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口服硫酸软骨素制剂中的残留硫酸角质素。

Residual keratan sulfate in chondroitin sulfate formulations for oral administration.

机构信息

Laboratório de Tecido Conjuntivo, Hospital Universitário Clementino Fraga Filho and Programa de Glicobiologia, Instituto de Bioquímica Médica, Universidade Federal do Rio de Janeiro, Cidade Universitária, Rio de Janeiro, RJ 21941-913, Brazil.

出版信息

Carbohydr Polym. 2012 Oct 1;90(2):839-46. doi: 10.1016/j.carbpol.2012.06.009. Epub 2012 Jun 16.

DOI:10.1016/j.carbpol.2012.06.009
PMID:22840010
Abstract

Chondroitin sulfate is a biomedical glycosaminoglycan (GAG) mostly used as a dietary supplement. We undertook analysis on some formulations of chondroitin sulfates available for oral administration. The analysis was based on agarose-gel electrophoresis, strong anion-exchange chromatography, digestibility with specific GAG lyases, uronic acid content, NMR spectroscopy, and size-exclusion chromatography. Keratan sulfate was detected in batches from shark cartilage, averaging ∼16% of the total GAG. Keratan sulfate is an inert material, and hazardous effects due to its presence in these formulations are unlikely to occur. However, its unexpected high percentage compromises the desired amounts of the real ingredient specified on the label claims, and forewarns the pharmacopeias to update their monographs. The techniques they recommended, especially cellulose acetate electrophoresis, are inefficient in detecting keratan sulfate in chondroitin sulfate formulations. In addition, this finding also alerts the manufacturers for improved isolation procedures as well as the supervisory agencies for better audits. Analysis based on strong anion-exchange chromatography is shown to be more reliable than the methods presently suggested by standard pharmacopeias.

摘要

硫酸软骨素是一种生物医学糖胺聚糖(GAG),主要用作膳食补充剂。我们对可口服的几种硫酸软骨素制剂进行了分析。分析基于琼脂糖凝胶电泳、强阴离子交换色谱、特定 GAG 裂解酶的消化、糖醛酸含量、NMR 光谱和尺寸排阻色谱。鲨鱼软骨中的批次检测到了角蛋白硫酸盐,平均占总 GAG 的约 16%。角蛋白硫酸盐是一种惰性物质,其在这些制剂中的存在不太可能产生有害影响。然而,其出乎意料的高比例会影响标签声称中指定的实际成分的所需量,并提醒药典更新其专论。他们推荐的技术,特别是醋酸纤维素电泳,在检测硫酸软骨素制剂中的角蛋白硫酸盐时效率不高。此外,这一发现还提醒制造商改进分离程序,以及监管机构加强审计。强阴离子交换色谱分析被证明比现行药典建议的方法更可靠。

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