Prediction of human pharmacokinetics of panipenem-betamipron, a new carbapenem, from animal data

Kurihara, Atsushi; Naganuma, Hideo; Hisaoka, Masafumi; Tokiwa, Hiroshi; Kawahara, Yukinori

doi:10.1128/aac.36.9.1810

Cited by 31 publications

(15 citation statements)

References 15 publications

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“…3 and Table 2, respectively) were similar to those reported in previous studies. 3,13 These results suggest that the clinical monitoring of carbapenem levels is possible with our HPLC method.…”

Section: Discussionmentioning

confidence: 88%

Simple and rapid determination of serum carbapenem concentrations by high-performance liquid chromatography

Kikuchi¹,

Kizu²,

Hori

2008

Journal of Infection and Chemotherapy

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Section: Discussionmentioning

confidence: 88%

Simple and rapid determination of serum carbapenem concentrations by high-performance liquid chromatography

Kikuchi¹,

Kizu²,

Hori

2008

Journal of Infection and Chemotherapy

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“…The steady-state distribution volume of panipenem in a human of mass 60 kg was calculated using the equation given above as V SS,hum = 12.1 (5.9 -25.1) L. The V SS for humans that was obtained earlier [62] from pharmacokinetic data was 11.1 L, which indicated that the accuracy of the extrapolation was fully satisfactory. The parameters of interspecies distribution volume functions were determined for many drugs using Eq.…”

Section: Interspecies Functions For Drug Distribution Volumesmentioning

confidence: 99%

“…For example, consider the interspecies function for the steady-state distribution volume of the antibiotic panipenem, which we constructed previously [62]. The drug pharmacokinetic parameters for six animal species were calculated from (2 ).…”

Section: Interspecies Functions For Drug Distribution Volumesmentioning

confidence: 99%

Interspecies Pharmacokinetics. 1. Allometric Scaling of Pharmacokinetic Parameters (a Review)

et al. 2014

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This review summarized some approaches to establishing interspecies allometric relationships for pharmacokinetic parameters of drugs defined by statistical analysis of individual time -concentration profiles of substances in blood of several animal species. The presented interspecies allometric relationships for basic pharmacokinetic parameters could be used in preclinical pharmacokinetics investigations.Preclinical pharmacokinetic studies of new drugs in animals are used to extrapolate the pharmacokinetic parameters to man, to select drug doses for phase I clinical trials, and to evaluate the safety for humans of new drug candidates [1,2]. The experimental pharmacological methodical approach that calculates the distribution of a candidate drug in human blood and organs from experimental data obtained in laboratory animal tests is called interspecies scaling of pharmacokinetic data. Work on interspecies scaling of pharmacokinetic data developed rapidly since the 1960s and is associated with researchers such as L. B. Mellet [3], R. L. Dedrick [4 -6], H. Boxenbaum [7 -12], and J. Mordenti [13 -15]. Their studies were a logical continuation of research on the physiological similarity of biological species that started already in the 1930s [16 -18].The methodology of interspecies scaling of pharmacokinetic data is currently developing in two relatively independent directions that differ in the pharmacokinetic models used to determine the drug pharmacokinetic parameters and employed interspecies scaling methods [19 -29]. The allometric method of pharmacokinetic data scaling is elaborated in the most detail. It is commonly used for interspecies analysis of drugs with different pharmacokinetics [19 -26].The present review analyzed the procedures for obtaining interspecies allometric functions for the principal drug pharmacokinetic parameters to be determined by statistical processing of individual drug concentration distributions in several animal species. Basic principles of allometric interspecies scaling of pharmacokinetic dataThe allometric method received its name because of the non-linear equations for the interspecies dependences of mammalian physiological parameters and drug pharmacokinetic parameters. The numerical parameters of the allometric equation are determined by statistical processing of experimental data obtained in tests on several biological species. Hence, another name for the method is statistical.The drug pharmacokinetics should be linear in the studied dose range and the metabolic pathways in man and animals used for the calculations should be similar in order to use this method. However, examples were reported where the allometric method was applied successfully and the metabolic pathways in animals and man differed, e.g., during an analysis of interspecies differences in theophylline distribution [30]. Much literature data demonstrated that the allometric equations were in general suitable for predicting pharmacokinetic parameters in man using animal data [11, 15, 22, 26, 31 -37].The allometri...

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“…mice, rats, rabbits and dogs, to investigate interspecies correlation and to predict human pharmacokinetics of the drug. Several reports concerned with animal scale-up of pharmacokinetic parameters of panipenem-betamipron [14], DA-1131, a new carbapenem [15], SJ-8029, a new anticancer agent [16], lamifiban, a new platelet aggregation inhibitor [17] and amphotericin B [18] by allometric scaling have been published. The purpose of this paper is to report the pharmacokinetics of oltipraz after intravenous and/or oral administration with various doses to mice, rats, rabbits and dogs, and to investigate the interspecies relationship of pharmacokinetic parameters of oltipraz, such as the time-averaged total body clearance (Cl) Â maximum life-span potential (MLP), Cl, and apparent volume of distribution at steady state (V ss ), and to predict the pharmacokinetics of the drug in humans from the four animal data.…”

Section: Introductionmentioning

confidence: 99%

Interspecies pharmacokinetic scaling of oltipraz in mice, rats, rabbits and dogs, and prediction of human pharmacokinetics

Bae

Lee

Kim

et al. 2005

Biopharm & Drug Disp

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Dose-independent pharmacokinetics of oltipraz after intravenous and/or oral administration at various doses to mice, rats, rabbits and dogs were evaluated. After both intravenous and/or oral administration of oltipraz to mice (5, 10 and 20 mg/kg for intravenous and 15, 30 and 50 mg/kg for oral administration), rats (5, 10 and 20 mg/kg for intravenous and 25, 50 and 100 mg/kg for oral administration), rabbits (5, 10 and 30 mg/kg for intravenous administration) and dogs (5 and 10 mg/kg for intravenous and 50 and 100 mg/kg for oral administration), the total area under the plasma concentration-time curve from time zero to time infinity (AUC) values of oltipraz were dose-proportional in all animals studied. Animal scale-up of some pharmacokinetics parameters of oltipraz was also performed based on the parameters after intravenous administration at a dose of 10 mg/kg to mice, rats, rabbits and dogs. Linear relationships were obtained between log time-averaged total body clearance (Cl) x maximum life-span potential (MLP) (1 year/h) and log species body weight (W) (kg) (r=0.999; p=0.0015), log Cl (l/h) and log W (kg) (r=0.979; p=0.0209), and log apparent volume of distribution at steady state (V(ss)) (l) and log W (kg) (r=0.999; p=0.0009). The corresponding allometric equations were ClxMLP=49.8 W(0.861), Cl=5.20 W(0.523) and V(ss)=4.46 W(0.764). Interspecies scale-up of plasma concentration-time data for the four species using pharmacokinetic time of dienetichron resulted in similar profiles. In addition, concentrations of oltipraz in a plasma concentration-time profile for humans predicted using the four animal data fitted to the dienetichron time transformation of animal data.

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Prediction of human pharmacokinetics of panipenem-betamipron, a new carbapenem, from animal data

Cited by 31 publications

References 15 publications

Simple and rapid determination of serum carbapenem concentrations by high-performance liquid chromatography

Simple and rapid determination of serum carbapenem concentrations by high-performance liquid chromatography

Interspecies Pharmacokinetics. 1. Allometric Scaling of Pharmacokinetic Parameters (a Review)

Interspecies pharmacokinetic scaling of oltipraz in mice, rats, rabbits and dogs, and prediction of human pharmacokinetics

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