PubMed · 15719787
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Paracetamol.. https://pubmed.ncbi.nlm.nih.gov/15719787/
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The ability to rapidly detect and characterize drug metabolites in biological fluids often relies on a combination of a high quality chromatographic separation and sensitive high resolution mass spectrometry. Here, the performance of two high throughput LC/MS approaches, namely monolith columns and sub-2 microm particle Ultra Performance Liquid Chromatography (UPLC) columns is compared for the detection and identification of the human metabolites of acetaminophen in urine. The UPLC system produced approximately three times the sensitivity and detected more metabolites than the monolithic column approach. The sharp peaks produced by UPLC seem to be particularly advantageous when coupled to electrospray mass spectrometry, apparently reducing ion suppression leading to superior sensitivity and hence lower limits of detection.
A polyglycolised glyceride carrier, Gelucire 50/13, was incorporated with paracetamol as a model drug, filled into hard gelatin capsules and stored at three different temperatures for various lengths of time. The resultant solidified matrix within the capsule was subjected to thermal analysis using differential scanning calorimetry (DSC) to ascertain its supramolecular structure. Polymorphic transformations towards more stable gelucire forms were observed upon aging the matrices, with samples stored at a temperature near the melting range of the lower temperature gelucire melting fraction showing the most profound changes. The increase in the rate of drug release from aged samples could be correlated to the alterations to the supramolecular structure of the gelucire. Accelerated drug release from aged samples could also be seen from in vivo studies using healthy human volunteers, although the extent of absorption was not affected. Therefore, even though the sustainability of release may be compromised by aging the gelucire matrices, the bioavailability of the incorporated drug is unlikely to be affected.
This paper reports on the cross-linking of dried (<5% moisture) paracetamol alginate granules with calcium chloride solutions. The effect of calcium concentration, temperature of the treatment solution, stirring speed and time used during cross-linking of granules on water uptake by the granules during cross-linking and physical properties of the cross-linked and dried granules were studied. A full factorial study of these factors each at two levels was used (CaCl2.2H2O: 20, 100 mg/ml; temperature: 25, 45 degrees C; stirrer speed: 25, 240 rpm; time: 1.5 and 5.5 min) to treat dried stock granules (size: 0.8-1.0 mm) containing the model drug paracetamol and sodium alginate powder (1:1) which were prepared using conventional aqueous granulation under low shear. In addition to SEM and photomicrography, the physical properties studied were water uptake during cross-linking, yield, aggregation behaviour, moisture content, drug content, early stage drug release [over 10 s (R10) and the next 50 s (R50)] and calcium and sodium content of the unwashed cross-linked granules. Dry granules were successfully cross-linked. The treatment factors significantly affected most of the response variables. The variables most affected were water uptake (78-254%), drug entrapment (58-86%), early release (R10: 1.2-6.4% and R50: 3.0-12.2%), granule aggregation (0-70%), calcium (6.02-12.4%) and sodium content (1.2-6.44%). SEM photographs suggest that low calcium treated granules were less porous in nature compared to high calcium treated granules. Low shear drug alginate granules can be cross-linked in dried state. The properties of the cross-linked granules can be modified by altering the treatment process.