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采用超高效液相色谱-串联质谱法比较两种剂量形式的气血双补方在大鼠体内 11 种主要生物活性成分的药代动力学。

Comparative pharmacokinetics of 11 major bioactive components between two dosage forms of Qixue Shuangbu Prescription in rats by ultra-high-performance liquid chromatography-tandem mass spectrometry.

机构信息

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

Department of Pharmacy, The Affiliated Taizhou People's Hospital of Nanjing Medical University, Taizhou, China.

出版信息

J Sep Sci. 2024 Jan;47(1):e2300677. doi: 10.1002/jssc.202300677. Epub 2023 Nov 22.

Abstract

Although Qixue Shuangbu Prescription (QSP) is a classic Chinese medicine prescription for treating chronic heart failure. Low bioavailability due to the insolubility and poor biofilm permeability of the main bioactive ingredients of QSP is still a key factor limiting its efficacy. In this study, a novel self-microemulsifying drug delivery system was proposed to effectively improve the bioavailability of QSP. The qualified ultra-high-performance liquid chromatography-tandem mass spectrometry methodology was established to investigate the pharmacokinetics characteristics of the QSP self-microemulsifying drug delivery system. Our results showed that 11 components in the self-microemulsifying drug delivery system group had prolonged T and MRT values compared with QSP extract. The Cmax of calycosin-7-glucoside (CG), vanillic acid and paeoniflorin increased 2.5 times, 2.4 times and 2.3 times, respectively. The relative bioavailability values of CG, paeoniflorin and ononin were most significantly affected, increasing by 383.2%, 336.5% and 307.1%, respectively. This study promoted the development of new dosage forms of QSP and provided a useful reference for improving dosage forms to solve the problem of low bioavailability of traditional Chinese medicine.

摘要

虽然芪血双补方(QSP)是治疗慢性心力衰竭的经典中药方剂,但由于 QSP 主要生物活性成分的不溶性和较差的生物膜通透性,其生物利用度低仍是限制其疗效的关键因素。在这项研究中,提出了一种新的自微乳药物传递系统,以有效提高 QSP 的生物利用度。建立了合格的超高效液相色谱-串联质谱法来研究 QSP 自微乳药物传递系统的药代动力学特征。我们的结果表明,自微乳药物传递系统组中的 11 种成分与 QSP 提取物相比,T 和 MRT 值延长。毛蕊异黄酮-7-葡萄糖苷(CG)、香草酸和芍药苷的 Cmax 分别增加了 2.5 倍、2.4 倍和 2.3 倍。CG、芍药苷和金雀异黄素的相对生物利用度值受影响最大,分别增加了 383.2%、336.5%和 307.1%。本研究促进了 QSP 的新剂型的发展,为解决中药生物利用度低的问题提供了改进剂型的有用参考。

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