<p><strong>Objective: </strong>This study was aimed at developing an HPLC method that would be suitable and sufficiently robust to analyze clarithromycin or spiramycin from bulk materials, amorphous solid dispersions as well as when included into solid dosage forms.</p><p><strong>Methods: </strong>A C<sub>8</sub> column (250 x 4.6 mm, 5 µm) was used as stationary phase, the mobile phase consisted of 0.1 M dipotassium hydrogen orthophosphate buffer (pH 6.0) and acetonitrile in a 50:50 (% v/v) ratio. The flow rate was set to 0.5 ml/min. UV detection of 210 nm was used for clarithromycin and 232 nm for spiramycin. Ambient column and sample tray temperatures were used.</p><p><strong>Results: </strong>The method proved to be suitable for the detection of both macrolide antibiotics in bulk samples, as part of amorphous solid dispersions as well as in dosage forms. The isocratic elution was rapid. The method was validated in terms of system suitability, limits of detection (LOD), limit of quantification (LOQ), accuracy, precision, linearity, and specificity. This method showed linearity across the concentration range of 4.0–5000.0 µg/ml for both antibiotics.</p><p><strong>Conclusion: </strong>The developed method showed to be a simple and sufficiently sensitive method for the detection and quantification of either clarithromycin or spiramycin from samples that might contain even very small quantities of the antibiotics.</p>
Parkinson’s disease is a complex neurodegenerative condition with current treatment only focussed on symptomatic therapy that does not slow or stop the progression of the disease. Since the discovery that adenosine A1 and A2A receptors are potential drug targets for the therapy of Parkinson’s disease, various research groups have attempted to identify adenosine antagonists. So the possibility exists that the administration of an adenosine A2A receptor antagonist may prevent further neurodegeneration. Furthermore, the antagonism of adenosine A1 receptors has the potential of treating Parkinson’s disease-associated cognitive deficits. Therefore, dual antagonism of adenosine A1 and A2A receptors would be of great benefit since this would potentially treat both the motor as well as the cognitive impairment associated with Parkinson’s disease. Based on the observation that a series of 1,4-dihydropyridine derivatives possess adenosine A1 and A2A receptor affinity, the current study investigated the potential of the structurally related 3,4-dihydropyrimidone analogues as adenosine A1 and A2A receptor antagonists. Overall, the 3,4-dihyropyrimidone analogues were found to possess weak affinity for the adenosine A2A receptor, but more promising adenosine A1 receptor affinity was found, ranging in the low micromolar range. Among the investigated compounds, the p-bromophenyl substituted dihydropyrimidone (6b) possesses the best adenosine A1 receptor affinity with a Ki value of 7.39 µM. In conclusion, this 3,4-dihydropyrimidone derivative can be used as a lead for the design of novel adenosine A1 receptor antagonists, although further structural modifications are required to enhance the adenosine A2A receptor affinity before a clinically viable candidate will be available as potential treatment of Parkinson’s disease.
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