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Home > Archive>Volume 32, Issue 1, 2022 >41-47. DOI:10. 3969 / j.issn.1671-7856. 2022. 01. 005
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Pharmacokinetic comparison of active components in an Eucommia ulmoides extract by multiple administrations between normal and spontaneously hypertensive rats
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1.Guizhou Medical University Guizhou Provincial Key Laboratory of Pharmaceutics, Guizhou Provincial Engineering Research Center for the Development and Application of Ethnic Medicine and TCM, School of Pharmacy, Guiyang 550004, China. 2. Institute of Chinese Materia Medica, China Academy of Chinese Medical Sciences, Beijing 100700

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R-33

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    Abstract:

    Objective To investigate differences in pharmacokinetics and accumulation of seven bioactive constituents, namely (+)-pinoresinol di-O-β-D-glucopyr-anoside (PDG), genipinic acid (GA), chlorogenic acid (CA), protocatechuic acid (PCA), neochlorogenic acid (NCA), cryptochlorogenic acid (CCA) and (+)-pinoresinol 4’-O-β-D- glucopyrano-side ( PG) in Eucommia ulmoides after multiple intragastric administrations between normal rats and spontaneously hypertensive rats ( SHRs). Methods Normal rats and SHRs received intragastric Eucommia ulmoides extract at a dose of 5.4 g / ( kg·d) for 7 consecutive days. Then, the pharmacokinetic parameters and tissue distribution were compared between normal rats and SHRs. Results Pharmacokinetic tests showed no obvious differences in all pharmacokinetic parameters of NCA and CCA between normal and model groups. The t1/ 2 value of PDG in SHRs was 0.26 times that of normal rats. In model group, the t1/ 2 , tmax and AUC0-t of GA were 2.20, 0.04 and 0.50 times those of normal group, respectively. For model group, the t1/ 2 value of PG was 0.55 times that of normal group. Compared with normal rats, the t1/ 2 of PCA in SHRs was increased by 2.04 times. The t1/ 2 and AUC0-t of CA in SHRs were 1.93 and 0.64 times of normal rats, respectively. Accumulation analysis showed that all representative active components were mainly distributed in the stomach, intestines, heart, liver and lungs. Except for CCA, the contents of the others in SHRs presented notable differences in tissues of two to seven compared with normal group. Conclusions The pharmacokinetics and accumulation of active anti-hypertensive components in Eucommia ulmoides extract after multiple administrations in rats were influenced remarkably by the pathological state of spontaneous hypertension. Moreover, it is important to learn about the pharmacokinetic characteristics of drugs for those who suffer from hypertension and need to take medicine persistently. This study provides a reference for clinical dosage adjustment of Eucommia ulmoides when used long-term.

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History
  • Received:October 28,2021
  • Online: March 15,2022
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