Application of physiologically based pharmacokinetic modeling in the prediction of pharmacokinetics of bicyclol controlled-release formulation in human

Wang, Baolian; Liu, Zhihao; Li, Dan; Yang, Shuang; Hu, Jiye; Chen, Hui; Li, Sheng; Li, Yan

doi:10.1016/j.ejps.2015.06.020

Cited by 20 publications

(13 citation statements)

References 29 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…It was expected that the discrepancy between the predicted and the measured PK profile was due to the difference between the predicted and the measured Vd values. The liver and kidney are mainly considered to be organs that determine the disposition of small molecule drug [ 19 20 ]. In case of carisbamate, the previous studies show little metabolic disposition in the kidney [ 24 32 33 ].…”

Section: Resultsmentioning

confidence: 99%

“…Recently, physiologically based pharmacokinetic (PBPK) model has been increasingly used as a powerful tool to predict clinical pharmacokinetic (PK) parameters and profiles by using preclinical Absorption, Distribution, Metabolism, and Excretion (ADME)/PK data [13][14][15][16][17][18][19][20]. PBPK modeling is a very complex mathematical model that reflects systemically specific physiological properties and drug's physicochemical properties [21].…”

Section: Introductionmentioning

confidence: 99%

See 1 more Smart Citation

Qualification and application of liquid chromatography-quadrupole time-of-flight mass spectrometric method for the determination of carisbamate in rat plasma and prediction of its human pharmacokinetics using physiologically based pharmacokinetic modeling

Lee

Lim

Park

et al. 2020

Transl Clin Pharmacol

View full text Add to dashboard Cite

Carisbamate is an antiepileptic drug and it also has broad neuroprotective activity and anticonvulsant reaction. In this study, a liquid chromatography-quadrupole time-of-flight mass spectrometric (LC-qTOF-MS) method was developed and applied for the determination of carisbamate in rat plasma to support in vitro and in vivo studies. A quadratic regression (weighted 1/concentration 2), with an equation y = ax 2 + bx + c, was used to fit calibration curves over the concentration range from 9.05 to 6,600 ng/mL for carisbamate in rat plasma. Preclinical in vitro and in vivo studies of carisbamate have been studied through the developed bioanalytical method. Based on these study results, human pharmacokinetic (PK) profile has been predicted using physiologically based pharmacokinetic (PBPK) modeling. The PBPK model was optimized and validated by using the in vitro and in vivo data. The human PK of carisbamate after oral dosing of 750 mg was simulated by using this validated PBPK model. The human PK parameters and profiles predicted from the validated PBPK model were similar to the clinical data. This PBPK model developed from the preclinical data for carisbamate would be useful for predicting the PK of carisbamate in various clinical settings.

show abstract

Section: Resultsmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

Qualification and application of liquid chromatography-quadrupole time-of-flight mass spectrometric method for the determination of carisbamate in rat plasma and prediction of its human pharmacokinetics using physiologically based pharmacokinetic modeling

Lee

Lim

Park

et al. 2020

Transl Clin Pharmacol

View full text Add to dashboard Cite

show abstract

“…These studies were also provided the setup of a preclinical pharmacokinetic animal model for IVIVC. Further, with the help of the physiologicalbased pharmacokinetic modelling and in vitro-in vivo extrapolation methods, preclinical pharmacokinetic profile of different formulations could be extrapolated to humans [22,23] . Finally, the preclinical IVIVC of TPM would provide cost reduction in formulation development as the numbers of trials for expected in vivo profile were reduced due to simulated IVIVC model.…”

Section: Resultsmentioning

confidence: 99%

Development and Validation of an In Vitro and In Vivo Correlation Model in NZ Rabbit for Topiramate Extended Release Capsules

Laxman¹,

Durgaprasad²,

Tirgar³

et al. 2016

pharmaceutical-sciences

View full text Add to dashboard Cite

Laxman, et al.: IVIVC of Topiramate Extended Release Capsule The purpose of this study was to build an in vitro-in vivo correlation model for topiramate extended release capsules. Three formulations with different release rates were developed by varying the percent content of the rate controlling polymer ethyl cellulose and pore former hypromellose. In vitro dissolution of all formulations was performed by United States Pharmacopeia type I apparatus using multimedia dissolution conditions such as 0.1 N hydrochloric acid pH 1.2 for initial 2 h followed by phosphate buffer pH 6.8 for the rest of 22 h. Total dissolution time was up to 24 h. In vivo pharmacokinetic profile of the immediate release suspension and different extended release formulations were investigated in a rabbit model after single oral administration of topiramate at a dose of 10.33 mg/kg. An in vitro-in vivo correlation model was established by using two-stage numerical deconvolution approaches. Unit impulse response was obtained from pharmacokinetic profile of immediate release suspension which was used as a reference formulation. A linear correlation model with a time scaling factor was found to be useful to build level A correlation. The developed in vitro-in vivo correlation model was validated as per Food and Drug Administration guideline and the % prediction error for maximum concentration observed (C max) and area under the concentration time curve was within acceptable limits of below 15%. The utility of the developed model was evaluated by testing the targeted formulations. The observed % prediction error was 2.61 and-0.43 for C max and area under the concentration time curve, respectively suggesting the usefulness of the present in vitro-in vivo correlation model.

show abstract

“…Several publications have demonstrated that mechanistic oral absorption/PBPK models have superior predictive power and are more accurate for interspecies scaling when compared to allometric scaling approaches. 9,10 Lysosomes are single-membrane intracellular organelles, characterized by a low internal pH of 4-5. They play a major role in cellular homoeostasis such as the recycling of defective organelles, breaking down of macromolecules, engulfment of exogenous pathogens, and cell death control.…”

Section: Introductionmentioning

confidence: 99%

The Irrelevance of In Vitro Dissolution in Setting Product Specifications for Drugs Like Dextromethorphan That are Subject to Lysosomal Trapping

Bolger

Macwan

Sarfraz

et al. 2019

Journal of Pharmaceutical Sciences

View full text Add to dashboard Cite

Application of physiologically based pharmacokinetic modeling in the prediction of pharmacokinetics of bicyclol controlled-release formulation in human

Cited by 20 publications

References 29 publications

Qualification and application of liquid chromatography-quadrupole time-of-flight mass spectrometric method for the determination of carisbamate in rat plasma and prediction of its human pharmacokinetics using physiologically based pharmacokinetic modeling

Qualification and application of liquid chromatography-quadrupole time-of-flight mass spectrometric method for the determination of carisbamate in rat plasma and prediction of its human pharmacokinetics using physiologically based pharmacokinetic modeling

Development and Validation of an In Vitro and In Vivo Correlation Model in NZ Rabbit for Topiramate Extended Release Capsules

The Irrelevance of In Vitro Dissolution in Setting Product Specifications for Drugs Like Dextromethorphan That are Subject to Lysosomal Trapping

Contact Info

Product

Resources

About