1,952 results match your criteria European Journal of Drug Metabolism and Pharmacokinetics[Journal]


Population Pharmacokinetics and Exposure-Response of Lithium Carbonate in Patients Based on Tubular Reabsorption Mechanisms.

Eur J Drug Metab Pharmacokinet 2018 Dec 7. Epub 2018 Dec 7.

Department of Pharmacy, Fukuoka University Hospital, 7-45-1 Nanakuma, Zyounan-ku, Fukuoka, 814-0180, Japan.

Background And Objective: Lithium, which is used to treat bipolar disorder, has a narrow therapeutic blood concentration range and quickly reaches clinically toxic levels. We performed a population pharmacokinetic analysis with a lithium tubular reabsorption model including urinary pH and investigated the relationship between blood lithium concentration and tremor as a side effect.

Methods: Routine clinical data, including 389 serum concentrations, were collected from 214 patients orally administered an adjusted amount of lithium carbonate. Read More

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http://dx.doi.org/10.1007/s13318-018-0536-0DOI Listing
December 2018

Advanced In Vitro HepaRG Culture Systems for Xenobiotic Metabolism and Toxicity Characterization.

Eur J Drug Metab Pharmacokinet 2018 Dec 10. Epub 2018 Dec 10.

Faculty of Pharmacy and Pharmaceutical Sciences, Katz Group Centre for Pharmacy and Health Research, Room 3-142D, 11361-87 Ave, Edmonton, AB, T6G 2E1, Canada.

Several HepaRG three-dimensional (3D) in vitro model systems have been developed to improve the predictability of xenobiotic metabolism and toxicity. In this review, we present a detailed summary and critique of the performance of various HepaRG 3D models compared to the conventional 2D monolayer culture. HepaRG 3D models can be broadly categorized into (1) scaffold-free, (2) scaffold-based, and (3) bioartificial liver (BAL) models. Read More

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http://dx.doi.org/10.1007/s13318-018-0533-3DOI Listing
December 2018

Population Pharmacokinetics, Safety and Tolerability of Extended-Release Bupropion and Its Three Metabolites in Chinese Healthy Volunteers.

Eur J Drug Metab Pharmacokinet 2018 Dec 5. Epub 2018 Dec 5.

Shanghai Mental Health Center, Shanghai Jiao Tong University School of Medicine, 4/F, 604 Lingling Road, Shanghai, 200030, China.

Background And Objective: Bupropion is used for the treatment of major depressive disorder. We determined the pharmacokinetics, safety, and tolerability of extended-release bupropion XL in healthy Chinese volunteers.

Methods: This open-label, single-center pharmacokinetic study was conducted between May 2016 and June 2016. Read More

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http://dx.doi.org/10.1007/s13318-018-0537-zDOI Listing
December 2018
2 Reads

Development of a Population Pharmacokinetic Model of Vancomycin and its Application in Chinese Geriatric Patients with Pulmonary Infections.

Eur J Drug Metab Pharmacokinet 2018 Nov 30. Epub 2018 Nov 30.

Department of Nephrology, Peking University First Hospital, No.1 Dahongluochang Street, Xicheng District, Beijing, China.

Background: The optimal use of vancomycin in the elderly requires information about the drug's pharmacokinetics and the influence of various factors on the drug's disposition. However, because of sampling restrictions, it is often difficult to perform traditional pharmacokinetic studies in elderly patients.

Objective: This study was conducted to estimate the population pharmacokinetics of vancomycin in Chinese geriatric patients (age ≥ 65 years) with pulmonary infections and to explore the clinical application of this information for vancomycin dose individualization. Read More

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http://dx.doi.org/10.1007/s13318-018-0534-2DOI Listing
November 2018
1 Read

Comparison of the Pharmacokinetic Profiles of Ceftriaxone Used Alone and Combined with Danhong Injection in Old Rats.

Eur J Drug Metab Pharmacokinet 2018 Dec 3. Epub 2018 Dec 3.

Jiangsu Collaborative Innovation Center of Chinese Medicinal Resources, Jiangsu Key Laboratory for High Technology Research of TCM Formulae, National and Local Collaborative Engineering Center of Chinese Medicinal Resources Industrialization and Formulae Innovative Medicine, Nanjing University of Chinese Medicine, No. 138, Xianlin Avenue, Nanjing, 210046, People's Republic of China.

Background And Objectives: Danhong injection is the most commonly prescribed adjuvant drug applied for the treatment of cardiovascular and cerebrovascular diseases in China. Ceftriaxone is usually prescribed along with Danhong injection to elderly patients with complications. However, the pharmacokinetic interactions between these two medications have not been investigated. Read More

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http://dx.doi.org/10.1007/s13318-018-0530-6DOI Listing
December 2018

A Gallbladder-Based Enterohepatic Circulation Model for Pharmacokinetic Studies.

Eur J Drug Metab Pharmacokinet 2018 Nov 28. Epub 2018 Nov 28.

Department of Experimental and Clinical Pharmacology, College of Pharmacy, University of Minnesota, Minneapolis, MN, USA.

Background And Objectives: Strategies for modeling the enterohepatic circulation (EHC) process reported in the literature vary; however, gallbladder-based models currently provide the best physiological representation of the process. Regardless, the addition of a gallbladder to the model does not fully depict the physiology of EHC. A more physiological gallbladder-based EHC model is needed. Read More

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http://link.springer.com/10.1007/s13318-018-0535-1
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http://dx.doi.org/10.1007/s13318-018-0535-1DOI Listing
November 2018
10 Reads

Conversion from Twice-Daily Prograf to Once-Daily Advagraf in Multi-ethnic Asian Adult Renal Transplant Recipients With or Without Concomitant Use of Diltiazem: Impact of CYP3A5 and MDR1 Genetic Polymorphisms on Tacrolimus Exposure.

Eur J Drug Metab Pharmacokinet 2018 Nov 23. Epub 2018 Nov 23.

National University Centre for Organ Transplantation, National University Hospital, Singapore, Republic of Singapore.

Background And Objectives: Tacrolimus is the mainstay of immunosuppression in renal transplantation. Given that once-daily administration improves patient compliance, 1:1 dose conversion from twice-daily Prograf to once-daily Advagraf is recommended. Although cytochrome P450 (CYP) 3A5 and multi-drug resistance 1 (MDR1) polymorphisms influence tacrolimus concentrations, it is unknown if these impact on conversion. Read More

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http://dx.doi.org/10.1007/s13318-018-0531-5DOI Listing
November 2018
3 Reads

A Physiologically Based Pharmacokinetic Model for Optimally Profiling Lamotrigine Disposition and Drug-Drug Interactions.

Eur J Drug Metab Pharmacokinet 2018 Nov 20. Epub 2018 Nov 20.

School of Pharmacy, Husson University, 1 College Circle, Bangor, ME, 04401, USA.

Background And Objectives: Lamotrigine (Lamictal) is a broad-spectrum antiepileptic drug available in both immediate-(IR) and extended-release (XR) formulations. Here, we present a new physiologically based pharmacokinetic (PBPK) model for IR and XR formulations of lamotrigine to predict disposition in adults and children, plus drug-drug interactions (DDIs).

Methods: Models for lamotrigine IR and XR formulations were constructed using a Simcyp Simulator. Read More

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http://dx.doi.org/10.1007/s13318-018-0532-4DOI Listing
November 2018
1 Read

Retraction Note to: Changes of Absorptive and Secretory Transporting System of (1 → 3) β-D-glucan Based on Efflux Transporter in Indomethacin-induced Rat.

Eur J Drug Metab Pharmacokinet 2018 Dec;43(6):769

Department of Drug Absorption and Pharmacokinetics, School of Pharmacy, Tokyo University of Pharmacy and Life Sciences, 1432-1 Horinouchi, Hachioji, Tokyo, 192-0392, Japan.

The Editor-in-Chief has retracted this article [1] based on an investigation by the Ministry of Education, Culture, Sports, Science and Technology, Japan, which found that the article contained overlap with a previously published article by Kalitsky-Szirtes J, et al. [2]. Read More

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http://dx.doi.org/10.1007/s13318-018-0529-zDOI Listing
December 2018

Clinical Application of Pharmacokinetics: Basis for Rational Dose Selection in a Critically Ill Patient on Renal Replacement Therapy.

Eur J Drug Metab Pharmacokinet 2018 Nov 13. Epub 2018 Nov 13.

Pharmacology and Toxicology Department, Faculty of Medical Sciences, University of Kragujevac, Svetozara Markovića Street, 69, 34000, Kragujevac, Serbia.

Background: Individualizing drug dosing regimens in critically ill patients on renal replacement therapy is a challenge to clinicians as guidelines are often imprecise and specific-validated pharmacokinetic software is unavailable.

Objective: A case of a septic patient on hemodialysis is presented, where a quick solution for antibiotic dose adjustment based on the application of pharmacokinetic principles was found.

Methods: The dose adjustment was made in two steps-the first step was to calculate total antibiotic clearance (using the formula: total drug clearance = dialysate flow rate × fraction of unbound drug in plasma + extrarenal clearance), and the second step was to calculate maintenance dose based on target plasma concentrations in steady-state (using the formula: maintenance dose = target plasma concentration × total drug clearance × dose interval). Read More

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http://link.springer.com/10.1007/s13318-018-0524-4
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http://dx.doi.org/10.1007/s13318-018-0524-4DOI Listing
November 2018
2 Reads

Hepatic Cytochrome P450 Activity and Nitric Oxide Production During Multiple Ovalbumin Challenges.

Eur J Drug Metab Pharmacokinet 2018 Nov 8. Epub 2018 Nov 8.

Laboratory of Pharmaceutics, Faculty of Pharmaceutical Sciences, Tokushima Bunri University, 180 Bouji Nishihama, Yamashiro-cho, Tokushima, Tokushima, 770-8514, Japan.

Background And Objectives: Mast cell-mediated allergic diseases are a significant global health problem. Nitric oxide (NO) produced by acute type 1 allergies greatly suppresses hepatic cytochrome P450 (CYP) metabolism. A recent in vitro study demonstrated that repeated FcεRI-mediated activation intrinsically modulates mast cell function. Read More

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http://link.springer.com/10.1007/s13318-018-0527-1
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http://dx.doi.org/10.1007/s13318-018-0527-1DOI Listing
November 2018
3 Reads

Pharmacokinetics and Pharmacodynamics of Cabotegravir, a Long-Acting HIV Integrase Strand Transfer Inhibitor.

Eur J Drug Metab Pharmacokinet 2018 Nov 1. Epub 2018 Nov 1.

Gestione Ambulatoriale Politerapie (GAP) Outpatient Clinic, ASST Fatebenefratelli Sacco University Hospital, via GB Grassi 74, 20157, Milan, Italy.

Available antiretroviral drugs have demonstrated effectiveness in both pre-exposure prophylaxis and treatment of HIV infection. However, some concerns still persist regarding these therapies, mainly related to patient adherence, drug toxicity and dosing convenience. Cabotegravir is a potent integrase strand transfer inhibitor with a chemical structure similar to dolutegravir that is under clinical evaluation both as oral and long-acting injectable (LAI) formulations for both the prevention or treatment of HIV infection. Read More

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http://dx.doi.org/10.1007/s13318-018-0526-2DOI Listing
November 2018

Pharmacokinetics and Safety of Recombinant Human Interleukin-1 Receptor Antagonist GR007 in Healthy Chinese Subjects.

Eur J Drug Metab Pharmacokinet 2018 Oct 31. Epub 2018 Oct 31.

Department of Pharmacy, Peking University First Hospital, Beijing, 100034, China.

Background And Objectives: The recombinant human interleukin-1 receptor antagonist (rhIL-1Ra) GR007 is a candidate drug with the potential to prevent the toxicity induced by chemotherapy agents by blocking the IL-1 signaling pathway. The aim of this study was to assess the pharmacokinetics and safety of GR007 in healthy Chinese subjects.

Methods: Thirty subjects received a single intramuscular injection of 30 mg (n = 10), 90 mg (n = 10), or 150 mg (n = 10) GR007. Read More

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http://link.springer.com/10.1007/s13318-018-0523-5
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http://dx.doi.org/10.1007/s13318-018-0523-5DOI Listing
October 2018
2 Reads

Effects of Phenothiazines on Aldehyde Oxidase Activity Towards Aldehydes and N-Heterocycles: an In Vitro and In Silico Study.

Eur J Drug Metab Pharmacokinet 2018 Oct 31. Epub 2018 Oct 31.

School of Pharmacy, Tabriz University of Medical Sciences, Tabriz, Iran.

Background: Aldehyde oxidase (AOX) is an important molybdenum-containing enzyme with high similarity with xanthine oxidase (XO). AOX involved in the metabolism of a large array of aldehydes and N-heterocyclic compounds and its activity is highly substrate-dependent.

Objectives: The aim of this work was to study the effect of five important phenothiazine drugs on AOX activity using benzaldehyde and phenanthridine as aldehyde and N-heterocyclic substrates, respectively. Read More

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http://dx.doi.org/10.1007/s13318-018-0514-6DOI Listing
October 2018

Population Pharmacokinetic Analysis of Immediate-Release Oral Tacrolimus Co-administered with Mycophenolate Mofetil in Corticosteroid-Free Adult Kidney Transplant Recipients.

Eur J Drug Metab Pharmacokinet 2018 Oct 30. Epub 2018 Oct 30.

Faculty of Pharmacy and Pharmaceutical Sciences, University of Alberta, Edmonton, AB, Canada.

Background And Objective: Tacrolimus is the mainstay calcineurin inhibitor frequently administered with mycophenolic acid with or without corticosteroids to prevent graft rejection in adult kidney transplant recipients. The primary objective of this study was to develop and evaluate a population pharmacokinetic model characterizing immediate-release oral tacrolimus co-administered with mycophenolate mofetil (a pro-drug of mycophenolic acid) in adult kidney transplant recipients on corticosteroid-free regimens. The secondary objective was to investigate the effects of clinical covariates on the pharmacokinetics of tacrolimus, emphasizing the interacting effects of mycophenolic acid. Read More

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http://dx.doi.org/10.1007/s13318-018-0525-3DOI Listing
October 2018

In Vitro Assessment of Potential for CYP-Inhibition-Based Drug-Drug Interaction Between Vonoprazan and Clopidogrel.

Eur J Drug Metab Pharmacokinet 2018 Oct 25. Epub 2018 Oct 25.

d3 Medicine, A Certara Company, London, UK.

Background And Objectives: It was recently proposed that CYP-mediated drug-drug interactions (DDIs) of vonoprazan with clopidogrel and prasugrel can attenuate the antiplatelet actions of the latter two drugs. Clopidogrel is metabolized to the pharmacologically active metabolite H4 and its isomers by multiple CYPs, including CYP2C19 and CYP3A4. Therefore, to investigate the possibility of CYP-based DDIs, in vitro metabolic inhibition studies using CYP probe substrates or radiolabeled clopidogrel and human liver microsomes (HLMs) were conducted in this work. Read More

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http://link.springer.com/10.1007/s13318-018-0521-7
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http://dx.doi.org/10.1007/s13318-018-0521-7DOI Listing
October 2018
3 Reads

Population Pharmacokinetic Modeling of Azithromycin Eyedrops in Tears Following Single-Dose Topical Administration in Healthy Volunteers.

Eur J Drug Metab Pharmacokinet 2018 Oct 24. Epub 2018 Oct 24.

Department of Pharmacy, Peking University First Hospital, Beijing, China.

Background And Objectives: The disposition of azithromycin in the human eye following topical administration has not been fully explored. Population pharmacokinetic (PopPK) modeling can allow useful conclusions to be drawn based on limited tear sampling data. The aim of this study was therefore to develop and evaluate a PopPK model of azithromycin eyedrops in tears, investigate typical model parameters, and identify potential covariates following single-dose ocular instillation. Read More

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http://link.springer.com/10.1007/s13318-018-0522-6
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http://dx.doi.org/10.1007/s13318-018-0522-6DOI Listing
October 2018
3 Reads

Mechanistic Assessment of the Effect of Omeprazole on the In Vivo Pharmacokinetics of Itraconazole in Healthy Volunteers.

Eur J Drug Metab Pharmacokinet 2018 Oct 16. Epub 2018 Oct 16.

Australian Centre for Pharmacometrics and Sansom Institute, School of Pharmacy and Medical Sciences, University of South Australia, Adelaide, SA, Australia.

Background And Objective: SUBA-itraconazole and Sporanox are two oral formulations of itraconazole. Drug-drug interactions with omeprazole have been previously reported; however, mechanistic understanding of the pharmacological and physiological interactions of omeprazole with orally administered itraconazole within a population modeling paradigm is lacking. The objective of this analysis was to mechanistically describe and quantify the effect of omeprazole on the pharmacokinetics of itraconazole and its major metabolite, hydroxyitraconazole from the SUBA itraconazole and Sporanox formulations. Read More

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http://dx.doi.org/10.1007/s13318-018-0519-1DOI Listing
October 2018

Improved Oral Absorption of Quercetin from Quercetin Phytosome®, a New Delivery System Based on Food Grade Lecithin.

Eur J Drug Metab Pharmacokinet 2018 Oct 16. Epub 2018 Oct 16.

Research and Development Department, Indena SpA, 20139, Milan, Italy.

Background And Objectives: The importance of quercetin and flavonoids in the diet and as food supplements is well known, and literature studies support their potential use to treat several human diseases. Many beneficial properties have been described for quercetin, so much effort has been directed into overcoming the major drawbacks of this natural compound-its poor solubility and low oral absorption. The aims of this study were to compare a new food-grade lecithin-based formulation of quercetin, Quercetin Phytosome, to unformulated quercetin in terms of solubility in simulated gastrointestinal fluids and oral absorption in a randomized crossover pharmacokinetic study of healthy volunteers. Read More

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http://link.springer.com/10.1007/s13318-018-0517-3
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http://dx.doi.org/10.1007/s13318-018-0517-3DOI Listing
October 2018
6 Reads

Clinical Pharmacokinetics and Pharmacodynamics of Delafloxacin.

Eur J Drug Metab Pharmacokinet 2018 Oct 15. Epub 2018 Oct 15.

Faculty of Pharmacy and Pharmaceutical Sciences, University of Alberta, Room 3-142D, 11,361-87 Ave, Edmonton, AB, T6G 2E1, Canada.

Delafloxacin has recently received approval by the US Food and Drug Administration for the treatment of acute bacterial skin and skin structure infections. This article provides a balanced and comprehensive systematic critique of the literature in order to provide an up-to-date summary of its clinical pharmacology. Oral delafloxacin is rapidly absorbed and exhibits comparable exposure characteristics (300 mg intravenous versus 450 mg oral) between the two formulations, allowing easy transition from intravenous to oral therapy. Read More

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http://link.springer.com/10.1007/s13318-018-0520-8
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http://dx.doi.org/10.1007/s13318-018-0520-8DOI Listing
October 2018
8 Reads

Pharmacokinetics Comparison, Intestinal Absorption and Acute Toxicity Assessment of a Novel Water-Soluble Astragaloside IV Derivative (Astragalosidic Acid, LS-102).

Eur J Drug Metab Pharmacokinet 2018 Oct 12. Epub 2018 Oct 12.

Chengdu Institute of Biology, Chinese Academy of Sciences, Chengdu, China.

Background And Objectives: Astragaloside IV (AGS IV) is the most important bioactive constituent of Radix Astragali. However, its disappointing clinical application is mainly caused by its very low solubility in biologic fluids, resulting in poor bioavailability after oral administration. We recently obtained a novel water-soluble derivative of AGS IV (astragalosidic acid, LS-102) that displayed significant cardioprotective potential against hypoxia-induced injury. Read More

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http://dx.doi.org/10.1007/s13318-018-0515-5DOI Listing
October 2018

Effect of 95% Ethanol Khat Extract and Cathinone on in vitro Human Recombinant Cytochrome P450 (CYP) 2C9, CYP2D6, and CYP3A4 Activity.

Eur J Drug Metab Pharmacokinet 2018 Oct 10. Epub 2018 Oct 10.

Department of Biomedical Science, The University of Nottingham Malaysia Campus, Jalan Broga, 43500, Semenyih, Selangor Darul Ehsan, Malaysia.

Background And Objective: A significant number of people worldwide consume khat on daily basis. Long term of khat chewing has shown negative impact on several organ systems. It is likely that these people are co-administered khat preparations and conventional medication, which may lead to khat-drug interactions. Read More

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http://dx.doi.org/10.1007/s13318-018-0518-2DOI Listing
October 2018

Comparison of In Vitro Stereoselective Metabolism of Bupropion in Human, Monkey, Rat, and Mouse Liver Microsomes.

Eur J Drug Metab Pharmacokinet 2018 Oct 8. Epub 2018 Oct 8.

Graduate School of Pharmaceutical Sciences, Duquesne University, 600 Forbes Avenue, Pittsburgh, PA, 15282, USA.

Background And Objectives: Bupropion is an atypical antidepressant and smoking cessation aid associated with wide intersubject variability. This study compared the formation kinetics of three phase I metabolites (hydroxybupropion, threohydrobupropion, and erythrohydrobupropion) in human, marmoset, rat, and mouse liver microsomes. The objective was to establish suitability and limitations  for subsequent use of nonclinical species to model bupropion central nervous system (CNS) disposition in humans. Read More

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http://link.springer.com/10.1007/s13318-018-0516-4
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http://dx.doi.org/10.1007/s13318-018-0516-4DOI Listing
October 2018
5 Reads
1.312 Impact Factor

Clinical Pharmacokinetics of Second-Generation Triazoles for the Treatment of Invasive Aspergillosis and Candidiasis.

Eur J Drug Metab Pharmacokinet 2018 Oct 3. Epub 2018 Oct 3.

Faculty of Medical Sciences, University of Kragujevac, Zmaj Jovina Street, 30, Kragujevac, 34000, Serbia.

Second-generation triazoles were developed in response to the quest for more efficacious and safer therapeutic options for the treatment of severe systemic aspergillosis and candidiasis. These agents include voriconazole, posaconazole, isavuconazole, and ravuconazole. The aim of this review was to present and compare the pharmacokinetic characteristics of second-generation triazoles for the treatment of invasive aspergillosis and candidiasis, emphasizing their clinical implications. Read More

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http://link.springer.com/10.1007/s13318-018-0513-7
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http://dx.doi.org/10.1007/s13318-018-0513-7DOI Listing
October 2018
7 Reads

Longitudinal Pharmacokinetics of Mycophenolic Acid in Elderly Renal Transplant Recipients Compared to a Younger Control Group: Data from the nEverOld Trial.

Eur J Drug Metab Pharmacokinet 2018 09 18. Epub 2018 Sep 18.

Renal Transplantation Service, Division of Urology, Hospital das Clínicas, São Paulo University School of Medicine, Av. Dr.Enéas de Carvalho Aguiar, 255, São Paulo, 05403-900, Brazil.

Background And Objectives: Elderly patients are increasingly likely to be recipients of transplants. However, the pharmacokinetics of mycophenolic acid (MPA) in this population are yet to be studied in detail. The objective of this study was to assess whether there were differences in MPA pharmacokinetic parameter values between elderly recipients and younger-adult recipients during the 6 months immediately following renal transplantation. Read More

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http://dx.doi.org/10.1007/s13318-018-0506-6DOI Listing
September 2018
2 Reads

Determination of the Pharmacokinetics and Tissue Distribution of Methyl 3,4-Dihydroxybenzoate (MDHB) in Mice Using Liquid Chromatography-Tandem Mass Spectrometry.

Eur J Drug Metab Pharmacokinet 2018 Sep 17. Epub 2018 Sep 17.

Department of Pharmacology, School of Medicine, Jinan University, Guangzhou, China.

Background And Objectives: Methyl 3,4-dihydroxybenzoate (MDHB) has the potential to prevent neurodegenerative diseases (NDDs). The present work aims to reveal the pharmacokinetics and tissue distribution characteristics of MDHB.

Methods: The pharmacokinetics and tissue distribution of MDHB were analyzed using LC-MS/MS after a single intragastric administration (50 to 450 mg/kg) in mice, and samples were collected from five animals at specific time points. Read More

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http://dx.doi.org/10.1007/s13318-018-0512-8DOI Listing
September 2018
1 Read
1.312 Impact Factor

Pharmacokinetics and Bioavailability Enhancement of Baicalin: A Review.

Eur J Drug Metab Pharmacokinet 2018 Sep 12. Epub 2018 Sep 12.

Department of Pharmacy, Tongji Hospital, Tongji Medical College, Huazhong University of Science and Technology, Wuhan, 430030, China.

Baicalin is one of the major bioactive components of Scutellaria radix, a Chinese herb that has been used since ancient times. Baicalin has various pharmacological activities, including antitumor, antimicrobial, and antioxidant, and has wide clinical applications. Baicalin displays a distinct pharmacokinetic profile including gastrointestinal hydrolysis, enterohepatic recycling, carrier-mediated transport, and complicated metabolism. Read More

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http://dx.doi.org/10.1007/s13318-018-0509-3DOI Listing
September 2018
11 Reads

Intestinal Absorption of Isoalantolactone and Alantolactone, Two Sesquiterpene Lactones from Radix Inulae, Using Caco-2 Cells.

Eur J Drug Metab Pharmacokinet 2018 Sep 12. Epub 2018 Sep 12.

School of Pharmacy, Shanghai Jiao Tong University, No. 800 Dongchuan Road, Minhang District, Shanghai, 200240, People's Republic of China.

Background: Isoalantolactone and alantolactone are the main sesquiterpene lactones in Radix Inulae (dried root of Inula helenium L. or I. racemosa Hook. Read More

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http://link.springer.com/10.1007/s13318-018-0510-x
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http://dx.doi.org/10.1007/s13318-018-0510-xDOI Listing
September 2018
7 Reads

Correction to: Evaluation of Generic Methods to Predict Human Pharmacokinetics Using Physiologically Based Pharmacokinetic Model for Early Drug Discovery of Tyrosine Kinase Inhibitors.

Eur J Drug Metab Pharmacokinet 2018 Sep 11. Epub 2018 Sep 11.

Shanghai PharmoGo Co., Ltd, 3F, Block B, Weitai Building, No. 58, Lane 91, Shanghai, 200127, People's Republic of China.

The original version of this article unfortunately contained a mistake. Conflict of interest statement was incorrect. The corrected COI statement is given below. Read More

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http://dx.doi.org/10.1007/s13318-018-0511-9DOI Listing
September 2018

The Influence of Diabetes Mellitus on Glucuronidation and Sulphation of Paracetamol in Patients with Febrile Neutropenia.

Eur J Drug Metab Pharmacokinet 2018 Sep 5. Epub 2018 Sep 5.

Department of Clinical Pharmacy and Biopharmacy, Medical University of Poznań, Marii Magdaleny 14, 61-861, Poznań, Poland.

Background And Objectives: Numerous studies have confirmed the influence of diabetes mellitus on the pharmacokinetics of drugs. Paracetamol (APAP) is an antipyretic that is commonly used in febrile neutropenia (FN) therapy. APAP is chiefly metabolised by glucuronidation and sulphation. Read More

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http://dx.doi.org/10.1007/s13318-018-0508-4DOI Listing
September 2018
1 Read

Impact of Efavirenz Metabolism on Loss to Care in Older HIV+ Africans.

Eur J Drug Metab Pharmacokinet 2018 Aug 30. Epub 2018 Aug 30.

Department of Medicine, Perelman School of Medicine, University of Pennsylvania, 3910 Powelton Ave., 2nd Floor, Philadelphia, PA, 19104, USA.

BACKGROUND AND OBJECTIVE: Efavirenz is commonly used in Africa and is frequently associated with neurocognitive toxicity, which may compromise clinical outcomes. Older individuals are at increased risk for drug toxicity and clinical outcomes may be worse in older age, particularly among those individuals with cytochrome P450 (CYP) 2B6 polymorphisms associated with slower efavirenz metabolism. The aim of this study was to determine if the CYP2B6 polymorphisms differentially impacts loss to care in older people. Read More

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http://link.springer.com/10.1007/s13318-018-0507-5
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http://dx.doi.org/10.1007/s13318-018-0507-5DOI Listing
August 2018
12 Reads

Evaluation of Drug Biliary Excretion Using Sandwich-Cultured Human Hepatocytes.

Eur J Drug Metab Pharmacokinet 2018 Aug 30. Epub 2018 Aug 30.

Centre de Recherche en Pharmacocinétique, Technologie Servier, 45000, Orléans, France.

Evaluation of hepatobiliary transport of drugs is an important challenge, notably during the development of new molecular identities. In this context, sandwich-cultured human hepatocytes (SCHH) have been proposed as an interesting and integrated tool for predicting in vitro biliary excretion of drugs. The present review was therefore designed to summarize key findings about SCHH, including their establishment, their main functional features and their use for the determination of canalicular transport and the prediction of in vivo biliary clearance and hepatobiliary excretion-related drug-drug interactions. Read More

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http://dx.doi.org/10.1007/s13318-018-0502-xDOI Listing
August 2018
16 Reads

Clinical Pharmacokinetics and Pharmacodynamics of Direct Oral Anticoagulants in Patients with Renal Failure.

Authors:
Roberto Padrini

Eur J Drug Metab Pharmacokinet 2018 Aug 30. Epub 2018 Aug 30.

Dipartimento di Medicina DIMED, Università degli Studi di Padova, Via Giustiniani 2, 35128, Padua, Italy.

A recent survey on the use of direct oral anticoagulants (DOACs) revealed that 43% of patients with atrial fibrillation and renal impairment were potentially overdosed and had a hazard ratio for major bleeding of 2.19. In this review, we analyse and discuss the effect of renal failure on the pharmacokinetics and pharmacodynamics of DOACs and of strategies proposed to adjust doses according to the level of renal dysfunction. Read More

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http://link.springer.com/10.1007/s13318-018-0501-y
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http://dx.doi.org/10.1007/s13318-018-0501-yDOI Listing
August 2018
6 Reads

Effect of CYP2C9 Polymorphisms on the Pharmacokinetics of Indomethacin During Pregnancy.

Eur J Drug Metab Pharmacokinet 2018 Aug 29. Epub 2018 Aug 29.

Department of Obstetrics and Gynecology, University of Texas Medical Branch, Galveston, TX, 77555, USA.

Background And Objective: Cytochrome P450 (CYP) 2C9 catalyzes the biotransformation of indomethacin to its inactive metabolite O-desmethylindomethacin (DMI). The aim of this work was to determine the effect of CYP2C9 polymorphisms on indomethacin metabolism in pregnant women.

Methods: Plasma concentrations of indomethacin and DMI at steady state were analyzed with a validated LC-MS/MS method. Read More

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http://link.springer.com/10.1007/s13318-018-0505-7
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http://dx.doi.org/10.1007/s13318-018-0505-7DOI Listing
August 2018
15 Reads

Simultaneous Determination of Rivaroxaban and Enalapril in Rat Plasma by UPLC-MS/MS and Its Application to A Pharmacokinetic Interaction Study.

Eur J Drug Metab Pharmacokinet 2018 Aug 27. Epub 2018 Aug 27.

Department of Neurosurgery, The People's Hospital of Lishui, Lishui, 323000, Zhejiang, China.

Background And Objectives: There have been no animal experiments and clinical studies on the pharmacokinetic interaction between rivaroxaban and enalapril. To investigate whether a potential pharmacokinetic interaction is present between rivaroxaban and enalapril, a rapid and sensitive Ultra performance liquid chromatography-tandem mass spectrometry (UPLC-MS/MS) method was developed and validated to determine the concentration of rivaroxaban and enalapril in rat plasma and was then applied to a pharmacokinetic interaction study.

Methods: The analytes were separated on an Acquity UPLC BEH C18 chromatography column (2. Read More

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http://dx.doi.org/10.1007/s13318-018-0504-8DOI Listing
August 2018
7 Reads

Predicting Human Pharmacokinetics: Physiologically Based Pharmacokinetic Modeling and In Silico ADME Prediction in Early Drug Discovery.

Authors:
Jian Shi Weibin Zha

Eur J Drug Metab Pharmacokinet 2018 Aug 23. Epub 2018 Aug 23.

MyoKardia Inc., 333 Allerton Ave, South San Francisco, CA, 94080, USA.

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http://dx.doi.org/10.1007/s13318-018-0503-9DOI Listing
August 2018
7 Reads

Biodistribution and Pharmacokinetics of Amblyomin-X, a Novel Antitumour Protein Drug in Healthy Mice.

Eur J Drug Metab Pharmacokinet 2018 Aug 21. Epub 2018 Aug 21.

Laboratory of Molecular Biology, Butantan Institute, São Paulo, SP, Brazil.

Background: Amblyomin-X is a recombinant protein under development for cancer treatment owing to its selective cytotoxic activity over several tumour cell lines and tumour regression in mice models. The aim of this study was to examine the distribution and pharmacokinetics of amblyomin-X in healthy female mice.

Methods: Amblyomin-X was injected intravenously into the healthy animals and at controlled times plasma and organs were removed and analysed for identification and quantification of the protein. Read More

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http://dx.doi.org/10.1007/s13318-018-0500-zDOI Listing
August 2018
8 Reads

Animal Pharmacokinetic/Pharmacodynamic Studies (APPS) Reporting Guidelines.

Eur J Drug Metab Pharmacokinet 2018 Oct;43(5):483-494

Polpharma Biologics, Gdański Park Naukowo-Technologiczny, ul. Trzy lipy 3, Gdańsk, Poland.

Animal pharmacokinetic/pharmacodynamic studies are commonly used to provide meaningful preclinical information that can be utilized by the scientific community to conduct first-in-human studies. Poor presentation and interpretation of the data limit study reproducibility, and may result in rejection when the study is submitted to a journal, leading to loss of time and resources at multiple levels. In addition, inconsistencies in reporting the results of animal studies may limit the ability to extrapolate the experimental findings to humans. Read More

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http://dx.doi.org/10.1007/s13318-018-0498-2DOI Listing
October 2018
13 Reads

Influence of Orally Administered Borneol on the Expression of Hepatic Transporters in Rats.

Eur J Drug Metab Pharmacokinet 2018 Aug 13. Epub 2018 Aug 13.

Hubei Province Key Laboratory of Biotechnology of Chinese Traditional Medicine, Hubei Collaborative Innovation Center for Green Transformation of Bio-resources, Hubei University, Wuhan, 430062, China.

Background And Objective: Borneol, a traditional Chinese medicine (TCM), is often orally co-administered with other TCM and chemical drugs, but the drug-drug interactions between borneol and the other compounds remains unclear. This work investigates the effect of orally administered borneol on the transcription and expression of hepatic uptake transporters (Ntcp, Oatp2b1, Oatp1a1, Oatp1a4, Oct1, Oct2, Octn2 and Oat2) and efflux transporters (Mdrla, Mrp2, Mrp4 and Mrp5) in rats, aiming to obtain essential information to guide its clinical applications.

Methods: Rats were administered borneol (33, 100 and 300 mg/kg/day, respectively) and vehicle (control) orally via intragastric gavage for 7 consecutive days. Read More

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http://link.springer.com/10.1007/s13318-018-0499-1
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http://dx.doi.org/10.1007/s13318-018-0499-1DOI Listing
August 2018
9 Reads

Clinical Pharmacokinetics and Drug Interactions of Doravirine.

Eur J Drug Metab Pharmacokinet 2018 Dec;43(6):637-644

College of Pharmacy, Qatar University, PO Box 2713, Doha, Qatar.

Doravirine is a new HIV-1 non-nucleoside reverse transcriptase inhibitor that has demonstrated a good efficacy and safety profile in clinical trials. It has a therapeutic profile that makes it an attractive option for treatment of HIV-1 infection. As such, there has been an increase in the published literature regarding the pharmacokinetics of doravirine and potential for drug-drug interactions. Read More

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http://dx.doi.org/10.1007/s13318-018-0497-3DOI Listing
December 2018
14 Reads

Evaluation of Generic Methods to Predict Human Pharmacokinetics Using Physiologically Based Pharmacokinetic Model for Early Drug Discovery of Tyrosine Kinase Inhibitors.

Eur J Drug Metab Pharmacokinet 2018 Jul 23. Epub 2018 Jul 23.

Shanghai PharmoGo Co., Ltd, 3F, Block B, Weitai Building, No. 58, Lane 91, Shanghai, 200127, People's Republic of China.

Background: Requirements for predicting human pharmacokinetics in drug discovery are increasing. Developing different methods of human pharmacokinetic prediction will facilitate lead optimization, candidate nomination, and dosing regimens before clinical trials at various early drug discovery stages.

Objectives: To develop and validate generic methods of human pharmacokinetic prediction to meet the requirements in early drug discovery. Read More

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http://dx.doi.org/10.1007/s13318-018-0496-4DOI Listing

Reduced Clearance of Phenobarbital in Advanced Cancer Patients near the End of Life.

Eur J Drug Metab Pharmacokinet 2018 Jul 19. Epub 2018 Jul 19.

Department of Pharmacy, NTT Medical Centre Tokyo, 5-9-22 Higashi-gotanda, Shinagawa-ku, Tokyo, 141-8625, Japan.

Background And Objectives: Little is known about the pharmacokinetics of phenobarbital in terminally ill cancer patients. We investigated whether phenobarbital clearance alters depending on the length of survival.

Methods: We retrospectively reviewed the clinical, laboratory, and therapeutic drug monitoring (TDM) records of patients who received parenteral or oral phenobarbital for 21 consecutive days or longer between 2000 and 2016. Read More

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http://dx.doi.org/10.1007/s13318-018-0495-5DOI Listing
July 2018
6 Reads

Pharmacokinetics of Tramadol and Celecoxib in Japanese and Caucasian Subjects Following Administration of Co-Crystal of Tramadol-Celecoxib (CTC): A Randomised, Open-Label Study.

Eur J Drug Metab Pharmacokinet 2018 Jun 28. Epub 2018 Jun 28.

Mundipharma Research Ltd, Cambridge Science Park, Milton Road, Cambridge, CB4 0AB, UK.

Background And Objectives: Co-Crystal of Tramadol-Celecoxib (CTC) is a first-in-class active pharmaceutical ingredient (API-API) co-crystal of rac-tramadol.HCl and celecoxib in a 1:1 molecular ratio (100 mg CTC: 44 mg rac-tramadol.HCl and 56 mg celecoxib). Read More

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http://dx.doi.org/10.1007/s13318-018-0491-9DOI Listing
June 2018
8 Reads

Bayesian Population Pharmacokinetic Modeling of Eltrombopag in Chronic Hepatitis C Patients.

Eur J Drug Metab Pharmacokinet 2018 Jun 14. Epub 2018 Jun 14.

School of Pharmacy, The University of Jordan, Amman, 11942, Jordan.

Background And Objectives: Eltrombopag is a thrombopoietic growth factor that is approved for the treatment of thrombocytopenia in chronic hepatitis C virus (HCV) patients. We aimed to describe eltrombopag population pharmacokinetics in hepatitis C patients. Bayesian statistical approach will be applied to screen for patients' characteristics associated with eltrombopag pharmacokinetic parameters. Read More

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http://dx.doi.org/10.1007/s13318-018-0490-xDOI Listing
June 2018
1 Read

Model-Informed Approaches for Alternative Aripiprazole Dosing Regimens and Missed Dose Management: Towards Better Adherence to Antipsychotic Pharmacotherapy.

Eur J Drug Metab Pharmacokinet 2018 Aug;43(4):471-473

Center for Drug Clinical Research, Shanghai University of Chinese Medicine, No. 1200 Cailun Rd, Shanghai, 201203, China.

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http://dx.doi.org/10.1007/s13318-018-0494-6DOI Listing
August 2018
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Population Pharmacokinetic Analysis and Model-Based Simulations of Aripiprazole for a 1-Day Initiation Regimen for the Long-Acting Antipsychotic Aripiprazole Lauroxil.

Eur J Drug Metab Pharmacokinet 2018 Aug;43(4):461-469

Alkermes, Inc., 852 Winter Street, Waltham, MA, 02451, USA.

BACKGROUND AND OBJECTIVES: Aripiprazole lauroxil (AL), a long-acting injectable antipsychotic for the treatment of schizophrenia, requires 21 days of oral aripiprazole supplementation upon initiation (21-day initiation regimen). An alternative 1-day initiation regimen utilizing a nano-crystalline milled dispersion of AL (AL) plus a single 30 mg oral aripiprazole dose achieved aripiprazole concentrations associated with therapeutic doses of aripiprazole in the same time frame as the 21-day initiation regimen when starting AL (441 or 882 mg). A population pharmacokinetic (PopPK) model was developed to describe aripiprazole pharmacokinetics following administration of AL, AL and oral aripiprazole, and evaluate dosing scenarios likely to be encountered in clinical practice. Read More

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http://dx.doi.org/10.1007/s13318-018-0488-4DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6060990PMC
August 2018
4 Reads

Application of a Volumetric Absorptive Microsampling Device to a Pharmacokinetic Study of Tacrolimus in Rats: Comparison with Wet Blood and Plasma.

Eur J Drug Metab Pharmacokinet 2018 Jun 25. Epub 2018 Jun 25.

Drug Metabolism and Pharmacokinetics, Eisai Co., Ltd, Tokodai 5-1-3, Tsukuba-shi, Ibaraki, 300-2635, Japan.

Background And Objectives: Volumetric absorptive microsampling (VAMS) devices are useful for sampling a smaller volume of blood from rodents in the preclinical setting. In the present study, we evaluated the proof of concept of a VAMS device by comparing the pharmacokinetic data of tacrolimus in rats among dried blood in VAMS, wet blood, and plasma.

Methods: Tacrolimus was administered orally, to rats, at a dose of 10 mg/kg. Read More

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http://dx.doi.org/10.1007/s13318-018-0493-7DOI Listing
June 2018
6 Reads

Population Pharmacokinetic Modeling of Remifentanil in Infants with Unrepaired Tetralogy of Fallot.

Eur J Drug Metab Pharmacokinet 2018 Jun 19. Epub 2018 Jun 19.

Department of Anesthesiology, Shanghai Children's Medical Center, Shanghai Jiao Tong University School of Medicine, 1678 Dongfang Rd, Shanghai, 200127, China.

Background: Although there is literature suggesting that pathophysiologic changes in children with congenital heart disease alter the pharmacokinetics of anesthetics and may result in dosage adjustment, limited information exists regarding the pharmacokinetics of remifentanil in infants with unrepaired tetralogy of Fallot (TOF). The objectives of the current analysis were to characterize the population pharmacokinetics of remifentanil in infants, and to evaluate the effects of TOF on remifentanil's pharmacokinetics.

Methods: Twenty-seven infants (16 with TOF and 11 with normal cardiac anatomy; aged 114-360 days) scheduled to undergo elective surgery under general anesthesia were recruited in the study. Read More

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http://dx.doi.org/10.1007/s13318-018-0489-3DOI Listing
June 2018
4 Reads

Pharmacokinetics of Ombitasvir, Paritaprevir, Ritonavir, and Dasabuvir in Healthy Chinese Subjects and HCV GT1b-Infected Chinese, South Korean and Taiwanese Patients.

Eur J Drug Metab Pharmacokinet 2018 Jun 16. Epub 2018 Jun 16.

Clinical Pharmacology and Pharmacometrics, AbbVie Inc, 1 North Waukegan Road, Bldg. AP31-3, North Chicago, IL, 60064, USA.

Background/purpose: The 3 direct-acting antiviral (3D) regimen of ombitasvir/paritaprevir/ritonavir plus dasabuvir has recently been approved in several Asian geographic regions for the treatment of hepatitis C virus (HCV) genotype (GT) 1 infection. The pharmacokinetics of the components of the 3D regimen with or without ribavirin were evaluated in healthy Chinese subjects and HCV GT1b-infected Chinese, South Korean, and Taiwanese patients, with or without cirrhosis, to determine how the drug exposures in Asian populations compare with historical data in Western populations.

Methods: Participants received ombitasvir/paritaprevir/ritonavir 25/150/100 mg once daily plus dasabuvir 250 mg twice daily for 14 days (healthy subjects, n = 36) or 12 weeks (HCV patients, n = 754). Read More

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http://dx.doi.org/10.1007/s13318-018-0492-8DOI Listing
June 2018
11 Reads

Nutritional Status Differentially Alters Cytochrome P450 3A4 (CYP3A4) and Uridine 5'-Diphospho-Glucuronosyltransferase (UGT) Mediated Drug Metabolism: Effect of Short-Term Fasting and High Fat Diet on Midazolam Metabolism.

Eur J Drug Metab Pharmacokinet 2018 Jun 6. Epub 2018 Jun 6.

Department of Hospital Pharmacy, Academic Medical Centre, University of Amsterdam, Meibergdreef 9, 1105 AZ, Amsterdam, The Netherlands.

Background And Objectives: Previous studies have shown that nutritional status can alter drug metabolism which may result in treatment failure or untoward side effects. This study assesses the effect of two nutritional conditions, short-term fasting, and a short-term high fat diet (HFD) on cytochrome P450 3A4 (CYP3A4) and uridine 5'-diphospho-glucuronosyltransferase (UGT) mediated drug metabolism by studying the pharmacokinetics of midazolam and its main metabolites.

Methods: In a randomized-controlled cross-over trial, nine healthy subjects received a single intravenous administration of 0. Read More

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http://dx.doi.org/10.1007/s13318-018-0487-5DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6244726PMC
June 2018
2 Reads