Objective: To investigate the transplacental transfer of the macrolide antibiotics erythromycin, roxithromycin and azithromycin.
Methods: Twenty-one term placentas were obtained with maternal consent immediately after delivery and a two-hour nonrecirculating perfusion of a single placental cotyledon was performed. Erythromycin (2 microg/mL), roxithromycin (2 microg/mL) and azithromycin (0.3 microg/mL) were infused to the maternal inflow at a constant rate, with antipyrine as a reference compound, and their appearance in the fetal circulation was followed. Drug concentrations were measured by high performance liquid chromatography for 120 min.
Results: The mean transplacental transfers (TPT(SS)) for erythromycin, roxithromycin and azithromycin were 3.0%, 4.3% and 2.6%, respectively, calculated as the ratio between the steady state concentrations in fetal venous and maternal arterial sides. Similar results were obtained when the TPT was calculated as the absolute amount of drug transferred across the placenta during 2-hour perfusion (TPT(A)). No significant differences were found among the three macrolides in TPT(SS) (P = 0.39) or TPT(A) (P = 0.35). The TPT(SS) of erythromycin, roxithromycin and azithromycin were 41%, 35% and 32% of the freely diffusable reference compound antipyrine, respectively. Steady state was reached in 60 minutes in each perfusion indicating sufficient perfusion time.
Conclusion: The limited transplacental transfer of erythromycin, roxithromycin and azithromycin suggests compromised efficacy in the treatment of fetal infections. On the other hand, the placenta seems to produce an effective barrier reducing the fetal exposure when these three macrolides are used to treat maternal infections.
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http://dx.doi.org/10.1111/j.1471-0528.2000.tb13339.x | DOI Listing |
Chem Pharm Bull (Tokyo)
December 2024
School of Traditional Chinese Medicines, Shenyang Pharmaceutical University.
Enteric-coated microcapsules can protect roxithromycin (ROX) from acid hydrolysis enhancing efficacy, solubility, and dissolution rate, representing a promising oral formulation for children and patients with swallowing difficulties. ROX-layered core particles were obtained with polyvinylpyrrolidone (PVP) K30 as the binder and Eudragit L30 D-55 as the coating material using the Wurster process in a fluidized bed processor. The enteric-coated microcapsules were characterized using powder X-ray diffraction, differential scanning calorimetry, and polarized optical microscopy.
View Article and Find Full Text PDFHuan Jing Ke Xue
December 2024
School of Ecological Technology and Engineering, Shanghai Institute of Technology, Shanghai 201418, China.
In recent years, due to large-scale production and widespread use, drugs have posed a potential threat to biological and human health and have received increasing attention. The occurrence and distribution of drugs in urban rivers are influenced by various factors, such as urbanization level, population density, regional geographical and climatic characteristics, and drug consumption habits. In October 2022, the Yongjiang River Basin was divided into four sub-basins: upstream, midstream, tributaries, and downstream.
View Article and Find Full Text PDFRapid Commun Mass Spectrom
December 2024
Departamento de Química, Faculdade de Filosofia, Ciências e Letras de Ribeirão Preto, Universidade de São Paulo, Ribeirão Preto, SP, Brazil.
Rationale: Macrolides are critical antibiotics featuring a macrocyclic lactone core with deoxy sugars. Understanding their gas-phase fragmentation is challenging but essential for improving structural elucidation in mass spectrometry, which has implications for drug discovery and development.
Methods: We used electrospray ionization collision-induced dissociation tandem mass spectrometry (ESI-CID-MS) combined with quantum chemical calculations to investigate the fragmentation pathways of erythromycin A and roxithromycin.
Environ Monit Assess
September 2024
School of Petrochemical Engineering, Changzhou University, Changzhou, 213164, Jiangsu, China.
This work examined the occurrence characteristics and ecological risks of 31 antibiotics across five classes and seven ARGs in the surface waters of Gaoyou Lake. A total of 27 antibiotics, spanning four classes, were detected in the surface waters of Gaoyou Lake, with an overall concentration ranging from 57.5 to 114 ng/L and an average of 78.
View Article and Find Full Text PDFChemosphere
September 2024
School of Environment and Civil Engineering, Jiangnan University, Wuxi, Jiangsu 214122, PR China; Jiangsu Key Laboratory of Anaerobic Biotechnology, Jiangnan University, Wuxi 214122, PR China; Jiangsu Engineering Laboratory of Biomass Energy and Carbon Reduction Technology, Jiangnan University, Wuxi 214122, PR China; Water Treatment Technology and Material Innovation Center, Suzhou University of Science and Technology, Suzhou 215009, PR China. Electronic address:
Microbial electrolysis cells (MEC) have emerged as a prominent technology for the treatment of antibiotics-containing wastewater in recent years. However, there remains a dearth of comprehensive exploration regarding the influence of extracellular polymers substances (EPS) on the distribution and transmission of antibiotic resistance genes (ARGs) in MEC. In this study, we quantified the distribution of ARGs in MEC by Fluorescence quantitative polymerase chain reaction and explored with emphasis on impact of EPS component on ARGs transmission at under different concentrations of roxithromycin.
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