caa a22 4500 477057373 CHVBK 20180405111350.0 cr unu---uuuuu 170330e19960601xx s 000 0 eng 10.1007/s002280050114 doi (NATIONALLICENCE)springer-10.1007/s002280050114 Effect of food intake on pharmacokinetics and effects of a new thromboxane A2 receptor antagonist, S-1452 [Elektronische Daten] [A. Fujimura, T. Shiga, Y. Kumagai, K. Ohashi, A. Ebihara, T. Kotegawa] Objective: To examine the effect of food ingestion on the pharmacokinetics of a new thromboxane A2 (TXA2) receptor antagonist, S-1452, and the inhibitory effect on platelet aggregation. Methods: Fifty milligrams of S-1452 was given orally to eight healthy subjects with or without food. Blood samples for determinations of plasma drug concentrations and of its effects on platelet aggregation were taken for a 12-h post-drug period. Results: The maximum plasma concentration of S-1452 was reduced by 47% and the time to maximum concentration was prolonged from 0.5 to 1.9 h after dosing with food. The inhibitory effect of S-1452 on platelet aggregations induced by U-46619, a TXA2 receptor agonist, and collagen persisted up to 9 h after dosing with and without food. The degrees of inhibition in the two trials did not differ significantly at any point. Conclusion: These results suggest that although the absorption of S-1452 is delayed and, consequently, its plasma concentration is decreased after dosing with food, the inhibitory effect on platelet aggregation is not significantly influenced after 50 mg of the drug. Springer-Verlag Berlin Heidelberg, 1996 Key words S-1452 nationallicence Thromboxane A2 receptor antagonist nationallicence food ingestion nationallicence Fujimura A. Department of Clinical Pharmacology, Jichi Medical School, Tochigi 329-04, Japan, JP aut Shiga T. Department of Clinical Pharmacology, Jichi Medical School, Tochigi 329-04, Japan, JP aut Kumagai Y. Department of Clinical Pharmacology, Jichi Medical School, Tochigi 329-04, Japan, JP aut Ohashi K. Department of Clinical Pharmacology, Jichi Medical School, Tochigi 329-04, Japan, JP aut Ebihara A. Department of Clinical Pharmacology, Jichi Medical School, Tochigi 329-04, Japan, JP aut Kotegawa T. Department of Clinical Pharmacology, Oita Medical University, Oita, Japan, JP aut https://doi.org/10.1007/s002280050114 text/html Onlinezugriff via DOI 1 research-article jats NATIONALLICENCE 856 40 https://doi.org/10.1007/s002280050114 text/html Onlinezugriff via DOI NATIONALLICENCE 700 1- Fujimura A. Department of Clinical Pharmacology, Jichi Medical School, Tochigi 329-04, Japan, JP aut NATIONALLICENCE 700 1- Shiga T. Department of Clinical Pharmacology, Jichi Medical School, Tochigi 329-04, Japan, JP aut NATIONALLICENCE 700 1- Kumagai Y. Department of Clinical Pharmacology, Jichi Medical School, Tochigi 329-04, Japan, JP aut NATIONALLICENCE 700 1- Ohashi K. Department of Clinical Pharmacology, Jichi Medical School, Tochigi 329-04, Japan, JP aut NATIONALLICENCE 700 1- Ebihara A. Department of Clinical Pharmacology, Jichi Medical School, Tochigi 329-04, Japan, JP aut NATIONALLICENCE 700 1- Kotegawa T. Department of Clinical Pharmacology, Oita Medical University, Oita, Japan, JP aut Metadata rights reserved Springer special CC-BY-NC licence nationallicence BK010053 XK010053 XK010000 NATIONALLICENCE NATIONALLICENCE NL-springer