Enantioselective determination of 3-n-butylphthalide (NBP) in human plasma by liquid chromatography on a teicoplanin-based chiral column coupled with tandem mass spectrometry

Diao, Xingxing; Ma, Zhiyu; Peng, Liming; Zhong, Dafang; Zhang, Yifan; Chen, Xiaoyan

doi:10.1016/j.jchromb.2013.09.014

Cited by 21 publications

(9 citation statements)

References 12 publications

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“…It is recommended to use a stable isotope-labeled analog as internal standard for quantitative LC–MS/MS analysis [11] and [12]. The best peak response was attained with acetonitrile and water with 0.1% FA as opposed to 0% and 0.2% FA.…”

Section: Resultsmentioning

confidence: 99%

Simultaneous determination and validation of oncrasin-266 and its metabolites by HPLC–MS/MS: Application to a pharmacokinetic study

White

et al. 2016

Journal of Chromatography B

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Oncrasins are a class of RNA polymerase II inhibitors. Oncrasin-72 is an indole-3 carbinol analog that has shown to inhibit growth and induce the cell death of various human cancer cell lines. Oncrasin-266, a prodrug of oncrasin-72, has been shown to have improved pharmacokinetic properties and safety than Oncrasin-72. With respect to the potential therapeutic advantages of this class of compounds, there is a need for further preclinical assessment for future clinical trials. The development of and validation of an analytical method is essential for the quantification of oncrasins in biological fluids for pharmacokinetic studies. This study focuses on the LC-MS/MS method development and validation of oncrasin-266, oncrasin-72 and its aldehyde metabolite in rat plasma. Blank rat plasma, coupled with 1-(3-chlorobenzyl)-1H-indole, as internal standard, was used for generating standard curves ranging from 1–250 ng/mL for oncrasin-266 and oncrasin-72; and 0.5–125 ng/mL for the aldehyde metabolite. The chromatographic separation was achieved by a Zorbax 300SB-C18 HPLC column at 50°C with a flow rate of 1.1 mL/min under gradient elution. Mass detection was performed under positive ionization electrospray. Intra- and inter-day accuracy and precision of the assay were less than 10%. We report a simple, specific and reproducible LC-MS/MS method for the quantification of oncrasins in rat plasma. This study was successfully used for the quantification of oncrasins in rat plasma for pharmacokinetic studies in three dose groups of 10, 25, and 50 mg/kg via intravenous administration.

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Section: Resultsmentioning

confidence: 99%

Simultaneous determination and validation of oncrasin-266 and its metabolites by HPLC–MS/MS: Application to a pharmacokinetic study

White

et al. 2016

Journal of Chromatography B

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“…The method was validated according to the US Food and Drug Administration bioanalytical method validation guidelines for industry and European Medicines Agency guidelines on validation of bioanalytical methods (Diao, Ma, Lei et al, 2013;Diao, Ma, Wang et al, 2013).…”

Section: Methods Validationmentioning

confidence: 99%

Pharmacokinetic properties of wogonin and its herb–drug interactions with docetaxel in rats with mammary tumors

Wang

Long

et al. 2018

Biomedical Chromatography

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Docetaxel, frequently used for the treatment of breast cancer, is mainly metabolized via hepatic cytochrome P450 (CYP) 3A in humans and is also a substrate of P-glycoprotein (P-gp). Wogonin has been shown to be able to modulate the activities of CYPs and P-gp, and it could serve as an adjuvant chemotherapeutic agent. However, the impacts of co-administration of wogonin and docetaxel on their pharmacokinetics have not been studied because of a lack of an analytical method for their simultaneous measurement. In the present study, we established an HPLC-MS/MS method for simultaneous measurement of wogonin and docetaxel in rat plasma, and it was then utilized to explore the pharmacokinetics of wogonin and the herb-drug interactions between wogonin and docetaxel after their combined administration in rats with mammary tumors. The rats received 10, 20 and 40 mg/kg wogonin via oral administration, with or without docetaxel intravenously administered at 10 mg/kg, and the plasma concentrations of wogonin and docetaxel were measured using the established and validated HPLC-MS/MS method. The C and AUC of wogonin were proportionally increased in the dose range from 10 to 40 mg/kg, suggesting a linear pharmacokinetics of wogonin. Moreover, the C and AUC of docetaxel and the AUC of wogonin were increased after co-administration (p < 0.05), indicating increased in vivo exposures of both wogonin and docetaxel, which might lead to an increase in not only therapeutic but also toxic effects. Thus the alterations of pharmacokinetics should be taken into consideration when wogonin and docetaxel are co-administered.

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“…Racemic NBP was approved for marketing in China by the Chinese Food and Drug Administration (CFDA) in 2004 [1,2] . Pharmacological studies have revealed that NBP exerts neuroprotective effects by increasing blood flow in the cerebral ischemic area and inhibiting the release of 5-hydroxytryptamine, glutamate and cytochrome c through the c-Jun N-terminal kinase pathway [3][4][5][6] .…”

Section: -N-butylphthalide (Nbp (±)-3-butyl-1(3h)-isobenzofuranone)mentioning

confidence: 99%

“…Overall, 60%±5.2% of 10-OH-NBP was unbound in rat plasma, whereas in rat brain homogenate, 82%±8.3% of 10-OH-NBP was unbound. The unbound fraction of non-diluted brain tissue recalculated from f u in brain homogenate was 49.9%±14.1% using Equation (2).…”

Section: Plasma and Brain Protein Binding Of 3-oh-nbp And 10-oh-nbpmentioning

confidence: 99%

Isomer-selective distribution of 3-n-butylphthalide (NBP) hydroxylated metabolites, 3-hydroxy-NBP and 10-hydroxy-NBP, across the rat blood-brain barrier

Diao

Zhong

et al. 2015

Acta Pharmacol Sin

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Aim: To investigate the mechanisms underlying the isomer-selective distribution of 3-n-butylphthalide (NBP) hydroxylated metabolites, 3-hydroxy-NBP (3-OH-NBP) and 10-hydroxy-NBP (10-OH-NBP), across the blood brain barrier (BBB). Methods: After oral administration of NBP (20 mg/kg) to rats, the pharmacokinetics of two major hydroxylated metabolites, 3-OH-NBP and 10-OH-NBP, in plasma and brains were investigated. Plasma and brain protein binding of 3-OH-NBP and 10-OH-NBP was also assessed. To evaluate the influences of major efflux transporters, rats were pretreated with the P-gp inhibitor tariquidar (10 mg/kg, iv) and BCRP inhibitor pantoprazole (40 mg/kg, iv), then received 3-OH-NBP (12 mg/kg, iv) or 10-OH-NBP (3 mg/kg, iv). The metabolic profile of NBP was investigated in rat brain homogenate. Results: After NBP administration, the plasma exposure of 3-OH-NBP was 4.64 times that of 10-OH-NBP, whereas the brain exposure of 3-OH-NBP was only 11.8% of 10-OH-NBP. In the rat plasma, 60%±5.2% of 10-OH-NBP was unbound to proteins versus only 22%±2.3% of 3-OH-NBP being unbound, whereas in the rat brain, free fractions of 3-OH-NBP and 10-OH-NBP were 100%±9.7% and 49.9%±14.1%, respectively. In the rats pretreated with tariquidar and pantoprazole, the unbound partition coefficient K p,uu of 3-OH-NBP was significantly increased, while that of 10-OH-NBP showed a slight but not statistically significant increase. Incubation of rat brain homogenate with NBP yielded 3-OH-NBP but not 10-OH-NBP. Conclusion: The isomer-selective distribution of 10-OH-NBP and 3-OH-NBP across the BBB of rats is mainly attributed to the differences in plasma and brain protein binding and the efflux transport of 3-OH-NBP. The abundant 10-OH-NBP is not generated in rat brains.

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Enantioselective determination of 3-n-butylphthalide (NBP) in human plasma by liquid chromatography on a teicoplanin-based chiral column coupled with tandem mass spectrometry

Cited by 21 publications

References 12 publications

Simultaneous determination and validation of oncrasin-266 and its metabolites by HPLC–MS/MS: Application to a pharmacokinetic study

Simultaneous determination and validation of oncrasin-266 and its metabolites by HPLC–MS/MS: Application to a pharmacokinetic study

Pharmacokinetic properties of wogonin and its herb–drug interactions with docetaxel in rats with mammary tumors

Isomer-selective distribution of 3-n-butylphthalide (NBP) hydroxylated metabolites, 3-hydroxy-NBP and 10-hydroxy-NBP, across the rat blood-brain barrier

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