Clinical Pharmacokinetic Study of the Ultrasound Contrast Agent YM454.

Accession number;02A0852165
Title;Clinical Pharmacokinetic Study of the Ultrasound Contrast Agent YM454.
Author;OTO MASAO(National Inst. Radiological Sci., JPN)   HASEGAWA SETSUO(Sekino Rinsho Yakuri Kurinikku)   TSUTSUMI RIE(Yamanouchi Pharmaceutical Co., Ltd., JPN)   UCHIDA TAISUKE(Yamanouchi Pharmaceutical Co., Ltd., JPN)   IMAI YASUHIKO(Yamanouchi Pharmaceutical Co., Ltd., JPN)   
Journal Title;Japanese Pharmacology & Therapeutics
Journal Code:Z0947A
ISSN:0386-3603
VOL.30;NO.9;PAGE.695-702(2002)
Figure&Table&Reference;FIG.2, TBL.4, REF.2
Pub. Country;Japan
Language;Japanese
Abstract;Objectives: Two open-labeled clinical pharmacology studies of YM454, a micro-bubble ultrasound contrast agent, were conducted in healthy adult subjects to evaluate the pharmacokinetic profile of perfluoropropane (PFP), the gas component of YM454. Methods: In each study, 12 subjects (6 males, 6 females) received an intravenous injection of YM454 (50 .MU.L/kg), and the blood PFP level and the expiratory PFP excretion were measured respectively. Results: After excluding the data of 2 subjects (1 male, 1 female) whose blood PFP level was below the quantification limit at all time points, the mean blood Cmax values were 1.5 nL/mL in both gender groups and the mean blood Tmax was 72 sec (1.20 min) in males and 84 sec (1.40 min) in females. The expiratory PFP excretion was quantifiable in all of the subjects. The mean expiratory Tmax was 1.33 min in males and 1.17 min in females. The mean expiratory excretion within 20 min post-dose was 250.71 .MU.L in males and 118.53 .MU.L in females, with recovery ranging from 29.37-71.13% and from 18.89-40.63%, respectively. The recovery extrapolated to infinity ranged from 30.42-85.76% in males and 23.22-41.44% in females. A positive correlation was observed between the expiratory excretion and the ventilation rate. Conclusions: PEP was rapidly eliminated from the systemic circulation after the administration of YM454 while the expiratory PFP recovery within 20 min was less than 100%. It was suggested that the ventilation rate might have affected the expiratory PFP excretion. There were no clinically significant findings after the treatment of YM454. (author abst.)