Cornelli U, Panucci A, Zingali G, Kirschner G, Baggio C, Cogo R
Fidia Research Laboratories, Abano Terme, Padova, Italy.
J Pharm Pharmacol. 1990 Oct;42(10):708-11. doi: 10.1111/j.2042-7158.1990.tb06564.x.
The pharmacokinetic parameters of monosialotetrahexosylganglioside (GM1) have been determined in healthy volunteers at 3 dose levels: 100, 200, 300 mg. Each dose was administered to separate groups of 12 volunteers. GM1 levels were determined in plasma, urine, and faeces by a method based on the property of the cholera toxin beta subunit to react specifically with GM1 ganglioside. A non-compartmental model was applied to determine standard pharmacokinetic parameters. The average AUC increased with dose (1002 +/- 121.2, 1306 +/- 146.1, 3155 +/- 121.6 micrograms mL-1 h after 100, 200, 300 mg, respectively). Plasma clearance was less than 3 mL min-1 and the distribution volume was close to the plasma volume (on average between 4.3 and 7.2 L). Mean residence time was about 43 h for all doses. GM1 was not detected in urine, while in faeces the amount of GM1 determined was similar to the baseline values obtained before dosing.
已在健康志愿者中测定了单唾液酸四己糖神经节苷脂（GM1）在3个剂量水平（100、200、300毫克）下的药代动力学参数。每个剂量分别给予12名志愿者组成的不同组。通过基于霍乱毒素β亚基与GM1神经节苷脂特异性反应特性的方法测定血浆、尿液和粪便中的GM1水平。应用非房室模型来确定标准药代动力学参数。平均AUC随剂量增加（100毫克、200毫克、300毫克后分别为1002±121.2、1306±146.1、3155±121.6微克·毫升-1·小时）。血浆清除率小于3毫升·分钟-1，分布容积接近血浆容积（平均在4.3至7.2升之间）。所有剂量的平均驻留时间约为43小时。尿液中未检测到GM1，而粪便中测定的GM1量与给药前获得的基线值相似。
