Abstract
Currently, there is still a need for broad-spectrum antibiotics. The new cephalosporin antibiotics include, among others, ceftobiprole, a fifth-generation gram-positive cephalosporin, active against Staphylococcus aureus methicillin agonist (MRSA). The main focus of the work was to optimize the conditions of ceftobiprole qualitative determination and to validate the developed procedure according to ICH guidelines. As a result of the optimization process, HPTLC Cellulose chromatographic plates as a stationary phase and a mixture consisting of ethanol:2-propanol: glacial acetic acid: water (4:4:1:3, v/v/v/v) as a mobile phase were chosen. The densitometric detection was carried out at maximum absorbance of ceftobiprole (λ = 232 nm). Next, the validation process of the developed procedure was carried out. The relative standard deviation (RSD) for precision was less than 1.65%, which proves the high compatibility of the results, as well as the LOD = 0.0257 µg/spot and LOQ = 0.0779 µg/spot values, which also confirm the high sensitivity of the procedure. The usefulness of the developed method for the stability studies of ceftobiprole was analyzed. Study was carried out under stress conditions, i.e., acid and alkaline environments, exposure to radiation imitating sunlight and high temperature (40–60 °C). It was found that cefotbiprole is unstable in an alkaline environment and during exposure to UV-VIS radiation. Moreover, the lipophilicity parameter, as a main physicochemical property of the biologically active compound, was determined using experimental and computational methods.
Highlights
Cephalosporins, which belong to the group of semi-synthetic β-lactam antibiotics, have their origins as early as in the middle of the 20th century
1945 the scientist became interested in people who swam in rivers polluted with faeces or consumed shellfish fished from them. These people did not get sick, while in other parts of Italy, there was a typhoid pandemic—at the time known as abdominal typhus. Brotzu hypothesised that these sewage systems probably contain microorganisms that inhibit the growth of pathogenic intestinal bacteria—Salmonella typhi—that can prevent the spread of typhus [1]
Research is being conducted which focuses on the search for new antibiotics with a broad spectrum of effects
Summary
Cephalosporins, which belong to the group of semi-synthetic β-lactam antibiotics, have their origins as early as in the middle of the 20th century. 1945 the scientist became interested in people who swam in rivers polluted with faeces or consumed shellfish fished from them These people did not get sick, while in other parts of Italy, there was a typhoid pandemic—at the time known as abdominal typhus. Despite its considerable advantages, such as high resistance to staphylococcal penicillinase enzyme and hydrolysis in an acidic environment, like the rest of the natural penicillin, it has not been used in Processes 2021, 9, 708 the therapeutic field due to its low activity. For this reason, we are currently using its semi-synthetic acid, which which was wasformed formedas semi-syntheticderivatives derivativesobtained obtainedfrom from7-aminocephalosporic
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