Introduction: Antibacterial quinolones class comprises a series of synthetic antibacterial agents, following the model of nalidixic acid. Because of their common 6-fl uorosubtituent on the quinolone ring, fluroquinolones are the most potent analogues with extended spectrum of activity and great pharmacokinetic properties. The applicability of capillary zone electrophoresis for the separation of fl uoroquinolones in acidic background electrolyte has been studied, our aim being the development of a capillary zone electrophoresis method for the simultaneous separation of six fl uoroquinolones and also to optimize the analytical conditions. The six studied fl uoroquinolones were ciprofloxacin, enoxacin, enrofloxacin, moxifloxacin, ofloxacin and sarafloxacin.
Material and methods: Preliminary, we studied the electrophoretic behavior of six fluoroquinolones in an acidic pH, which highlighted the possibility of developing a separation method in this area of pH. Electrophoretic parameters infl uencing separation performance were studied and optimized.
Results: A fast and reliable method has been developed, using a background electrolyte containing 100 mM phosphoric acid and the following conditions: applied voltage: + 25 kV, temperature: 20°C, injection pressure 30 mbar - 5 sec, UV detection at 280 nm, capillary: 60 cm (52 cm effective length) x 50 μm, analyte concentration: 167 μg/ml. The separation of the studied fl uoroquinolones was achieved in less than 8 minutes.
Conclusions: Capillary zone electrophoresis using an acidic background electrolyte proved to be an efficient tool in the separation of fluoroquinolones from different generations. Also the proposed methods are particular environment-friendly replacement and improvement of a common high performance liquid chromatography determination with rapid analysis time without using any organic solvents.
Bissera A. Pilicheva, Margarita I. Kassarova, Plamen I. Zagorchev and Yordanka I. Uzunova
Betahistine dihydrochloride is a histamine-like drug widely used in relieving the symptoms associated with Ménière’s syndrome. Pharmacokinetic studies of betahistine have demonstrated that it has a short plasma half-life of 3-4 hours. In such cases frequent administration of the drug is required in order to keep plasma concentration within the therapeutic range. However, this may lead to noncompliance and aggravate patients’ comfort. An advanced approach for achieving sustained release of drugs is their incorporation in microparticulate carriers. AIM: To design a sustained release microsphere formulation of betahistine providing reduced dose frequency and lower risk of side effects occurrence. MATERIALS AND METHODS: Betahistine-loaded chitosan microspheres were obtained via W/O emulsion solvent evaporation technique and were characterized for particle size, drug loading and entrapment efficiency. Drug release into phosphate buffer saline pH 7.4 was performed and dissolution profiles of the formulations were obtained. To study the mechanism of drug release from the microspheres the dissolution data was fitted to various mathematic models. RESULTS: Betahistine-loaded microspheres were produced with a high drug loading and entrapment efficiency. The microcarriers were spherical in shape with mean particle size of 3.82 μm to 7.69 μm. Betahistine release studies from the microspheres showed similar and slightly increasing dissolution profiles. The drug release proceeded in a controlled manner following Fickian diffusion. CONCLUSION: The obtained results suggest that betahistine-loaded chitosan microspheres prepared by solvent evaporation method are capable of sustained release of drugs and therefore can be used as drug delivery systems in the treatment of Ménière’s syndrome.
Robert-Alexandru Vlad, Lenard Farczadi, Silvia Imre, Adriana Daniela Ciurba, Nicoleta Todoran, Emoke Redai, Paula Antonoaea and Daniela Lucia Muntean
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Danijela Tasic, Nebojsa Tasic, Dalibor Dragisic and Miroslav Mitrovic
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Irina Magdalena Dumitru, Roxana Carmen Cernat and S. Rugină
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The main goal of treating rheumatic diseases is to achieve rapid and effective suppression of inflammation. More and more drugs have been proven to be able to achieve these goals nowadays. The current practice is to give a recommended dose of drugs to our patients according to the body weight, risk factors and tolerance, etc. However, all our patients are different individuals who have different pharmacokinetics, and this difference in pharmacokinetics can affect the true drug concentration that is working inside them. This may create