Chang Chuck, Ibi Afoke, Zhang Yiming, Du Min, Roh Yoon Seok, O'Brien Robert, Solnier Julia
Clinical Research, ISURA, Burnaby, BC V3N 4S9, Canada.
Biology Department, University of British Columbia, Kelowna, BC V1V 1V7, Canada.
Nutrients. 2025 Jul 30;17(15):2491. doi: 10.3390/nu17152491.
: Crystalline glucosamine sulfate (cGS) claims to be a stabilized form of glucosamine sulfate with a defined crystalline structure intended to enhance chemical stability. It is proposed to offer pharmacokinetic advantages over regular glucosamine sulfate (rGS) which is stabilized with potassium or sodium chloride. However, comparative human bioavailability data are limited. Since both forms dissociate in gastric fluid into constituent ions, the impact of cGS formulation on absorption remains uncertain. This pilot study aimed to compare the bioavailability of cGS and rGS using a randomized, double-blind, crossover design. : Ten healthy adults received a single 1500 mg oral dose of either cGS or rGS with a 7-day washout between interventions. Capillary blood samples were collected over 24 h. Glucosamine and its metabolite concentrations were quantified by Liquid Chromatography-High Resolution Mass Spectrometry (LC-HRMS), and pharmacokinetic parameters-including maximum concentration (C), time to reach C (T), and area under the curve (AUC)-were calculated. : Mean AUC, C, T, and T values for glucosamine and glucosamine-6-sulfate (GlcN-6-S) were comparable between cGS and rGS. Although the AUC for glucosamine was modestly higher with rGS (18,300 ng·h/mL) than with cGS (12,900 ng·h/mL), the difference was not statistically significant ( = 0.136). GlcN-6-S exposure was also similar between formulations (rGS: 50,700 ng·h/mL; cGS: 50,600 ng·h/mL), with a geometric mean ratio of 1.39, a delayed T (6-8 h) and longer half-life, consistent with its role as a downstream metabolite. N-acetylglucosamine levels remained stable, indicating potential homeostatic regulation. : This pilot study found no significant pharmacokinetic advantage of cGS over rGS. These preliminary findings challenge claims of cGS' pharmacokinetic superiority, although the small sample size limits definitive conclusions. Larger, adequately powered studies are needed to confirm these results.
结晶型硫酸葡萄糖胺（cGS）据称是一种具有特定晶体结构的硫酸葡萄糖胺稳定形式，旨在提高化学稳定性。有人提出，与用氯化钾或氯化钠稳定的普通硫酸葡萄糖胺（rGS）相比，它具有药代动力学优势。然而，关于人体的比较生物利用度数据有限。由于两种形式在胃液中都会解离成组成离子，cGS制剂对吸收的影响仍不确定。这项初步研究旨在采用随机、双盲、交叉设计比较cGS和rGS的生物利用度。10名健康成年人单次口服1500毫克cGS或rGS，两次干预之间有7天的洗脱期。在24小时内采集毛细血管血样。通过液相色谱-高分辨率质谱（LC-HRMS）对葡萄糖胺及其代谢物浓度进行定量，并计算药代动力学参数，包括最大浓度（C）、达到C的时间（T）和曲线下面积（AUC）。cGS和rGS之间葡萄糖胺和硫酸葡萄糖胺-6-硫酸盐（GlcN-6-S）的平均AUC、C、T和T值具有可比性。虽然rGS（18300 ng·h/mL）的葡萄糖胺AUC略高于cGS（12900 ng·h/mL），但差异无统计学意义（P = 0.136）。两种制剂之间的GlcN-6-S暴露也相似（rGS：50700 ng·h/mL；cGS：50600 ng·h/mL），几何平均比为1.39，T延迟（6 - 8小时）且半衰期更长，这与其作为下游代谢物的作用一致。N-乙酰葡萄糖胺水平保持稳定，表明存在潜在的稳态调节。这项初步研究发现cGS相对于rGS没有显著的药代动力学优势。这些初步发现对cGS药代动力学优越性的说法提出了挑战，尽管样本量小限制了得出确定性结论。需要更大规模、有足够效力的研究来证实这些结果。
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