Conte A, de Bernardi M, Palmieri L, Lualdi P, Mautone G, Ronca G
Istituto di Chimica Biologica, Scuola Medica, Università degli Studi di Pisa, Italy.
Arzneimittelforschung. 1991 Jul;41(7):768-72.
Chondroitin sulfate is administered as a drug to man by intravenous, intramuscular or oral route. However, few data are available on the metabolic fate of exogenous chondroitin sulfate in man. After intravenous administration of 0.5 g of chondroitin sulfate to healthy volunteers, the plasma level decreases according to a two-compartmental open model. The half-lives of distribution and elimination are 25.5 +/- 6.6 and 281 +/- 32 min, respectively. The volumes of central and tissue compartments are 6.0 +/- 1.0 and 22.9 +/- 7.7 l, respectively. More than 50% of the administered chondroitin sulfate is excreted with urine during the first 24 h as high and low molecular weight derivatives. After oral administration of 3 g of chondroitin sulfate to 12 healthy volunteers, a main peak (11.4 +/- 3.7 micrograms/ml) preceded by a lower peak is observed after 190 +/- 21 min. The elimination half-life is 363 +/- 109 min. The absolute bioavailability following oral administration calculated from AUC of plasma concentration is 13.2%. A peak of oligo- and polysaccharides with a molecular weight lower than 5000 Daltons derived from partial digestion of exogenous chondroitin sulfate is also present in plasma. These observations indicate that the metabolic fate of exogenous chondroitin sulfate is similar in man and in experimental animals.
硫酸软骨素作为一种药物，通过静脉、肌肉或口服途径施用于人体。然而，关于外源性硫酸软骨素在人体中的代谢命运，可用的数据很少。向健康志愿者静脉注射0.5克硫酸软骨素后，血浆水平根据二室开放模型下降。分布半衰期和消除半衰期分别为25.5±6.6分钟和281±32分钟。中央室和组织室的容积分别为6.0±1.0升和22.9±7.7升。超过50%的施用硫酸软骨素在最初24小时内以高分子量和低分子量衍生物的形式随尿液排出。向12名健康志愿者口服3克硫酸软骨素后，在190±21分钟后观察到一个主峰（11.4±3.7微克/毫升），之前有一个较低的峰。消除半衰期为363±109分钟。根据血浆浓度-时间曲线下面积计算，口服后的绝对生物利用度为13.2%。血浆中还存在一个由外源性硫酸软骨素部分消化产生的分子量低于5000道尔顿的寡糖和多糖峰。这些观察结果表明，外源性硫酸软骨素在人体和实验动物中的代谢命运相似。
