Pharmacokinetics and pharmacodynamics of long-acting capsule of carteolol hydrochloride.
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Pharmacokinetics and pharmacodynamics of long-acting (LA) capsule of carteololhydrochloride were investigated in healthy adult male volunteers in the two comparisonstudies;<BR>Study I: Comparison with single administration of 15 mg/person of LA and conventionaltablets (CT) under fasting condition<BR>Study II: Comparison with single administration of 15 mg/person of LA and separateadministration of CT, 5mg/person, three times a day after meals<BR>In study I, AUC was not significantly different between LA and CT, while C<SUB>max</SUB> of LA was significantly lower than that of CT. The long-acting profile of LA was establishedfrom the prolongation of pharmacokinetic parameters; Tmax t<SUB>1/2</SUB>, MRT and VRT of LAwere significantly longer than those of CT.<BR>In study II, C<SUB>max</SUB> of LA was not significantly different from that of CT. The pharmacodynamic indexes, heart rate, systolic blood pressure and double product during exercise, were not significantly different between the two groups.<BR>The urinary excretion curves in study I and II supported the plasma concentration.<BR>Pharmacokinetics of LA were not influenced by food consumption, since the pharmacokinetic parameters of LA did not differ significantly in study I and II.<BR>In conclusion, a once-daily administration by LA is proposed as being clinically useful.
- 一般社団法人 日本臨床薬理学会の論文
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- 塩酸ブプレノルフィン坐剤の臨床第1相試験
- Pharmacokinetics and pharmacodynamics of long-acting capsule of carteolol hydrochloride.