and there is a pressing need to expand pharmacokinetics to the new age of cellular pharmacokinetics. This review aims to present and summary the current knowledge of cellular pharmacokinetics of antibiotics including the PK/PD parameters governing the intracellular activity of antibiotics, and to discuss strategies for optimizing this activity.