Giovanni Boccardi

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Chemical degradation and stability in formulation is a recurrent issue in pharmaceutical development of drugs. The objective of the present study was to develop an in silico risk assessment of active pharmaceutical ingredients (APIs) stability with respect to autoxidation. The chemical degradation by autoxidation of a diverse series of APIs has been(More)
The major route of degradation of tetrazepam (1) is oxidation to 7-chloro-5-(3-keto-cyclohexen-1-yl)-1,3-dihydro-1-methyl-2H-1, 4-benzodiazepin-2-one (3) via the stable 7-chloro-5-(3-hydroperoxy-cyclohexen-1-yl)-1,3-dihydro-1-methyl-2H -1, 4 benzodiazepin-2-one (2). Minor degradation products are(More)
In the study of the degradation of drug substances by molecular oxygen, their specific reaction mechanisms must be taken into account. The rate-determining step is usually the reaction of the substrate with a radical chain initiator, which is often an unknown impurity. The reactivity and selectivity of autoxidation can be controlled better by using a(More)
1. We have assessed the relative abilities of compounds belonging to the new aryloxypropanolaminotetralin (APAT) class and of the reference beta-adrenoceptor-blocking agent, alprenolol, to antagonize functional responses in vitro and in vivo involving atypical (beta 3) or conventional (beta 1 and beta 2) beta-adrenoceptors. 2. The range of pA2 values for(More)
In the context of the Quantitative Structure-Activity Relationship (QSAR) for new drugs, knowledge and understanding of the behavior of the molecules in solution and simulated media are key points to provide the best formulated compounds. Current analytical determinations can give solubility data and dedicated techniques can provide other physico-chemical(More)
The rounding of an analytical result is a process that should take into account the uncertainty of the result, which is in turn assessed during the validation exercise. Rounding rules are known in physical and analytical chemistry since a long time, but are often not used or misused in pharmaceutical analysis. The paper describes the theoretical background(More)
An NMR HSQC method has recently been proposed for the quantitative determination of the mono- and disaccharide subunits of heparin and low molecular weight heparins (LMWH). The focus of the current study was the validation of this procedure to make the 2D-NMR method suitable for pharmaceutical quality control applications. Pre-validation work investigated(More)
The quantitative use of NMR spectroscopy was investigated by a reproducibility study of 1H-NMR integrals involving five laboratories. A significant laboratory effect was found confirming the difficulty to obtain very precise data by integration of complex signals. The reproducibility of any NMR assay measurement, which requires a high precision should be(More)
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