Talent J M, Gracy R W
Department of Biochemistry and Molecular Biology, University of North Texas Health Science Center, Fort Worth, USA.
Clin Ther. 1996 Nov-Dec;18(6):1184-90. doi: 10.1016/s0149-2918(96)80073-7.
Glucosamine and its derivatives, such as glucosamine sulfate and N-acetyl-D-glucosamine (NAG), have been shown to be effective in the treatment of patients with osteoarthritis. Unfortunately, the half-life of glucosamine in the blood is relatively short; therefore, a sustained-release form of the compound would be highly desirable. The purpose of this pilot study was to determine whether the polymeric form of NAG (POLY-Nag) could provide a longer-lasting oral source of NAG. Ten healthy subjects each ingested 1 g/d of either NAG or POLY-Nag for 3 days. After a 4-day washout period, each subject was crossed over to receive the other compound for 3 days. Serum samples were collected and analyzed using high-performance liquid chromatography. Results show that orally ingested NAG and POLY-Nag are absorbed, resulting in increased serum levels of NAG, and POLY-Nag appears to be at least as effective as NAG. Serum levels of NAG had decreased by 48 hours after cessation of ingestion of NAG or POLY-Nag but were still above baseline levels. Increases in serum glucosamine levels indicate that NAG and POLY-Nag are converted to glucosamine in vivo. In conclusion, POLY-Nag may provide a source of serum glucosamine for treatment of patients with osteoarthritis. Longer and more rigorous pharmaco-kinetic and clinical studies need to be done.
氨基葡萄糖及其衍生物，如硫酸氨基葡萄糖和N-乙酰-D-氨基葡萄糖（NAG），已被证明对骨关节炎患者的治疗有效。不幸的是，氨基葡萄糖在血液中的半衰期相对较短；因此，该化合物的缓释形式将非常受欢迎。这项初步研究的目的是确定NAG的聚合物形式（POLY-Nag）是否能提供更持久的口服NAG来源。10名健康受试者每人每天摄入1克NAG或POLY-Nag，持续3天。经过4天的洗脱期后，每位受试者交叉接受另一种化合物，持续3天。采集血清样本并使用高效液相色谱法进行分析。结果表明，口服摄入的NAG和POLY-Nag被吸收，导致血清NAG水平升高，并且POLY-Nag似乎至少与NAG一样有效。停止摄入NAG或POLY-Nag后48小时，血清NAG水平下降，但仍高于基线水平。血清氨基葡萄糖水平的升高表明NAG和POLY-Nag在体内转化为氨基葡萄糖。总之，POLY-Nag可能为骨关节炎患者的治疗提供血清氨基葡萄糖来源。需要进行更长时间、更严格的药代动力学和临床研究。
