A Convenient Method to Measure Blood–Plasma Concentration Ratio Using Routine Plasma Collection in In Vivo Pharmacokinetic Studies

Berezhkovskiy, Leonid M.; Zhang, Xiaolin; Cheong, Jonathan

doi:10.1002/jps.22709

Cited by 14 publications

(6 citation statements)

References 10 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…The knowledge of blood‐plasma cocentration ratio is needed primarily for the routine interpretation of pharmacokinetic data 14,15. The maximum value of hepatic clearance calculated with respect to plasma concentration is equal to rQ h (but not Q h ), where Q h is the liver blood flow.…”

Section: Resultsmentioning

confidence: 99%

See 1 more Smart Citation

Prediction of Drug Terminal Half-Life and Terminal Volume of Distribution After Intravenous Dosing Based on Drug Clearance, Steady-State Volume of Distribution, and Physiological Parameters of the Body

Berezhkovskiy¹

2013

Journal of Pharmaceutical Sciences

Self Cite

View full text Add to dashboard Cite

Section: Resultsmentioning

confidence: 99%

“…If necessary, r should be determined by the common in vitro assay. The measurement of blood–plasma ratio can also be easily incorporated in routine pharmacokinetic studies using a convenient method suggested recently 15…”

Section: Resultsmentioning

confidence: 99%

Prediction of Drug Terminal Half-Life and Terminal Volume of Distribution After Intravenous Dosing Based on Drug Clearance, Steady-State Volume of Distribution, and Physiological Parameters of the Body

Berezhkovskiy¹

2013

Journal of Pharmaceutical Sciences

Self Cite

View full text Add to dashboard Cite

“…In addition, information on blood distribution is necessary to evaluate the distribution of xenobiotics in human organs by performing physiologically based pharmacokinetic modeling. 33 A recent study of Jin et al found that partitioning behaviors between plasma and RBCs played an important role in the excretion of perfluoroalkyl substances in the human body. 34 To date, the partitioning behaviors of BPs in human blood have not been assessed.…”

Section: ■ Introductionmentioning

confidence: 99%

“…Considering BPs may have different partitioning potentials between plasma and RBCs, monitoring BPs only in serum or plasma may substantially underestimate the extent of total BP exposure. In addition, information on blood distribution is necessary to evaluate the distribution of xenobiotics in human organs by performing physiologically based pharmacokinetic modeling . A recent study of Jin et al found that partitioning behaviors between plasma and RBCs played an important role in the excretion of perfluoroalkyl substances in the human body .…”

Section: Introductionmentioning

confidence: 99%

Occurrence and Partitioning of Bisphenol Analogues in Adults’ Blood from China

Jin

Zhu

Chen

et al. 2017

Environ. Sci. Technol.

152

View full text Add to dashboard Cite

Widespread human exposure and associated adverse health effects led to regulations on the usage of bisphenol A (BPA). Several bisphenol analogues (BPs) have been introduced as BPA alternatives in various applications. However, these BPs have been shown to exhibit similar or even stronger endocrine-disrupting activities compared with that of BPA. Currently, information on the human exposure to BPA alternatives remains limited. In this study, nine BPs were quantified in 81 pairs of plasma and red blood cell (RBC) samples from Chinese participants. In human plasma, the predominant BPs was BPA, bisphenol S (BPS), and bisphenol AF (BPAF), with the mean concentrations of 0.40, 0.15, and 0.073 ng/mL, respectively. BPA (accounting for 63% of total BPs) and BPS (18%) were the major BPs in the RBC fraction. Mass fractions in plasma (F) were found to be highest for BPS (mean, 0.78), followed by BPAF (0.71) and BPA (0.67), indicating strong partitioning to the plasma fraction. However, bisphenol AP was more frequently detected in the RBC fraction. Estimated total daily intake (EDI) of BPA was in the range of 0.0048-0.75 μg/kg bw/day for the participants, and adults aged >50 years had comparatively lower EDI. To our knowledge, this is the first study to assess the occurrence and partitioning of BPA alternatives in paired human plasma and RBCs from the Chinese general population.

show abstract

“…Plasma protein binding was performed using the single‐use RED device as described previously (Chen et al., 2019; Leung et al., 2020). Blood‐to‐plasma ratio was experimentally measured as described previously (Berezhkovskiy et al., 2011; Yu et al., 2005). Metabolic stability in suspended hepatocytes was measured to determine the intrinsic CL of each molecule as described previously (Jones et al., 2022).…”

Section: Methodsmentioning

confidence: 99%

Shared learning from a physiologically based pharmacokinetic modeling strategy for human pharmacokinetics prediction through retrospective analysis of Genentech compounds

Mao

et al. 2023

Biopharm & Drug Disp

View full text Add to dashboard Cite

The quantitative prediction of human pharmacokinetics (PK) including the PK profile and key PK parameters are critical for early drug development decisions, successful phase I clinical trials, and the establishment of a range of doses to enable phase II clinical dose selection. Here, we describe an approach employing physiologically based pharmacokinetic (PBPK) modeling (Simcyp) to predict human PK and to validate its performance through retrospective analysis of 18 Genentech compounds for which clinical data are available. In short, physicochemical parameters and in vitro data for preclinical species were integrated using PBPK modeling to predict the in vivo PK observed in mouse, rat, dog, and cynomolgus monkey. Through this process, the in vitro to in vivo extrapolation (IVIVE) was determined and then incorporated into PBPK modeling in order to predict human PK. Overall, the prediction obtained using this PBPK‐IVIVE approach captured the observed human PK profiles of the compounds from the dataset well. The predicted Cmax was within 2‐fold of the observed Cmax for 94% of the compounds while the predicted area under the curve (AUC) was within 2‐fold of the observed AUC for 72% of the compounds. Additionally, important IVIVE trends were revealed through this investigation, including application of scaling factors determined from preclinical IVIVE to human PK prediction for each molecule. Based upon the analysis, this PBPK‐based approach now serves as a practical strategy for human PK prediction at the candidate selection stage at Genentech.

show abstract

A Convenient Method to Measure Blood–Plasma Concentration Ratio Using Routine Plasma Collection in In Vivo Pharmacokinetic Studies

Cited by 14 publications

References 10 publications

Prediction of Drug Terminal Half-Life and Terminal Volume of Distribution After Intravenous Dosing Based on Drug Clearance, Steady-State Volume of Distribution, and Physiological Parameters of the Body

Prediction of Drug Terminal Half-Life and Terminal Volume of Distribution After Intravenous Dosing Based on Drug Clearance, Steady-State Volume of Distribution, and Physiological Parameters of the Body

Occurrence and Partitioning of Bisphenol Analogues in Adults’ Blood from China

Shared learning from a physiologically based pharmacokinetic modeling strategy for human pharmacokinetics prediction through retrospective analysis of Genentech compounds

Contact Info

Product

Resources

About