[Translation] Bioequivalence of balofloxacin capsules produced by Yuekang Pharmaceutical Group Co., Ltd. and balofloxacin tablets imported from South Korea in healthy Chinese men

研究中国健康成年男性志愿者单次口服由悦康药业集团有限公司生产的巴洛沙星胶囊与韩国Choongwae Pharma生产的巴洛沙星片的相对生物利用度，评价试验制剂与参比制剂的生物等效性。

[Translation]

To study the relative bioavailability of balofloxacin capsules produced by Yuekang Pharmaceutical Group Co., Ltd. and balofloxacin tablets produced by Choongwae Pharma, South Korea, after a single oral administration to healthy adult male volunteers in China, and to evaluate the bioequivalence of the test preparation with the reference preparation.

Start Date28 Jun 2013

Sponsor / Collaborator

Yuekang Pharmaceutical Group Co., Ltd.

[+1]

100 Clinical Results associated with Balofloxacin

100 Translational Medicine associated with Balofloxacin

100 Patents (Medical) associated with Balofloxacin

Literatures (Medical) associated with Balofloxacin

01 Dec 2023·The Lancet Microbe

Antimicrobial susceptibility of Treponema pallidum subspecies pallidum: an in-vitro study

Article

Author: Mitjà, Oriol ; González-Beiras, Camila ; Ubals, Maria ; Lieberman, Nicole A P ; Mueller, John ; Tantalo, Lauren C ; Giacani, Lorenzo ; Greninger, Alexander L ; Canut, Andrés ; Pérez-Mañá, Clara ; Tapia, Kenneth ; Rodríguez-Gascón, Alicia ; Suñer, Clara ; Vall Mayans, Marti ; González-Candelas, Fernando

BACKGROUNDThe increasing incidence of syphilis and the limitations of first-line treatment with penicillin, particularly in neurosyphilis, neonatal syphilis, and pregnancy, highlight the need to expand the therapeutic repertoire for effective management of this disease. We assessed the in-vitro efficacy of 18 antibiotics from several classes on Treponema pallidum subspecies pallidum (T pallidum), the syphilis bacteria.METHODSUsing the in-vitro culture system for T pallidum, we exposed the pathogen to a concentration range of each tested antibiotic. After a 7-day incubation, the treponemal burden was evaluated by quantitative PCR targeting the T pallidum tp0574 gene. The primary outcome was the minimum inhibitory concentration (MIC) at which the quantitative PCR values were not significantly higher than the inoculum wells. We also investigated the susceptibility of macrolide-resistant strains to high concentrations of azithromycin, and the possibility of developing resistance to linezolid, a proposed candidate for syphilis treatment.FINDINGSAmoxicillin, ceftriaxone, several oral cephalosporins, tedizolid, and dalbavancin exhibited anti-treponemal activity at concentrations achievable in human plasma following regular dosing regimens. The experiments revealed a MIC for amoxicillin at 0·02 mg/L, ceftriaxone at 0·0025 mg/L, cephalexin at 0·25 mg/L, cefetamet and cefixime at 0·0313 mg/L, cefuroxime at 0·0156 mg/L, tedizolid at 0·0625 mg/L, spectinomycin at 0·1 mg/L, and dalbavancin at 0·125 mg/L. The MIC for zoliflodacin and balofloxacin was 2 mg/L. Ertapenem, isoniazid, pyrazinamide, and metronidazole had either a poor or no effect. Azithromycin concentrations up to 2 mg/L (64 times the MIC) were ineffective against strains carrying mutations associated to macrolide resistance. Exposure to subtherapeutic doses of linezolid for 10 weeks did not induce phenotypic or genotypic resistance.INTERPRETATIONCephalosporins and oxazolidinones are potential candidates for expanding the current therapeutic repertoire for syphilis. Our findings warrant testing efficacy in animal models and, if successful, clinical assessment of efficacy.FUNDINGEuropean Research Council.

01 Mar 2023·Journal of Molecular Graphics and Modelling

Q-RepEx: A Python pipeline to increase the sampling of empirical valence bond simulations

Article

Author: Brickel, Sebastian ; Kamerlin, Shina Caroline Lynn ; Pinto, Gaspar P ; Crean, Rory M ; Demkiv, Andrey O

The exploration of chemical systems occurs on complex energy landscapes. Comprehensively sampling rugged energy landscapes with many local minima is a common problem for molecular dynamics simulations. These multiple local minima trap the dynamic system, preventing efficient sampling. This is a particular challenge for large biochemical systems with many degrees of freedom. Replica exchange molecular dynamics (REMD) is an approach that accelerates the exploration of the conformational space of a system, and thus can be used to enhance the sampling of complex biomolecular processes. In parallel, the empirical valence bond (EVB) approach is a powerful approach for modeling chemical reactivity in biomolecular systems. Here, we present an open-source Python-based tool that interfaces with the Q simulation package, and increases the sampling efficiency of the EVB free energy perturbation/umbrella sampling approach by means of REMD. This approach, Q-RepEx, both decreases the computational cost of the associated REMD-EVB simulations, and opens the door to more efficient studies of biochemical reactivity in systems with significant conformational fluctuations along the chemical reaction coordinate.

01 Jan 2023·Environmental Pollution

Structural and antimicrobial property changes of veterinary antibiotics in thermal treatment

Article

Author: Chen, Guanyi ; Chen, Xi ; Yang, Yongkui ; Sun, Peizhe ; Cheng, Zhanjun

Agricultural application contributes major consumption of antibiotics worldwide. As veterinary antibiotics are poorly metabolized by animals, most of them end up in agricultural waste, which is increasingly subject to thermal treatment, such as torrefaction, pyrolysis, etc. However, there is a lack of research on their thermal decomposition mechanisms and products elucidation. Therefore, this study investigated the thermal decomposition of four major veterinary antibiotics groups (β-lactams, tetracyclines, fluoroquinolones, sulfonamides) with emphasis on their thermal stability, structural transformation and antibacterial activity. Results show that thermal treatment can remove the parent antibiotics with their antibacterial activity except for gatifloxacin (GAT). Although the parent form of GAT was fully removed at 200 °C, its products showed significant antibacterial activity against E. coli. We present novel evidence that the PhO-CH₃ chemical bond on GAT preferentially brake to generate methyl radical, which underwent a substitution reaction at the para position of phenol. This reaction also occurred during the thermal decomposition of antibiotic analogues, balofloxacin and moxifloxacin, whose thermolysis products also showed significant antibacterial activity. Furthermore, these thermolysis products may present potentially cardiotoxic and pose higher risks to human health than their parent forms, based on the comparison with a group of drugs withdrawn from the market.

100 Deals associated with Balofloxacin

External Link

KEGG	Wiki	ATC	Drug Bank
D02463	Balofloxacin	J01MA	-

R&D Status

Approved

10 top approved records.

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Indication	Country/Location	Organization	Date
Bacterial Infections	KR	JW PHARMACEUTICAL Corp.	06 May 1993
Urinary Tract Infections	CN	Jiangsu Hansoh Pharmaceutical Co. Ltd.	-

Developing

10 top R&D records.

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Indication	Highest Phase	Country/Location	Organization	Date
Bacterial Infections	Preclinical	JP	Kyoto Pharmaceutical University	01 Aug 1992

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