Jantzen J P, Erdmann K, Witton P K, Klein A M
Anaesthesist. 1986 Aug;35(8):496-9.
The factors underlying the unpredictability of the pharmacokinetics of rectally administered methohexitone remain unclear. The "pH partition hypothesis" offers an explanation. We investigated six children with rectal pH values ranging from 7.5 to 9.8, who were given 25 mg/kg methohexitone 10% via the rectal route under general anaesthesia. Blood samples were taken at zero, 3, 5, 7, 10, 15, 20, 30, 40, 60, 90 and 120 min; rectal pH was measured at zero and 1 min. The methohexitone plasma levels reached a maximum (Cmax) of 2.63 micrograms/ml (median) after 17.5 min (median). The elimination half-life ranged from 37 to 218 min. No positive correlation between lower pH and better resorption (AUC and Cmax) was found. The resorption kinetics of rectally administered methohexitone cannot be explained by its electrochemical properties alone.
直肠给药美索比妥药代动力学不可预测性背后的因素仍不清楚。“pH分配假说”提供了一种解释。我们研究了6名直肠pH值在7.5至9.8之间的儿童,他们在全身麻醉下经直肠途径给予25mg/kg的10%美索比妥。在0、3、5、7、10、15、20、30、40、60、90和120分钟采集血样;在0和1分钟测量直肠pH值。美索比妥血浆水平在17.5分钟(中位数)后达到最大值(Cmax)2.63微克/毫升(中位数)。消除半衰期为37至218分钟。未发现较低pH值与更好的吸收(AUC和Cmax)之间存在正相关。直肠给药美索比妥的吸收动力学不能仅由其电化学性质来解释。