Inhibitory Effects of Multiple‐Dose Treatment with Baicalein on the Pharmacokinetics of Ciprofloxacin in Rats

Hwang, Youn–Hwan; Yang, Hye Jin; Kim, Dong‐Gun; Yeul, Jin

doi:10.1002/ptr.5728

Cited by 8 publications

(6 citation statements)

References 41 publications

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“…However, the bioavailability of CPFX after oral administration is reported to be 20% in rats, 33) while, bioavailability in humans is 69%. 34) In addition, the elimination half-life in the rat is 1.55 h, 33) compared to 4.11 h in humans. 34) Therefore, considering these differences between rats and humans, the dose of CPFX was set at 20 mg/kg for rats, which is 5-fold higher than that of humans, to ensure the C max would be approximately the same.…”

Section: Discussionmentioning

confidence: 99%

“…34) In addition, the elimination half-life in the rat is 1.55 h, 33) compared to 4.11 h in humans. 34) Therefore, considering these differences between rats and humans, the dose of CPFX was set at 20 mg/kg for rats, which is 5-fold higher than that of humans, to ensure the C max would be approximately the same. Accordingly, thylakoid-rich spinach extract was administered at 500 mg/kg to keep the dose ratio of 1 : 25.…”

Section: Discussionmentioning

confidence: 99%

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Effects of Thylakoid-Rich Spinach Extract on the Pharmacokinetics of Drugs in Rats

Saito

Usami

Katoh

et al. 2019

Biological & Pharmaceutical Bulletin

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Thylakoid-rich spinach extract is being used as dietary weight-loss supplements in Japan. A recent rat study has suggested that intake of thylakoid-rich spinach extract with dietary oil inhibits dietary fat absorption via binding to bile acids, which promotes excretion of bile acids in feces. While, we confirmed that a serving size of thylakoid-rich spinach extract contains a large amount of calcium (130 mg/5 g). Therefore, using rats, we evaluated whether one-time ingestion of thylakoid-rich spinach extract affects the gastrointestinal absorption of water-insoluble drugs, such as griseofulvin (GF) and indomethacin (IM), or ciprofloxacin (CPFX) that chelate with polyvalent metal cations. Pretreatment of the rats with thylakoid-rich spinach extract (100 or 300 mg/kg) for 15 min prior to oral administration of GF (50 mg/kg) or IM (10 mg/kg) did not significantly alter the pharmacokinetic properties of either drug. Meanwhile, co-administration of thylakoidrich spinach extract (500 mg/kg) and CPFX (20 mg/kg) significantly reduced the peak plasma concentration and the area under the plasma concentration-time curve of CPFX to 25 and 40%, respectively in rats. In vitro studies demonstrated that when a mixture of thylakoid-rich spinach extract and CPFX was centrifuged, there was a significant reduction in the supernatant concentration of CPFX relative to the control. When the experiment was repeated in the presence of ethylenediaminetetraacetic acid, the concentration of CPFX was unchanged. These results suggest that the intake of thylakoid-rich spinach extract may reduce the absorption of drugs that form a chelate with polyvalent metal cations, such as CPFX.

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Section: Discussionmentioning

confidence: 99%

Section: Discussionmentioning

confidence: 99%

Effects of Thylakoid-Rich Spinach Extract on the Pharmacokinetics of Drugs in Rats

Saito

Usami

Katoh

et al. 2019

Biological & Pharmaceutical Bulletin

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“…PAH model was induced by intraperitoneal injection of 50 mg/kg of monocrotaline (MCT) for 6 weeks (Sigma‐Aldrich) as per our previously described with modifications 16 . Blood samples were collected at specific time points, the plasma concentration was determined, 18 and we choose the drug concentration according to the report 15 . In the present study, we have tested the lower dose (20 mg/kg, 50 mg/kg) and higher dose (200 mg/kg), the most effective dose is 100 mg/kg, and the main purpose of this present study is to explore the mechanism, so we only choose 100 mg/kg.…”

Section: Methodsmentioning

confidence: 99%

“…A recent study showed that inflammatory mediator tumor necrosis factor-α (TNF-α) can further promote the development of PAH by reducing BMPR2 expression in PASMCs [Yang et al, 2017]. Our previous studies have shown that baicalin could inhibit inflammation and improve PAH vascular remodeling by reducing TNF-α factor expression and regulation of BMPR2 signaling pathways in MCT-induced PAH rats, respectively.…”

Section: Introductionmentioning

confidence: 99%

Protective effect of baicalin against pulmonary arterial hypertension vascular remodeling through regulation of TNF‐α signaling pathway

Xue

Zhang

Wen

et al. 2021

Pharmacology Res & Perspec

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Pulmonary arterial hypertension (PAH) is a progressive cardiovascular disease with high mortality. However, there were no efficient medical drugs for PAH to enormously improve the survival and quality of life measures. The present study aimed to explore the protective effect of baicalin against experimental PAH in vivo and vitro. All the experimental rats received intraperitoneal injection of monocrotaline (MCT) to induce PAH model. Baicalin was given by intragastric administration from 2 days after MCT injection. Forty animals were randomly divided into four groups: Control, MCT, saline‐, and baicalin‐treated groups (n = 10 in each). Post‐operation, hemodynamic data, and index of right ventricular hypertrophy (RVHI) were recorded to evaluate the inhibition of baicalin on MCT‐induced PAH. Furthermore, pulmonary artery smooth muscle cells (PASMCs) model induced by tumor necrosis factor‐α (TNF‐α) was used to observe the inhibition of vascular cells proliferation in vitro. The results demonstrated that baicalin significantly attenuated MCT‐induced right ventricular systolic pressure (RVSP), the index of right ventricular hypertrophy, and vessel wall thickness; inhibit inflammatory and cell proliferation induced by MCT or TNF‐α, respectively. In addition, we found that baicalin might protect against experimental PAH via regulating the TNF‐α/BMPR2 signaling pathway.

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“…However, there few literatures have been reported about the pharmacokinetic studies of ZgI during the past 20 years [9]. Recently years, a large number of studies have demonstrated that pharmacokinetics of drugs can be affected by many factors, including age, gender, altitude, drugs and variety of diseases, such as diabetes, Hypertension, estrogen level and so on [10][11][12][13][14][15][16][17]. Actually, drugs are used to treat diseases, and the patients are the ultimate consumers of drugs [18].…”

Section: Introductionmentioning

confidence: 99%

Comparative Plasma Pharmacokinetics of Ziyuglycoside I from Sanguisorba Officinalis L. between Leukopenia and Normal Rats via UHPLC-MS/MS

Qin¹

2019

ACIM

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Objectives: Ziyuglycoside I (ZgI), one of the main active ingredients of Diyushengbai tablet made from Sanguisorba officinalis L., has been proved to relieve leukopenia. In our study, we compared the difference of pharmacokinetics of ZgI between normal and leukopenia rats.Materials and methods: 24 rats were divided into four groups, low and high dose (orally taken ZgI 5 or 20 mg/kg, respectively) control or leukopenia groups, induced by intraperitoneal injection of 70 mg/ kg Cyclophosphamide (CY) twice. plasma samples were collected from orbital venous plexus at 0, 5, 10, 20, 40, 60 min, 1.5, 2, 4, 8, 12, 24, 48 h after oral administrated of ZgI, and concentrations of ZgI were analyzed by Ultra-High Performance Liquid Chromatography-tandem Mass-spectrometry (UHPLC-MS/MS).Results: Compared with20 mg/kg normal group, peak time (T max ) was significantly shortened (0.93 h to 0.33 h) and maximum Concentration (C max ) was remarkably decreased (7.96 ng/L to 3.40 ng/L) in 20 mg/kg leukopenia group, on the contrary, elimination half-life (T 1/2β ) in it was obviously prolonged (5.02 h to 18.51 h). However, there were no clearly differences in distributed half-life (T 1/2α ) and area under the plasma concentration vs. time curve from zero to last sampling time (AUC 0-t ) between20 mg/kg leukopenia and control group (p>0.05). All above changes were similar between 5 mg/kg model and control group, except C max were nearly equal between them. Interestedly, there was also no evidently difference between the two leukopenia groups. Conclusion:The pharmacokinetic process especially absorption and metabolism of ZgI were evidently influenced by leukopenia. Our study may provide guidance for clinical use of Diyushengbai tablet and development of ZgI as an agent for the treatment of leukopenia.

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Inhibitory Effects of Multiple‐Dose Treatment with Baicalein on the Pharmacokinetics of Ciprofloxacin in Rats

Cited by 8 publications

References 41 publications

Effects of Thylakoid-Rich Spinach Extract on the Pharmacokinetics of Drugs in Rats

Effects of Thylakoid-Rich Spinach Extract on the Pharmacokinetics of Drugs in Rats

Protective effect of baicalin against pulmonary arterial hypertension vascular remodeling through regulation of TNF‐α signaling pathway

Comparative Plasma Pharmacokinetics of Ziyuglycoside I from Sanguisorba Officinalis L. between Leukopenia and Normal Rats via UHPLC-MS/MS

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