Degradation products of proguanil — 4-chloroaniline and related components with regard to genotoxicity
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Katharina Schulz
,
Ulrich Oberdieck
Abstract
In the event of genotoxic impurities in drug products, knowledge of the origin and fate of these components is of particular importance. In the present study, commercially available proguanil tablets (Paludrine®) were investigated in respect of formation of the main degradation product, 4-chloroaniline (PCA), which is known to be genotoxic. The investigations made use of high performance liquid chromatography coupled with fluorescence detection (HPLC-FLD) and gas chromatography coupled with flame ionisation detection (GC-FID) systems. In addition, proposals for the structure of further proguanil degradation products were developed based on results obtained by mass spectroscopy (HPLC-MS). Database analysis using DEREK, MCASE, and Vitic was performed to obtain an initial toxicological evaluation of the proposed chemical structures. Finally, the absence of the newly established structures in stored proguanil tablets was verified.
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Artikel in diesem Heft
- Enzymatic synthesis of kojic acid esters and their potential industrial applications
- KI-catalysed synthesis of 4-methylcatechol dimethylacetate and fragrant compound Calone 1951®
- Sequestration of supercritical CO2 by mercury oxide
- Assessment of the fate of some household micropollutants in urban wastewater treatment plant
- Synthesis in water-free DMF, characterization, electrical, and gas sensing properties of bis[2-(2-aminoethylamino)ethanol]copper(II) dibromide
- Mechanism of α-acetyl-γ-butyrolactone synthesis
- Spirocyclisation of phytoalexin 1-methoxybrassinin in the presence of Grignard reagents
- Synthesis of new aryl(hetaryl)-substituted tandospirone analogues with potential anxiolytic activity via reductive Heck type hydroarylations
- Methyl-2-arylidene hydrazinecarbodithioates: synthesis and biological activity
- Degradation products of proguanil — 4-chloroaniline and related components with regard to genotoxicity
- In situ bioconversion of compactin to pravastatin by Actinomadura species in fermentation broth of Penicillium citrinum
- Mineral element content in prized matsutake mushroom (Tricholoma matsutake) collected in China
