聚古罗糖醛酸丙酯硫酸酯钠的荧光标记及其在大鼠体内的药代动力学研究

彭霞; 刘欢#; 李建杰; 王箴言; 辛萌; 赵建春; 李春霞; 胡婷

彭霞,刘欢#,李建杰,等.聚古罗糖醛酸丙酯硫酸酯钠的荧光标记及其在大鼠体内的药代动力学研究[J].中国海洋药物,2026,(5):-.

聚古罗糖醛酸丙酯硫酸酯钠的荧光标记及其在大鼠体内的药代动力学研究

Fluorescent labeling of sodium polyguluronate propyl sulfate ester and its pharmacokinetic study in rats

投稿时间：2025-03-11 修订日期：2025-06-16

DOI：

中文关键词: PGGS 荧光标记异硫氰酸荧光素药代动力学

English Keywords:PGGS fluorescent labeling fluorescein isothiocyanate pharmacokinetics

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作者	单位	邮编
彭霞	中国海洋大学海洋药物教育部重点实验室，山东省糖科学与糖工程重点实验室，医药学院	266003
刘欢#	中国海洋大学海洋药物教育部重点实验室，山东省糖科学与糖工程重点实验室，医药学院
李建杰	1.中国海洋大学海洋药物教育部重点实验室，山东省糖科学与糖工程重点实验室，医药学院；2.青岛海洋生物医药研究院
王箴言	1.中国海洋大学海洋药物教育部重点实验室，山东省糖科学与糖工程重点实验室，医药学院；2.青岛海洋生物医药研究院
辛萌	1.中国海洋大学海洋药物教育部重点实验室，山东省糖科学与糖工程重点实验室，医药学院；2.青岛海洋生物医药研究院
赵建春	1.中国海洋大学海洋药物教育部重点实验室，山东省糖科学与糖工程重点实验室，医药学院；2.青岛海洋生物医药研究院
李春霞	1.中国海洋大学海洋药物教育部重点实验室，山东省糖科学与糖工程重点实验室，医药学院；2.青岛海洋生物医药研究院
胡婷^*	1.中国海洋大学海洋药物教育部重点实验室，山东省糖科学与糖工程重点实验室，医药学院；2.青岛海洋生物医药研究院

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中文摘要:

目的建立一种快速、灵敏的荧光标记法,用于大鼠血浆中聚古罗糖醛酸丙酯硫酸酯钠(PGGS)的含量分析,并研究PGGS在大鼠体内的药代动力学特征。方法采用异硫氰酸荧光素(FITC),通过还原胺化反应制备PGGS的荧光标记物(F-PGGS)。利用紫外可见光谱和红外光谱对F-PGGS进行结构确征。采用荧光分光光度法建立了大鼠血浆中PGGS的含量测定方法。按25 mg.kg_-1^{单剂量静脉注射给药后},测定血浆中F-PGGS含量,并应用DAS 3.0软件计算药代动力学参数。结果 F-PGGS的标记率为0.22%±0.025%,血浆中质量浓度在2~100 μg.mL_-1浓度范围内线性关系良好(R₂⁼0.9996),定量下限为2 μg.mL_-1^；低、中、高3个浓度准确度、日内及日间精密度均小于15%,且3个浓度血浆样品在室温放置6 h,-20 ℃冰箱中放置30天及反复冻融3次后均能保持稳定。大鼠单剂量尾静脉注射给予25 mg.kg_-1F-PGGS,其在血浆中的主要药代动力学参数为：AUC_(0-t)为(284.76 ±41.67)mg.L_-1^.h,T_1/2为(0.952±0.28)h,T_max为0.08 h,C_max为(324.17±45.15)mg.L_-1^。结论：该方法准确可靠,可用于PGGS等多糖的体内药代动力学研究。

English Summary:

Objective To establish a rapid and sensitive fluorescence labeling method for the determination of Propylene glycol polyguluronate sulfate sodium (PGGS) in rat plasma and to study the pharmacokinetic characteristics of PGGS in rats. Methods Fluorescein isothiocyanate (FITC) was used to prepare the fluorescent labeled PGGS (F-PGGS) through a reductive amination reaction. The structure of F-PGGS was confirmed by ultraviolet-visible spectroscopy and infrared spectroscopy. A fluorescence spectrophotometic method was developed for the determination of PGGS in rat plasma. After a single intravenous injection of 25 mg.kg^-1, the content of F-PGGS in plasma was determined, and the pharmacokinetic parameters were calculated using DAS 3.0 software. Results The labeling rate of F-PGGS was 0.22% ± 0.025%. The linear relationship of F-PGGS in plasma was excellent in the concentration range of 2-100 μg.mL-1^(r² = 0.9996), and the lower limit of quantification was 2 μg.mL^-1. The accuracy and intra- and inter-day precisions of three concentrations were all less than 15%. The plasma of three concentrations were kept at room temperature for 6h, and were stable after being placed in refrigerator at -20℃ for 30 days and repeatedly frozen and thawed for 3 times. After a single tail vein injection of 25 mg.kg^-1 F-PGGS in rats, the main pharmacokinetic parameters in plasma were as follows: AUC(0-t) was(284.76±41.67)mg.L-1^{.h, T}1/2 was(0.952±0.28)h, Tmax was 0.08 h, and Cmax was (324.17±45.15)mg.L-1^. Conclusion This method is accurate and reliable and can be used for the in vivo pharmacokinetic study of PGGS and other polysaccharides.

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