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Influence of Simulated Weightlessness on the Oral Pharmacokinetics of Acetaminophen as a Gastric Emptying Probe in Man: A Plasma and a Saliva Study

From Laboratoire de Pharmacocinétique et Toxicologie Clinique, Hôpital Rangueil-Larrey, Toulouse, France (Dr. Gandia, Dr. Saivin, Dr. Lavit, Dr. Houin) and Medes, Clinique Spatiale, Hôpital Rangueil-Larrey, Toulouse, France (Dr. Bareille, Dr. Pavy le-Traon, Dr. Guell).

This study evaluated the effect of simulated weightlessness on gastric emptying, using acetaminophen as a probe and -6° head-down bed rest to simulate zero gravity. Eighteen volunteers were given 1 g of acetaminophen orally before the bed rest and at days 1, 18, and 80. C_max, t_max, AUC_0-, AUC_0-t, and t_1/2 were calculated for plasma and saliva. The plasma C_max showed a significant increase (10.43 µg/mL [day 1] to 14.74 µg/mL [day 80]), while t_max significantly decreased (1.41 h [day 1] to 0.91 h [day 80]). Similar results were obtained with saliva, and there were significant increases in the AUCs. The good correlation between the plasma and saliva data suggests that saliva sampling can be valid for acetaminophen pharmacokinetics. The changes in C_max and t_max indicated more rapid drug absorption, which could have been as a result of faster gastric emptying or an increased blood flow to the intestine.

Key Words: Acetaminophen pharmacokinetics • bed rest • gastric emptying • simulated weightlessness

Address for reprints: Georges Houin, PharmD, PhD, Laboratoire de Pharmacocinétique et Toxicologie Clinique, Hôpital Rangueil-Larrey, TSA 50032, 1 avenue Jean Poulhès, 31059 Toulouse cedex 9, France.

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