AbstractDrugs that are largely restricted to the gastro‐intestinal tract (GIT) for their therapeutic efficacy and that are not substantially absorbed into the body are usually inadequately studied in terms of systemic bioavailability. The possibility of systemic effects requires that bioavailabilities be studied to ensure against enhanced toxicity resulting from formulation differences. Pyrantel pamoate falls into this category. High‐performance liquid chromatography was employed in this study to determine plasma levels of pyrantel in nine healthy human subjects after administration of tablet and suspension dosage forms. Mean peak plasma concentrations of 37.56 ± 9.37, 35.89 ± 8.94, and 36.22 ± 10.10 ng mL−1were obtained following administration of 750 mg pyrantel pamoate in three different formulations. The meantmaxvalues were 2.02 ± 0.12, 2.05 ± 0.356, and 2.05 ± 0.339 h respectively for the above dosage forms; the respective AUC0–9values were 81.01 ± 12.97, 94.59 ± 17.18, and 101.47 ± 19.59 h ng mL−1. There was no statistically significant difference between the bioavailabilities of the dosage forms tested. Large inter‐subject variations were observed. One subject experienced abdominal discomfort and one experienced dizziness. It was not possible to clearly correlate individual variations in absorption with the observed adverse effect because the number of incidents was low (two o
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