Girard M, Granier F, Schmitt L, Cotonat J, Escande M, Blanc M
Encephale. 1984;10(4):171-6.
Plasma kinetics of pipotiazine have been studied in ten schizophrenic patients after oral administration of single dose of pipotiazine at 7 a.m. (30 mg, drops). Peak plasma concentrations are reached one hour after administration (41.8 +/- 19,9 ng/ml) and then rapidly decline until 24 h (2.2 +/- 1.2 ng/ml). During the following days plasma concentrations remain stable at the same sampling times. After 3 days wash-out and first intramuscular injection of pipotiazine palmitate (100 mg) main pharmacokinetic data are found: plasma concentrations of pipotiazine are not detectable during at less 3 days after injection, maximal drug level is attained during second week after i.m. (1.7 +/- 0.9 ng/ml). A period of decline is then recorded. Furthermore the mean ratio between pipotiazine plasma concentration after oral and i.m. administration is about 20. When pipotiazine palmitate is given every fourth week, steady state seems to be reached as early as the second month.
在10例精神分裂症患者中,于上午7点口服单剂量哌泊噻嗪(30mg,滴剂)后研究了其血浆动力学。给药后1小时达到血浆峰值浓度(41.8±19.9ng/ml),然后迅速下降,直至24小时(2.2±1.2ng/ml)。在随后几天,相同采样时间的血浆浓度保持稳定。经过3天洗脱期后首次肌内注射棕榈酸哌泊噻嗪(100mg),得到主要药代动力学数据:注射后至少3天内未检测到哌泊噻嗪血浆浓度,肌内注射后第二周达到最大药物水平(1.7±0.9ng/ml)。随后记录到一个下降期。此外,口服和肌内注射后哌泊噻嗪血浆浓度的平均比值约为20。当每四周给予棕榈酸哌泊噻嗪时,最早在第二个月似乎达到稳态。