Herrstedt J, Jørgensen M, Angelo H R, Rassing M R, Møller-Sonnergaard J, Dombernowsky P
Department of Oncology, Herlev Hospital, University of Copenhagen, Denmark.
Br J Clin Pharmacol. 1996 Jun;41(6):613-5. doi: 10.1046/j.1365-2125.1996.35220.x.
The absorption of the antiemetic metopimazine (MPZ) given as a single dose of (a) 40 mg microenema, (b) 40 mg orally and (c) 10 mg as a 60 min i.v. continuous infusion was investigated in six healthy volunteers. Blood samples were drawn and the serum concentrations of MPZ and its acid metabolite were measured. The bioavailability of MPZ given orally and as enemas was 22.3 and 19.5% respectively. Partial avoidance of hepatic first pass metabolism was seen with the enemas, which in contrast to suppositories, seems to represent a reliable form of rectal administration.
在6名健康志愿者中研究了单剂量给予（a）40mg微灌肠剂、（b）40mg口服和（c）10mg静脉连续输注60分钟的止吐药美托哌丙嗪（MPZ）的吸收情况。采集血样并测定MPZ及其酸性代谢物的血清浓度。口服和灌肠给予MPZ的生物利用度分别为22.3%和19.5%。灌肠剂可部分避免肝脏首过代谢，与栓剂不同，灌肠剂似乎是一种可靠的直肠给药方式。
