Wang Hai-yan, Yang Jun, Yin Wang, Yang Ling-hui, Zhang Wen-sheng
Sichuan Da Xue Xue Bao Yi Xue Ban. 2015 Mar;46(2):214-7.
To estimate the median effective dose (EDs0) of oral administrated HX0969w, fospropofol disodium and propofol emulsion in rats, and to compare the sedative-hypnotic effects and safety of the three drugs.
The ED50 of the three drugs were determined using sequential method. Thirty healthy adult Sprague-Dawley rats were divided into three groups randomly, being orally administered with HX0969w (n=10), fospropofol disodium (n=10) and propofol emulsion (n=10), respectively. The neurobehavioral performance of the rats was observed. The time of loss of forepaw righting reflex (LRR) and the time of recovery of forepaw righting reflex (RRR) were recorded.
The ED50 of oral HX0969w, fospropofol disodium and propofol emulsion were 96.5 mg/kg, 130.0 mg/kg and 113.8 mg/kg, respectively. HX0969w, fospropofol disodium and propofol emulsion had a mean LRR of (10.0 +/- 2.9) min,(7.5 +/- 2.8) min and (16.0 +/- 5.9) min; respectively; and a mean RRR of (66.9 +/- 21.5) min, (131.9 +/- 32.7) min and (198.9 +/- 110.0) min, respectively.
HX0969w, fospropofol disodium and propofol emulsion can produce sedative-hypnotic effects and they are safe when administered by oral route. The two propofol prodrugs HX0969w and fospropofol disodium have shorter LRR than propofol emulsion. HX0969w also has a shorter RRR than fospropofol disodium and propofol emulsion.
评估大鼠口服HX0969w、丙泊酚二钠和丙泊酚乳剂的半数有效剂量（ED50），并比较这三种药物的镇静催眠效果及安全性。
采用序贯法测定三种药物的ED50。将30只健康成年Sprague-Dawley大鼠随机分为三组，分别口服HX0969w（n = 10）、丙泊酚二钠（n = 10）和丙泊酚乳剂（n = 10）。观察大鼠的神经行为表现，记录右前肢翻正反射消失时间（LRR）和右前肢翻正反射恢复时间（RRR）。
口服HX0969w、丙泊酚二钠和丙泊酚乳剂的ED50分别为96.5 mg/kg、130.0 mg/kg和113.8 mg/kg。HX0969w、丙泊酚二钠和丙泊酚乳剂的平均LRR分别为（10.0±2.9）分钟、（7.5±2.8）分钟和（16.0±5.9）分钟；平均RRR分别为（66.9±21.5）分钟、（131.9±32.7）分钟和（198.9±110.0）分钟。
HX0969w、丙泊酚二钠和丙泊酚乳剂可产生镇静催眠作用，口服给药安全。两种丙泊酚前体药物HX0969w和丙泊酚二钠的LRR比丙泊酚乳剂短。HX0969w的RRR也比丙泊酚二钠和丙泊酚乳剂短。
