Comparative pharmacokinetics of four active components on normal and diabetic rats after oral administration of Gandi capsules

Xu, Renjie; Jia, Qi; Zhan, Ruan-Juan; Zhou, Guisheng; Hao, Bin; Ma, Jianhua; Wei, Xin; Xu, Ajing; Zhang, Jian

doi:10.1039/c7ra11420f

Cited by 7 publications

(8 citation statements)

References 35 publications

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“…The P app values determined in the present study indicated good intestinal absorption of loganin. At first instance this high permeability observed in the Caco-2 model seems to be inconsistent with the previously reported low oral bioavailability of loganin [11]. Besides its low water solubility, a strong metabolism may be regarded as the major cause of the low oral bioavailability of loganin in vivo.…”

Section: Resultsmentioning

confidence: 57%

“…Chromatographic and mass spectrometry detection were performed according to a previous method [11]. Briefly, loganin and puerarin (internal standard, IS) were isolated using a ZORBAX Eclipse Plus C 18 column (50 mm × 2.1 mm, 1.8 μ m) with an API5500 triple-quadrupole mass spectrometer (Applied Biosystems-SCIEX, Concord, Canada).…”

Section: Methodsmentioning

confidence: 99%

“…Unfortunately, these pharmacological activities of loganin are curtailed due to its low oral bioavailability [11]. Analogously to other iridoid glycosides, it is well known that loganin exhibits low water solubility which limits its absorption and bioavailability.…”

Section: Introductionmentioning

confidence: 99%

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Elucidation of the Intestinal Absorption Mechanism of Loganin in the Human Intestinal Caco‐2 Cell Model

Yuan

Jia

et al. 2018

Evidence-Based Complementary and Alternative Medicine

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Loganin, iridoid glycosides, is the main bioactive ingredients in the plant Strychnos nux-vomica L. and demonstrates various pharmacological effects, though poor oral bioavailability in rats. In this study, the intestinal absorption mechanism of loganin was investigated using the human intestinal Caco-2 cell monolayer model in both the apical-to-basolateral (A-B) and the basolateral-to-apical (B-A) direction; additionally, transport characteristics were systematically investigated at different concentrations, pHs, temperatures, and potential transporters. The absorption permeability (PappAB) of loganin, which ranged from 12.17 to 14.78 × 10−6cm/s, was high at four tested concentrations (5, 20, 40, and 80μM), while the major permeation mechanism of loganin was found to be passive diffusion with active efflux mediated by multidrug resistance-associated protein (MRP) and breast cancer resistance protein (BCRP). In addition, it was found that loganin was not the substrate of efflux transporter P-glycoprotein (P-gp) since the selective inhibitor (verapamil) of the efflux transporter exhibited little effects on the transport of loganin in the human intestinal Caco-2 cells. Meanwhile, transport from the apical to the basolateral side increased 2.09-fold after addition of a MRP inhibitor and 2.32-fold after addition of a BCRP inhibitor. In summary, our results clearly demonstrate, for the first time, a good permeability of loganin in the human intestinal Caco-2 cell model and elucidate, in detail, the intestinal absorption mechanism and the effects of transporters on iridoid glycosides compounds.

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Section: Resultsmentioning

confidence: 57%

Section: Methodsmentioning

confidence: 99%

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Elucidation of the Intestinal Absorption Mechanism of Loganin in the Human Intestinal Caco‐2 Cell Model

Yuan

Jia

et al. 2018

Evidence-Based Complementary and Alternative Medicine

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“…The exposure of baicalin and also of wogonin and wogonoside was significantly higher in diabetic rats (models induced with streptozotocin) than in healthy rats, and this seemed to be related not to an increase of absorption (the intestinal permeability for baicalin rather decreased), but to an increase in the activity of β-glucuronidase [270,271,272,273,274,275]; a delay in gastric emptying and thus prolongation of the mean residence time in the gastro-intestinal tract of the flavones was also suggested as possibly contributing to this increase in exposure in diabetic animals [275]. A similar effect was also reported in diabetic mice (model of diabetes used in the experiment not reported), the sample of which also contained oroxylin A and baicalin (unlike the non-diabetic mice used as a control) [276].…”

Section: Intra-species Differences (Pk Variability)mentioning

confidence: 99%

Pharmacokinetics of B-Ring Unsubstituted Flavones

et al. 2019

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B-ring unsubstituted flavones (of which the most widely known are chrysin, baicalein, wogonin, and oroxylin A) are 2-phenylchromen-4-one molecules of which the B-ring is devoid of any hydroxy, methoxy, or other substituent. They may be found naturally in a number of herbal products used for therapeutic purposes, and several have been designed by researchers and obtained in the laboratory. They have generated interest in the scientific community for their potential use in a variety of pathologies, and understanding their pharmacokinetics is important for a grasp of their optimal use. Based on a comprehensive survey of the relevant literature, this paper examines their absorption (with deglycosylation as a preliminary step) and their fate in the body, from metabolism to excretion. Differences among species (inter-individual) and within the same species (intra-individual) variability have been examined based on the available data, and finally, knowledge gaps and directions of future research are discussed.

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“…Furthermore, most studies concentrated on the pharmacokinetic characteristics of DZXXI under normal states [18,19]. However, the pharmacokinetic behavior of the TCM under pathological state may differ from that of normal status [20][21][22][23][24]. Besides, numerous studies have shown that the pharmacokinetics features of TCM are affected under the condition of disease [25][26][27].…”

Section: Introductionmentioning

confidence: 99%

A sensitive ultra‐fast liquid chromatography with tandem mass spectrometry method for simultaneous determination of ten constituents of Deng‐Zhan‐Xi‐Xin injection in rat plasma and its application to a comparative pharmacokinetic study in sham and middle cerebral artery occlusion rats

Guo

Lin

Liang

et al. 2020

J of Separation Science

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Deng-Zhan-Xi-Xin injection is widely used to treat cerebrovascular and cardiovascular diseases in clinical practice. A rapid and selective method based on ultra-fast liquid chromatography with tandem mass spectrometry was established and validated to simultaneously quantify chlorogenic acid, 1,3-Odicaffeoylquinic acid, isochlorogenic acid A, neochlorogenic acid, erigeside I, cryptochlorogenic acid, apigenin-7-O-glucuronide, scutellarin, isochlorogenic acid B, and isochlorogenic acid C of Deng-Zhan-Xi-Xin injection in both sham and middle cerebral artery occlusion rats. This was the first quantitative analysis of these ten constituents in both sham and middle cerebral artery occlusion rats. Chromatographic separation of these ten constituents was accomplished on an Acquity HSS T3 column with the mobile phase consisting of acetonitrile and 0.1% formic acid in water. Mass analysis was performed in negative ion mode with an electrospray ionization source using multiple reaction monitoring technology. The pharmacokinetic study of the ten constituents in sham and middle cerebral artery occlusion rats after intravenous administration of Deng-Zhan-Xi-Xin injection was successfully accomplished by using this validated method. Based on the results of pharmacokinetic parameters, significant differences were observed between the two groups, which might be due to the pathological factors of middle cerebral artery occlusion and pharmacological effects of Deng-Zhan-Xi-Xin injection.

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Comparative pharmacokinetics of four active components on normal and diabetic rats after oral administration of Gandi capsules

Abstract: The Gandi capsule, a famous traditional Chinese medicine (TCM), is a hospital preparation that has been widely used in China for decades for the treatment of diabetes.

Cited by 7 publications

References 35 publications

Elucidation of the Intestinal Absorption Mechanism of Loganin in the Human Intestinal Caco‐2 Cell Model

Elucidation of the Intestinal Absorption Mechanism of Loganin in the Human Intestinal Caco‐2 Cell Model

Pharmacokinetics of B-Ring Unsubstituted Flavones

A sensitive ultra‐fast liquid chromatography with tandem mass spectrometry method for simultaneous determination of ten constituents of Deng‐Zhan‐Xi‐Xin injection in rat plasma and its application to a comparative pharmacokinetic study in sham and middle cerebral artery occlusion rats

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