Abstract：
BACKGROUND: Panax notoginseng saponins (PNS), as the main active component of Panax notoginseng, shows broad pharmacological effects but with low oral bioavailability. Borneol (BO) is commonly used as an adjuvant drug in the field of traditional Chinese medicine, which has been proven to facilitate the absorption of ginsenosides such as Rg1 and Rb1 in vivo. The presence of chiral carbons has resulted in three optical isomers of BO commercially available in the market, all of which are documented by national standards.
OBJECTIVE: This study aimed to investigate the role of BO in promoting the oral absorption of PNS from the perspective of optical configuration and compatibility ratios.
METHODS: In this study, an ultra-performance liquid chromatography coupled with triple quadrupole-linear ion trap tandem mass spectrometry (UPLC-QTRAP-MS/MS) method was validated and applied to determine the concentrations of five main saponins in PNS in rat plasma. The kinetic characteristics of PNS were compared when co-administered with BO based on optical isomerism and different compatibility ratios.
RESULTS: The results showed that BO promoted the exposure of PNS in rats. Three forms of BO, namely d-borneol (DB), l-borneol (LB), and synthetic borneol (SB), exhibited different promotion strengths. SB elevated PNS exposure in rats more than DB or LB. It is also interesting to note that under different compatibility ratios, SB can exert a strong promoting effect only when PNS and BO were combined in a 1:1 ratio (PNS 75 mg/kg; BO 75 mg/kg). As a pharmacokinetic booster, the dosage of BO is worthy of consideration and should follow the traditional medication principles of Chinese medicine.
CONCLUSIONS: This study shed new light on the compatible use of PNS and BO from the perspective of \"configuration-dose-influence\" of BO. The results provide important basis for the clinical application and selection of BO.
OBJECTIVE: This study aimed to investigate the role of BO in promoting the oral absorption of PNS from the perspective of optical configuration and compatibility ratios.
METHODS: In this study, an ultra-performance liquid chromatography coupled with triple quadrupole-linear ion trap tandem mass spectrometry (UPLC-QTRAP-MS/MS) method was validated and applied to determine the concentrations of five main saponins in PNS in rat plasma. The kinetic characteristics of PNS were compared when co-administered with BO based on optical isomerism and different compatibility ratios.
RESULTS: The results showed that BO promoted the exposure of PNS in rats. Three forms of BO, namely d-borneol (DB), l-borneol (LB), and synthetic borneol (SB), exhibited different promotion strengths. SB elevated PNS exposure in rats more than DB or LB. It is also interesting to note that under different compatibility ratios, SB can exert a strong promoting effect only when PNS and BO were combined in a 1:1 ratio (PNS 75 mg/kg; BO 75 mg/kg). As a pharmacokinetic booster, the dosage of BO is worthy of consideration and should follow the traditional medication principles of Chinese medicine.
CONCLUSIONS: This study shed new light on the compatible use of PNS and BO from the perspective of \"configuration-dose-influence\" of BO. The results provide important basis for the clinical application and selection of BO.
摘要：
背景：三七总皂苷（PNS），作为三七的主要活性成分，显示广泛的药理作用，但口服生物利用度低。冰片(BO)是中药领域常用的辅助药物,已被证明促进人参皂苷如Rg1和Rb1在体内的吸收。手性碳的存在导致市场上可商购的BO的三种光学异构体，所有这些都是由国家标准记录。
目的：本研究旨在从光学构型和配伍比的角度探讨BO在促进PNS口服吸收中的作用。
方法：在本研究中，验证了超高效液相色谱-三重四极杆-线性离子阱串联质谱（UPLC-QTRAP-MS/MS）方法，并将其用于测定大鼠血浆中PNS中5种主要皂苷的浓度。基于光学异构现象和不同的相容性比，比较了与BO共同给药时PNS的动力学特征。
结果：结果显示BO促进大鼠PNS的暴露。BO的三种形式，即d-冰片(DB)，l-冰片（LB），和合成冰片（SB），表现出不同的晋升优势。SB比DB或LB升高大鼠的PNS暴露。同样有趣的是，在不同的兼容比例下，只有当PNS和BO以1:1的比例(PNS75mg/kg;BO75mg/kg)组合时,SB才能发挥强的促进作用。作为药代动力学的助推器，BO的用量值得考虑,应遵循中医传统用药原则。
结论：这项研究从BO的“配置-剂量-影响”的角度为PNS和BO的兼容使用提供了新的思路。研究结果为BO的临床应用和选择提供了重要依据。
目的：本研究旨在从光学构型和配伍比的角度探讨BO在促进PNS口服吸收中的作用。
方法：在本研究中，验证了超高效液相色谱-三重四极杆-线性离子阱串联质谱（UPLC-QTRAP-MS/MS）方法，并将其用于测定大鼠血浆中PNS中5种主要皂苷的浓度。基于光学异构现象和不同的相容性比，比较了与BO共同给药时PNS的动力学特征。
结果：结果显示BO促进大鼠PNS的暴露。BO的三种形式，即d-冰片(DB)，l-冰片（LB），和合成冰片（SB），表现出不同的晋升优势。SB比DB或LB升高大鼠的PNS暴露。同样有趣的是，在不同的兼容比例下，只有当PNS和BO以1:1的比例(PNS75mg/kg;BO75mg/kg)组合时,SB才能发挥强的促进作用。作为药代动力学的助推器，BO的用量值得考虑,应遵循中医传统用药原则。
结论：这项研究从BO的“配置-剂量-影响”的角度为PNS和BO的兼容使用提供了新的思路。研究结果为BO的临床应用和选择提供了重要依据。
