High-performance liquid chromatographic assay and erythrocyte partitioning of fleroxacin, a new fluoroquinolone antibiotic

Brunt, Elsbeth; Limberg, Jobst; Derendorf, Hartmut

doi:10.1016/0731-7085(90)80008-d

Cited by 18 publications

(7 citation statements)

References 6 publications

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“…For example, studying the binding of fleroxacin by means of equilibrium dialysis showed that 23% of the drug was bound, while the same study carried out using the ultrafiltration method reported a 47% (8). It is also possible that results obtained in different laboratories may differ considerably, showing the importance of using the same equipment for all determinations, and on the basis of a properly chosen and validated procedure (9).…”

mentioning

confidence: 94%

Human Serum Albumin Binding of Novel Antiretroviral Nucleoside Derivatives of AZT

Quevedo

Moroni

Briñón

2001

Biochemical and Biophysical Research Communications

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mentioning

confidence: 94%

Human Serum Albumin Binding of Novel Antiretroviral Nucleoside Derivatives of AZT

Quevedo

Moroni

Briñón

2001

Biochemical and Biophysical Research Communications

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“…For example, equilibrium dialysis of fleroxacin indicated 23% protein binding, whereas ultrafiltration indicated 47% binding. 4 Moreover, the extent of protein binding determined by the same method in different laboratories may differ considerably. For example, the amount of ofloxacin bound to protein was reported to be in the range 8-30%, 5,7 and that of enoxacin was in the range of 30-50%.…”

Section: Introductionmentioning

confidence: 99%

Plasma Protein Binding of Gyrase Inhibitors

Zlotos

Bücker

Kinzig‐Schippers

et al. 1998

Journal of Pharmaceutical Sciences

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Plasma protein binding of a wide range of gyrase inhibitors in clinical practice or trials has been determined by ultrafiltration to determine structure-protein binding relationships. The protein binding was independent of overall lipophilicity. In particular, the "western" part of the "quinolone" skeleton, consisting of a heterocyclus at position 7 and varying substituents at position 8, strongly influences the extent of protein binding, indicating that this part interacts with the plasma protein. In contrast, substituents in position N1 do not show an effect on the protein binding in this series of compounds.

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“…The concentrations in plasma and bone from all patients were modeled simultaneously. The blood to plasma concentration ratio of ciprofloxacin in humans closely approximates unity. , Thus, the concentration of ciprofloxacin measured in plasma was used as a surrogate of blood concentration. The ciprofloxacin concentrations in the blood compartment ( C B ) were modeled as where V B is blood volume, Q CO is cardiac output blood flow, C 1 and C 2 are the ciprofloxacin concentrations in (nonbone) tissue compartments 1 and 2, f d1 and f d2 are the fractions of Q CO going to tissue compartments 1 and 2, and K p1 and K p2 are the tissue partition coefficients for these compartments.…”

Section: Methodsmentioning

confidence: 99%

Physiologically Based Population Pharmacokinetic Modeling Approach for Ciprofloxacin in Bone of Patients Undergoing Orthopedic Surgery

Landersdorfer

Kinzig

Höhl

et al. 2020

ACS Pharmacol. Transl. Sci.

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Ciprofloxacin is highly active against bacteria that commonly cause bone infections. However, the time-course of ciprofloxacin in bone has not been characterized using population pharmacokinetic modeling. Thirty-nine patients received a 1-h infusion of 400 mg of ciprofloxacin before orthopedic surgery. Blood and bone samples were collected at 0.5 to 20 h following the start of the infusion. Bone samples were separated into cortical and cancellous bone and pulverized under liquid nitrogen using a cryogenic mill. Ciprofloxacin in plasma, and cortical and cancellous bone was quantified by liquid chromatography−tandem mass spectrometry. A physiologically based pharmacokinetic modeling approach was utilized to describe the concentration−time profiles in plasma and bone. Ciprofloxacin concentrations ranged from 0.176 to 5.98 mg/L (median, 1.67; density, 1.99 g/cm 3 ) in cortical, and 0.224 to 14.6 mg/L (median, 1.22; 1.92 g/cm 3 ) in cancellous bone. The average observed cortical bone/plasma concentration ratio was 0.67 at 0.5 to 2 h (n = 7) and 5.1 at 13 to 20 h (n = 9). For cancellous bone the respective average ratios were 0.77 and 4.4. The population PK model included a central (blood) compartment, two peripheral tissue compartments, and compartments for the organic and inorganic (hydroxyapatite) matrix in cortical and cancellous bone. The population mean ciprofloxacin clearance was 20.7 L/h. The estimated partition coefficients of the organic bone matrix were 3.39 for cortical and 5.11 for cancellous bone. Ciprofloxacin achieved higher concentrations in bone than plasma. Slow redistribution from bone to plasma may have been due to binding to the inorganic bone matrix. The developed model presents a step toward optimized antibiotic dosing in osteomyelitis.

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High-performance liquid chromatographic assay and erythrocyte partitioning of fleroxacin, a new fluoroquinolone antibiotic

Cited by 18 publications

References 6 publications

Human Serum Albumin Binding of Novel Antiretroviral Nucleoside Derivatives of AZT

Human Serum Albumin Binding of Novel Antiretroviral Nucleoside Derivatives of AZT

Plasma Protein Binding of Gyrase Inhibitors

Physiologically Based Population Pharmacokinetic Modeling Approach for Ciprofloxacin in Bone of Patients Undergoing Orthopedic Surgery

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