Impurity study of marbofloxacin, the "miracle drug" against influenza

Influenza is an acute respiratory infection caused by the influenza virus. The current means of combating influenza mainly include vaccine prevention and medication, and medication remains an important means of combating influenza.

Common anti-influenza viral drugs include neuraminidase inhibitors such as oseltamivir, zanamivir, and paramivir, as well as the haemagglutinin inhibitor abidol and the polymerase inhibitor famciclovir, etc. The application of anti-influenza viral drugs at an early stage, especially within 48 hours of the onset of the disease, can significantly reduce the incidence of severe influenza illness and death.

Marbofloxacavir is a cap-dependent nucleic acid endonuclease inhibitor that blocks influenza faster than oseltamivir by inhibiting influenza viruses from seizing the cap structure at the 5‘ end of host mRNA from the host cells for their own mRNA transcription, which deprives the viruses of the ability to replicate themselves, and thus inhibits influenza viruses from reproducing themselves at an early stage. It is the first anti-influenza drug with an innovative mechanism of action in the past 20 years, and is effective against both influenza A and B.

The impurities of Marbovir mainly come from the side reaction of synthesis, China Institute of Food and Drug Administration (CFDA) participated in the study of "Reversed-phase High Performance Liquid Chromatography (RP-HPLC) for Simultaneous Determination of 3 Stereoisomers in Marbovir APIs", which pointed out that in the synthesis of Marbovir to build up a biphasic centre, 1 enantiomer and 2 diastereoisomers will be produced in the synthesis process. 2 diastereoisomers. Chiral drugs containing different stereoisomers have significant differences in pharmacokinetics, pharmacodynamics and toxicology, and may have certain toxic side effects, affecting efficacy and safety. In addition, the enantiomeric and diastereoisomers of marbofloxacin are present in APIs, which directly affect the drug quality.

 

In this study, a chromatographic method based on the principle of reversed-phase elution was established to detect the contents of different stereoisomers in marbalosavir, and the three stereoisomeric impurities were confirmed to be process impurities rather than degradation impurities. Under the premise that the quality standard of Marboloxavir API is not included in foreign pharmacopoeias, the limit of stereoisomeric impurities was set at 0.1% by the results of the sample measurement during the stability test of Marboloxavir API and the results of the original development agent.

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