Biopharmaceutics of rectal administration of drugs in man
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In this report it will be shown that rectally administered paracetamol may be regarded as an alternative to oral administration.
Plasma paracetamol and paracetamol-glucuronide concentrations were measured in 6 volunteers after single oral (1000 mg) and rectal (500 mg and 1000 mg) doses of the drug, suspended in aqueous vehicles.
Compared with oral administration rectal absorption can be equally rapid depending on the volume of administered suspension. This effect is due to differences in absorption surface involved in the human rectum. Relative bioavailability has been found in the same range for the oral and rectal route of administration. The results indicate that rectally administered paracetamol does not reach the general circulation without liver passage.
It is concluded that hepatic first pass metabolism is strongly dependent upon the rate of uptake of paracetamol from the rectum.
KeywordsParacetamol Relative Bioavailability Rectal Administration Pass Metabolism Sennoside
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