Phase i study of beraprost sodium (TRK-100), a prostacyclin derivative-Single oral administration study.:Single Oral Administration Study
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A phase I study by single oral administration of beraprost sodium (TRK-100), a prostacyclin derivative, was performed in 32 healthy male volunteers. The safety, pharmaco-kinetics, and pharmacological effects were studied in two single oral administration clinical trials.<BR>Study 1 was performed in 12 volunteers to investigate the safety and pharmacokinetics of TRK-100. The 12 men received 50, 100, and 200 μg of TRK-100 at intervals of two wk.<BR>Study 2 was performed in 20 volunteers, randomly divided into three groups, to investigate the pharmacological effects and safety of TRK-100 at the dose of 25, 50, and 100μg. The results were as follows:<BR>1) Subjective symptoms: Facial flushing, feeling of congestion, dull headache, headache, and sleepiness, etc., appeared in some subjects. These symptoms were observed more frequently in the groups receiving 100 and 200μg. Almost all symptoms disappeared within 2 or 3 hr after administration.<BR>2) Physical and laboratory tests: Plasma calcification time and prothrombin time were prolonged slightly. But no abnormality was observed in other test items.<BR>3) Pharmacokinetics: Following a single oral administration of 100 and 200μg, C<SUB>max</SUB> was twice as high in the group receiving 200μg as in the group receiving 100μg. T<SUB>max</SUB> was 1. 42 hr in the group receiving 100μg and 1.07 hr in the group receiving 200μg. T<SUB>1/2</SUB> was 1.11 hr and 0.89 hr, respectively.<BR>4) Pharmacological effect: TRK-100 inhibited platelet aggregation induced by ADP, collagen, and epinephrine dose-dependently.<BR>The above results indicated the safety and pharmacological effects of TRK-100 in single oral administration in healthy male volunteers.
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