PubMed · 7376647
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B H Rumack, R G Peterson. 1980. Acetaminophen toxicity.. https://pubmed.ncbi.nlm.nih.gov/7376647/
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Substituted amylose (SA) matrix drug tablets prepared by direct compression show sustained drug-release properties. The influence of compression force (CF) and tablet weight (TW) on release properties was studied. CF ranging from 0.5 to 5.0 tons/cm(2) has no significant effect on the release properties of SA,G (glycidol) polymers, with a degree of substitution (DS) greater than 1.5. For a low DS, an augmentation of CF increases the release time of acetaminophen, used as a model drug, until a certain limit is reached. On the other hand, TW has a major effect on the release time of acetaminophen. Release time is directly proportional to TW. The effect of the nature of the active material, its solubility and its concentration in the formulation on the release properties of SA, G polymers was also evaluated, demonstrating the versatility of the system.
AIMS: Oral activated charcoal is used to treat drug overdose and is effective at reducing drug absorption when administered within 1 h of drug ingestion. There are fewer data on efficacy when the delay is longer, as is the case in most drug overdoses. This study investigated the efficacy of activated charcoal at preventing paracetamol (acetaminophen) absorption after simulated overdose when administration was delayed between 1 and 4 h. METHODS: An open randomized-order four-way crossover study was performed in healthy volunteers comparing the effect of activated charcoal 50 g on the absorption of 3 g paracetamol tablets when administered after an interval of 1, 2 or 4 h or not at all. Plasma paracetamol concentrations were measured over 9 h after paracetamol ingestion using h.p.l.c. and areas under the curve between 4 and 9 h (AUC(4,9 h)) calculated as a measure of paracetamol absorption. RESULTS: Activated charcoal significantly reduced paracetamol AUC(4,9 h) when administered after 1 h (mean reduction 56%; 95% Confidence intervals 34, 78; P<0.002) or 2 h (22%; 6, 39; P<0.03) but not after 4 h (8%; -8, 24). When administered after 1 h activated charcoal reduced individual plasma paracetamol concentrations significantly at all times between 4 and 9 h after paracetamol administration. Administration at 2 or 4 h had no significant effect. CONCLUSIONS: These results in healthy volunteers cannot be extrapolated directly to poisoned patients. However, they provide no evidence of efficacy for activated charcoal when administered after an interval of more than 2 h.
Great differences between published Heckel parameters, obtained from 'at pressure' data or the 'in-die' method, are outlined. The general validity of the concept of yield pressures derived from slopes of such Heckel plots is questioned. When the ability of the Heckel and the Walker equations is compared to fit density/pressure data from tabletting different pharmaceutical powders, a generally better fit is obtained with the Walker equation in the region of 5-100 MPa. The ability to discriminate between materials by data from the compression phase is improved by using the Walker model. For Emcompress(R), apparent yield pressures derived from Heckel plots are dependent strongly on the maximum pressure of the compression process.