PHARMACOKINETICS OF GM1 GANGLIOSIDE FOLLOWING PARENTERAL ADMINISTRATION

Abstract— 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 β 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 μg 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. 1990 Royal Pharmaceutical Society of Great Britain