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Evrard, P.; Cumps, Jean; Verbeeck, Roger K.

doi:10.1023/a:1016008712756

Cited by 27 publications

(12 citation statements)

References 15 publications

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“…The pharmacokinetic parameters (Table 3) 16) and a similar effect of concentration-dependent plasma protein binding on the half-life was demonstrated for flurbiprofen. 17) As shown in Fig. 3, during the early period after drug administration, the concentration of unbound ketoprofen following intravenous administration of the LM was lower than that after intravenous administration of ketoprofen solution, implying the removal of LM from the blood circulation, probably by the reticuloendothelial system-rich organs.…”

Section: )mentioning

confidence: 87%

Pharmacokinetic Study of Ketoprofen Isopropyl Ester-Loaded Lipid Microspheres in Rat Blood Using Microdialysis

Tang

Cui

2006

Biological & Pharmaceutical Bulletin

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A blood microdialysis technique coupled with high-performance liquid chromatography was used to investigate the pharmacokinetics of unbound ketoprofen in rats after intravenous administration of a lipid-soluble ketoprofen derivate, ketoprofen isopropyl ester (KPI), loaded into lipid microspheres (LM) and ketoprofen solution. A microdialysis probe was inserted into the jugular vein of male Wistar rats. KPI-loaded LM or ketoprofen solution (24 mg/kg, i.v.) was then administrated via a femoral vein. Dialysate samples were analyzed using HPLC. The in vitro and in vivo recovery rate of the microdialysis probe was 30.42؎0.74% (n‫)3؍‬ and 40.27؎2.74% (n‫,)3؍‬ respectively. The pharmacokinetic parameters for ketoprofen after intravenous administration of KPIloaded LM and ketoprofen solution exhibited no statistically significant differences. The results of this pharmacokinetic study indicate that the microdialysis technique can be widely applicable to investigations of in vivo freedrug of microcarrier systems.

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Section: )mentioning

confidence: 87%

Pharmacokinetic Study of Ketoprofen Isopropyl Ester-Loaded Lipid Microspheres in Rat Blood Using Microdialysis

Tang

Cui

2006

Biological & Pharmaceutical Bulletin

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“…Thus, concentration dependent effect of disopyramide on renal clearance and distribution has been described . Similarly, a concentration dependent bounding of flurbiprofen to plasma protein in rat has been described …”

Section: Figurementioning

confidence: 89%

“…Experimental evidences are available describing the importance of concentration dependent plasma binding on pharmacokinetics as well as pharmacodynamics of the drug ,. During pharmacokinetic studies of small molecules, concentration dependent plasma binding is defined by experimental procedure.…”

Section: Figurementioning

confidence: 99%

CDPBC: A Software Application for Estimation of Concentration Dependent Plasma Binding Capacity of Small Molecule

Prakash

Dwivedi

2018

Molecular Informatics

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Drug-plasma binding (DPB) is an important aspect during pharmacokinetics (PK) studies. DPB of small molecule cannot be evaluated through computational means. Here we present CDPBC; a standalone application for evaluation of small molecule for its capacity (concentration dependent) of binding with plasma proteins. This application is freely available at URL (https://github.com/undwive di/CDPBC.git). The application is enriched with evaluation of five major proteins of plasma. Input for application is a docked complex against the suggested PDBs of plasma proteins. As part of the analysis, software compares interaction of query compound with control compound. Main output comes as plot as well as table displaying percentage of binding in reference of concentration gradient of small molecule used in docking. The application is an advanced add-on component to ADME analysis of small molecules as well as lead optimization.

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“…That study revealed that the protein content can directly affect microdialysis probe recovery [21]. Comparing microdialysis sampling with blood sample withdrawal for an in vivo pharmacokinetics of flurbiprofen revealed that simultaneous sampling of blood and intravenous microdialysis has become possible to study the pharmacokinetics of flurbiprofen in an individual rat [22].…”

Section: Protein Binding and Equilibrium Dialysismentioning

confidence: 99%

Assaying protein unbound drugs using microdialysis techniques

Tsai

2003

Journal of Chromatography B

115

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Abstract: Monitoring the fraction of drug unbound in blood of an individual rat throughout a pharmacokinetic experiment has now become possible by using simultaneous sampling of blood and intravenous microdialysates.

Cited by 27 publications

References 15 publications

Pharmacokinetic Study of Ketoprofen Isopropyl Ester-Loaded Lipid Microspheres in Rat Blood Using Microdialysis

Pharmacokinetic Study of Ketoprofen Isopropyl Ester-Loaded Lipid Microspheres in Rat Blood Using Microdialysis

CDPBC: A Software Application for Estimation of Concentration Dependent Plasma Binding Capacity of Small Molecule

Assaying protein unbound drugs using microdialysis techniques

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