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采用 UPLC-MS/MS 同时定量测定 7 种皂苷的大鼠生晒和蒸制根的比较药代动力学分析。

Comparative pharmacokinetic analysis of raw and steamed roots in rats by UPLC-MS/MS for simultaneously quantifying seven saponins.

机构信息

College of Pharmacy, Nanjing University of Chinese Medicine, Nanjing, PR China.

Key Research Laboratory of Chinese Medicine Processing of Jiangsu Province, Nanjing University of Chinese Medicine, Nanjing, PR China.

出版信息

Pharm Biol. 2021 Dec;59(1):653-661. doi: 10.1080/13880209.2021.1928239.

Abstract

CONTEXT

After being steamed, the restorative effects of (Burk.) F. H. Chen (Araliaceae) will be strengthened. However, the underlying mechanism remains elusive.

OBJECTIVE

To compare the pharmacokinetics of ginsenosides Rg, Rb, Rd, Re, Rg, Rk, notoginsenoside R (GRg, GRb, GRd, GRe, GRg, GRk and NGR) in the raw and steam-processed (RPN and SPN).

MATERIALS AND METHODS

The pharmacokinetics of seven components after oral administration of SPN and RPN extracts (1.0 g/kg) were investigated, respectively, in SD rats (two groups,  = 6) using UPLC-MS/MS.

RESULTS

The approach elicited good linear regression ( > 0.991). The accuracy, precision and stability were all within ± 15%. The extraction recoveries and matrix effects were 75.0-100.8% and 85.1-110.3%, respectively. Compared with the RPN group, AUC of GRg (176.63 ± 42.49 ng/h/mL), GRb (5094.06 ± 1453.14 ng/h/mL), GRd (1396.89 ± 595.14 ng/h/mL), and NGR (135.95 ± 54.32 ng/h/mL), along with of GRg (17.41 ± 5.43 ng/mL), GRb (361.48 ± 165.57 ng/mL), GRd (62.47 ± 33.65 ng/mL) and NGR (23.97 ± 16.77 ng/mL) decreased remarkably with oral administration of the SPN extracts, while GRe showed no significantly difference. Of note, GRg and GRk could not be detected in the plasma.

CONCLUSIONS

Influence of the processing reduced the systemic exposure levels to GRg, GRb, GRd and NGR. It is the first report of comparative pharmacokinetic study of multiple saponins analysis after oral administration of RPN and SPN extract, which might be helpful for further studies on its steam-processing mechanism.

摘要

上下文

经过蒸制后,(Burk.)F. H. Chen(伞形科)的修复效果将会增强。然而,其潜在机制仍不清楚。

目的

比较生品和蒸制品(RPN 和 SPN)中人参皂苷 Rg、Rb、Rd、Re、Rg、Rk、三七皂苷 R(GRg、GRb、GRd、GRe、GRg、GRk 和 NGR)的药代动力学。

材料和方法

采用 UPLC-MS/MS 法分别检测 SD 大鼠(两组,n = 6)口服 SPN 和 RPN 提取物(1.0 g/kg)后 7 种成分的药代动力学。

结果

该方法的线性回归良好(>0.991)。准确度、精密度和稳定性均在±15%范围内。提取回收率和基质效应分别为 75.0-100.8%和 85.1-110.3%。与 RPN 组相比,GRg(176.63 ± 42.49 ng/h/mL)、GRb(5094.06 ± 1453.14 ng/h/mL)、GRd(1396.89 ± 595.14 ng/h/mL)和 NGR(135.95 ± 54.32 ng/h/mL)的 AUC 以及 GRg(17.41 ± 5.43 ng/mL)、GRb(361.48 ± 165.57 ng/mL)、GRd(62.47 ± 33.65 ng/mL)和 NGR(23.97 ± 16.77 ng/mL)的 显著降低,而 GRe 无显著差异。值得注意的是,血浆中未检测到 GRg 和 GRk。

结论

炮制的影响降低了系统暴露于 GRg、GRb、GRd 和 NGR 的水平。这是首次报道口服 RPN 和 SPN 提取物后多种皂苷的比较药代动力学研究,这可能有助于进一步研究其蒸制机制。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/54b4/8172216/dbc7f1d21f66/IPHB_A_1928239_F0001_C.jpg

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