Determination of plasma protein binding for sympathomimetic drugs by means of ultrafiltration

Volpp, M.; Holzgrabe, Ulrike

doi:10.1016/j.ejps.2018.10.027

Cited by 18 publications

(8 citation statements)

References 15 publications

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“…The potential LDH-inhibitory activity of I. obliquus was determined by UF-LC. The ultrafiltration process included culture, washing, and separation [ 28 ]. I. obliquus extract (50 mg) was dissolved in 50% MeOH (1 mL) and filtered using a 0.45-μm membrane.…”

Section: Methodsmentioning

confidence: 99%

Total Triterpenoid Extraction from Inonotus Obliquus Using Ionic Liquids and Separation of Potential Lactate Dehydrogenase Inhibitors via Ultrafiltration High-Speed Countercurrent Chromatography

et al. 2021

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Extracts of the fungus Inonotus obliquus exhibit cytotoxic properties against different cancers; hence, this fungal species has been extensively studied. This study aimed to extract total triterpenoids from Inonotus obliquus using ionic liquids (ILs) and separate potential lactate dehydrogenase (LDH) inhibitors via ultrafiltration (UF)-high-speed countercurrent chromatography (HSCCC). Total triterpenoids from Inonotus obliquus were extracted by performing a single-factor experiment and employing a central composite design via ultrasonic-assisted extraction (UAE) and heat-assisted extraction (HAE). The extract was composed of 1-butyl-3-methylimidazolium bromide as the IL and methanol as the dispersant. Ultrafiltration-liquid chromatography (UF-LC) was used to rapidly scan the LDH inhibitors and betulin and lanosterol were identified as potential inhibitors. To obtain these target compounds, betulin and lanosterol with the purities of 95.9% and 97.8% were isolated from HSCCC within 120 min. Their structures were identified using several techniques, among which IL-HAE was fast and effective. This study reports the extraction of triterpenoids from Inonotus obliquus by IL for the first time. Collectively, the findings demonstrate that UF-LC is an effective tool for screening potential LDH inhibitors from crude extracts of I. obliquus and may help to identify bioactive substances against myocardial infarction, whereas high-purity compounds can be separated via UF-HSCCC.

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Section: Methodsmentioning

confidence: 99%

Total Triterpenoid Extraction from Inonotus Obliquus Using Ionic Liquids and Separation of Potential Lactate Dehydrogenase Inhibitors via Ultrafiltration High-Speed Countercurrent Chromatography

et al. 2021

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“…In the preliminary phase of the PPB experiment, we considered several measures to evaluate the PPB of NAI59, including equilibrium dialysis, ultrafiltration, and ultra‐centrifugation (Rabbani‐Chadegani et al, 2017; Volpp & Holzgrabe, 2019). Compared with the other two methods, the equilibrium dialysis method is easy to control temperature, has an adjustable pH value, and is inexpensive for determining the binding rate of plasma protein (BRPP).…”

Section: Resultsmentioning

confidence: 99%

Anti‐fibrosis attributes: UHPLC‐MS/MS‐based pharmacokinetics profiling of a novel autotaxin inhibitor with excellent in vivo efficacy in rat

Wang

Long

Zhang

et al. 2022

Biomedical Chromatography

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3,4-Difluorobenzyl(1-ethyl-5-(4-((4-hydroxypiperidin-1-yl)-methyl)thiazol-2-yl)-1Hindol-3-yl)carbamate (NAI59), a small molecule with outstanding therapeutic effectiveness to anti-pulmonary fibrosis, was developed as an autotaxin inhibitor candidate compound. To evaluate the pharmacokinetics and plasma protein binding of NAI59, a UPLC-MS/MS method was developed to quantify NAI59 in plasma and phosphate-buffered saline. The calibration curve linearity ranged from 9.95 to 1990.00 ng/mL in plasma. The accuracy was À6.8 to 5.9%, and the intra-and interday precision was within 15%. The matrix effect and recovery, as well as dilution integrity, were within the criteria. The chromatographic and mass spectrometric conditions were also feasible to determine phosphate-buffered saline samples, and it has been proved that this method exhibits good precision and accuracy in the range of 9.95-497.50 ng/mL in phosphate-buffered saline. This study is the first to determine the pharmacokinetics, absolute bioavailability, and plasma protein binding of NAI59 in rats using this established method. Therefore, the pharmacokinetic profiles of NAI59 showed a dose-dependent relationship after oral administration, and the absolute bioavailability in rats was 6.3%. In addition, the results of protein binding showed that the combining capacity of NAI59 with plasma protein attained 90% and increased with the increase in drug concentration.

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“…This may be related to the degree of plasma protein-binding of the SCRT components. The degrees of plasma protein-binding of ephedrine, paeoniflorin, and cinnamic acid, the main components of SCRT, was about 4-6% [45], 10-20% [46], and 60-65% [18], respectively. Therefore, as SCRT is administered multiple times, competition occurs in plasma proteinbinding between the components with the accumulation of components in the blood, and as a result, the V d /F values of paeoniflorin and cinnamic acid, which have relatively higher plasma protein-binding degrees than that of ephedrine, may be significantly reduced.…”

Section: Pharmacokinetic Studymentioning

confidence: 94%

Pharmacokinetic Changes According to Single or Multiple Oral Administrations of Socheongryong-Tang to Rats: Presented as a Typical Example of Changes in the Pharmacokinetics Following Multiple Exposures to Herbal Medicines

et al. 2021

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The purpose of this study was to investigate the pharmacokinetic properties of ephedrine, paeoniflorin, and cinnamic acid after single or multiple doses of Socheongryong-tang (SCRT) were administered to rats, and to present an example of the pharmacokinetic changes following multiple doses of an herbal medicine. SCRT is a traditional herbal medicine that has been used clinically for a long time, and its main ingredients include ephedrine, paeoniflorin, and cinnamic acid. However, studies on the pharmacokinetic properties of SCRT are insufficient, and particularly, no pharmacokinetic information has been reported for multiple doses. In this study, SCRT was administered orally to rats once or multiple times, and plasma sampled at different times was quantitatively analyzed for ephedrine, paeoniflorin, and cinnamic acid using ultra-high-performance liquid chromatography-tandem mass spectrometry. There was a difference between the pharmacokinetic parameter values of each component (especially in paeoniflorin and cinnamic acid) obtained after single or multiple doses of SCRT. The actual observed values of each component obtained after multiple doses of SCRT were clearly different from the predicted results of multiple-dose simulations based on the pharmacokinetic profiles obtained after a single dose. The results confirmed that the plasma concentrations and, thus, exposures to paeoniflorin and cinnamic acid were significantly increased when SCRT was administered multiple times, whereas that of ephedrine was not. The results of this study are expected to provide useful pharmacokinetic data for the safety and efficacy evaluation of SCRT in the future and demonstrate the necessity of pharmacokinetic comparison studies according to single or multiple oral administrations of herbal medicines.

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Determination of plasma protein binding for sympathomimetic drugs by means of ultrafiltration

Cited by 18 publications

References 15 publications

Total Triterpenoid Extraction from Inonotus Obliquus Using Ionic Liquids and Separation of Potential Lactate Dehydrogenase Inhibitors via Ultrafiltration High-Speed Countercurrent Chromatography

Total Triterpenoid Extraction from Inonotus Obliquus Using Ionic Liquids and Separation of Potential Lactate Dehydrogenase Inhibitors via Ultrafiltration High-Speed Countercurrent Chromatography

Anti‐fibrosis attributes: UHPLC‐MS/MS‐based pharmacokinetics profiling of a novel autotaxin inhibitor with excellent in vivo efficacy in rat

Pharmacokinetic Changes According to Single or Multiple Oral Administrations of Socheongryong-Tang to Rats: Presented as a Typical Example of Changes in the Pharmacokinetics Following Multiple Exposures to Herbal Medicines

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