Biopharmaceutics and pharmacokinetics of plain and soluble brands of aspirin tablets embedded in food bolus orally administered to human volunteers

Many people ingest solid drugs embedded in food bolus to alleviate the problems of gastric irritation, unpleasant taste and odour which may affect the biopharmaceutics and pharmacokinetics of the drugs. This study investigated the biopharmaceutics and pharmacokinetics of plain and soluble brands of aspirin tablets embedded in food bolus orally administered to human volunteers. The pharmacokinetic profiles of two brands of commercial, uncoated aspirin tablets (300 mg) were assessed in eight healthy human volunteers when taken unembedded and when embedded in food bolus. The tablet samples were coded as S (soluble or dispersible aspirin tablet), P (plain or immediate-release aspirin tablet), SB (soluble aspirin tablet embedded in food bolus) and PB (plain aspirin tablet embedded in food bolus). Pharmacokinetic parameters generated from the salivary excretion data were evaluated. The biopharmaceutics factors of the drugs were also considered. The cumulative drug excreted up to 24 hours [E24h] and maximum excretion rate [dE/dt]max of S were significantly higher (P < 0.05) than P, SB and PB. Time for maximum excretion rate [Tmax] of S was significantly lower (P < 0.05) than P, SB and PB. There was no significant difference (P > 0.05) between P and SB, but PB had significantly lower E24h, and [dE/dt]max (P < 0.05) and significantly higher Tmax (P < 0.05) than P and SB. Food coating and excipients were observed as the biopharmaceutics factors that influenced the pharmacokinetics of the aspirin tablets. Biopharmaceutics and pharmacokinetics of aspirin tablets may be significantly altered when embedded in food bolus.