美罗培南
生物利用度
碳青霉烯
前药
抗生素
广谱
抗菌剂
药理学
生物制药
医学
药品
抗生素耐药性
微生物学
生物
化学
生物活性
生药学
体外
生物化学
组合化学
作者
Aun Raza,Shih Chen Ngieng,Fekade B. Sime,Peter J. Cabot,Jason A. Roberts,Amirali Popat,Tushar Kumeria,James R. Falconer
标识
DOI:10.1016/j.drudis.2020.11.004
摘要
An increase in the number of multidrug-resistant microbial strains is the biggest threat to global health and is projected to cause >10 million deaths by 2055. The carbapenem family of antibacterial drugs are an important class of last-resort treatment of infections caused by drug-resistant bacteria and are only available as an injectable formulation. Given their instability within the gut and poor permeability across the gut wall, oral carbapenem formulations show poor bioavailability. Meropenem (MER), a carbapenem antibiotic, has broad-spectrum antibacterial activity, but suffers from the above-mentioned issues. In this review, we discuss strategies for improving the oral bioavailability of MER, such as inhibiting tubular secretion, prodrug formulations, and use of nanomedicine. We also highlight challenges and emerging approaches for the development of oral MER.
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