Santos Gustavo R C, Piquet Adriana A, Glauser Bianca F, Tovar Ana M F, Pereira Mariana S, Vilanova Eduardo, Mourão Paulo A S
Laboratório de Tecido Conjuntivo, Hospital Universitário Clementino Fraga Filho and Instituto de Bioquímica Médica Leopoldo de Meis, Universidade Federal do Rio de Janeiro (UFRJ), P.O. Box 68041, Rio de Janeiro RJ 21941-913, Brazil.
Pharmaceuticals (Basel). 2017 Apr 1;10(2):38. doi: 10.3390/ph10020038.
Glycosaminoglycans are carbohydrate-based compounds widely employed as nutraceuticals or prescribed drugs. Oral formulations of chondroitin sulfate combined with glucosamine sulfate have been increasingly used to treat the symptoms of osteoarthritis and osteoarthrosis. The chondroitin sulfate of these combinations can be obtained from shark or bovine cartilages and hence presents differences regarding the proportions of 4- and 6-sulfated -acetyl β-d-galactosamine units. Herein, we proposed a systematic protocol to assess pharmaceutical batches of this combination drug. Chemical analyses on the amounts of chondroitin sulfate and glucosamine in the batches were in accordance with those declared by the manufacturers. Anion-exchange chromatography has proven more effective than electrophoresis to determine the type of chondroitin sulfate present in the combinations and to detect the presence of keratan sulfate, a common contaminant found in batches prepared with shark chondroitin sulfate. 1D NMR spectra revealed the presence of non-sulfated instead of sulfated glucosamine in the formulations and thus in disagreement with the claims declared on the label. Moreover, 1D and 2D NMR analyses allowed a precise determination on the chemical structures of the chondroitin sulfate present in the formulations. The set of analytical tools suggested here could be useful as guidelines to improve the quality of this medication.
糖胺聚糖是一类基于碳水化合物的化合物，被广泛用作营养保健品或处方药。硫酸软骨素与硫酸葡萄糖胺的口服制剂越来越多地用于治疗骨关节炎和骨关节病的症状。这些组合中的硫酸软骨素可从鲨鱼或牛软骨中获得，因此在4-硫酸化和6-硫酸化的N-乙酰-β-D-半乳糖胺单元的比例上存在差异。在此，我们提出了一种系统的方案来评估这种复方药物的批次。对批次中硫酸软骨素和葡萄糖胺含量的化学分析与制造商宣称的一致。阴离子交换色谱已被证明比电泳更有效地确定组合中存在的硫酸软骨素类型，并检测硫酸角质素的存在，硫酸角质素是用鲨鱼硫酸软骨素制备的批次中常见的污染物。一维核磁共振谱显示制剂中存在未硫酸化而非硫酸化的葡萄糖胺，因此与标签上宣称的内容不一致。此外，一维和二维核磁共振分析能够精确确定制剂中硫酸软骨素的化学结构。这里建议的这套分析工具可作为提高这种药物质量的指导方针。
