Setnikar I, Giachetti C, Zanolo G
Pharmatherapeutica. 1984;3(8):538-50.
Blood levels, tissue distribution and excretion patterns of radioactivity were studied in the rat after administration of [14C] glucosamine sulphate by the intravenous or oral route. After intravenous administration, plasma radioactivity declined in the first 30 min, then increased, reaching a peak at the 2nd hour, and disappeared, with a half-disappearance time of 28 hours. The radioactivity diffused rapidly in the tissues. Higher levels than in plasma were reached in the liver and kidneys. There was early incorporation of radioactivity in the skeletal tissues (cartilage and bone). About 50% of the administered radioactivity was excreted with the expired CO2 and about 35% with the urine. Faecal excretion was small (2% of the administered dose). After oral administration, radioactivity was quickly found in plasma, where it reached a peak at 4 hours. It then declined slowly, with biphasic kinetics. The tissue distribution, including uptake in the skeleton, repeated the pattern found after intravenous administration. There was only small faecal excretion, showing an almost complete bioavailability of glucosamine given orally, and the large excretion with the CO2 (82%) showed that glucosamine is to a large extent broken down to smaller fragments. Autoradiographic studies confirmed the tissue distribution pattern and showed in more detail the tissue localization of radioactivity.
通过静脉或口服途径给予大鼠[14C]硫酸葡萄糖胺后,研究了其放射性的血药浓度、组织分布和排泄模式。静脉给药后,血浆放射性在最初30分钟内下降,然后上升,在第2小时达到峰值,随后消失,半衰期为28小时。放射性在组织中迅速扩散。肝脏和肾脏中的放射性水平高于血浆。骨骼组织(软骨和骨骼)中早期就有放射性掺入。约50%的给药放射性随呼出的二氧化碳排出,约35%随尿液排出。粪便排泄量很少(占给药剂量的2%)。口服给药后,血浆中很快就发现了放射性,在4小时时达到峰值。然后它以双相动力学缓慢下降。组织分布,包括在骨骼中的摄取,与静脉给药后发现的模式相同。粪便排泄量很少,表明口服葡萄糖胺的生物利用度几乎完全,而随二氧化碳大量排泄(82%)表明葡萄糖胺在很大程度上分解为较小的片段。放射自显影研究证实了组织分布模式,并更详细地显示了放射性的组织定位。