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Biopharmaceutics & Drug Disposition

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https://www.readbyqxmd.com/read/28744858/d-malate-decreases-renal-content-of-%C3%AE-ketoglutarate-a-driving-force-of-organic-anion-transporters-oat1-and-oat3-resulting-in-inhibited-tubular-secretion-of-phenolsulfonphthalein-in-rats
#1
Yuichi Uwai, Tatsuya Kawasaki, Tomohiro Nabekura
D-Malate inhibits a Krebs cycle enzyme and the tubular transport of α-ketoglutarate, an intermediate of the Krebs cycle and the driving force for rat organic anion transporter 1 (rOAT1) and rOAT3 in the kidney. In this study, we examined effects of D-malate on the rat organic anion transport system. Uptake of 6-carboxyfluorescein by HEK293 cells expressing rOAT1 or rOAT3 was not affected by D-malate and L-malate. Until 60 min after the intravenous injection of phenolsulfonphthalein (PSP), a typical substrate of the renal organic anion transporters, as a bolus to rats, 47...
July 25, 2017: Biopharmaceutics & Drug Disposition
https://www.readbyqxmd.com/read/28741675/pharmacokinetics-of-dinalbuphine-sebacate-and-nalbuphine-in-human-after-intramuscular-injection-of-dinalbuphine-sebacate-in-an-extended-release-formulation
#2
Yu En Tien, Wen-Chuan Huang, Hui-Yuan Kuo, Lily Tai, Yow-Shieng Uang, Wendy H Chern, Jin-Ding Huang
Nalbuphine is a semi-synthetic opioid indicated for the relief of moderate to severe pain. Its short half-life requires frequent injections in clinical practices, resulting in greater incidences of adverse events. We have developed a prodrug of nalbuphine, dinalbuphine sebacate (DNS), dissolved in a simple oil-based injectable formulation, which could deliver and maintain effective blood nalbuphine level. An open-label, prospective, two-period study was performed in healthy volunteers to verify the extended blood concentration profile of nalbuphine...
July 25, 2017: Biopharmaceutics & Drug Disposition
https://www.readbyqxmd.com/read/28710808/the-application-of-physiologically-based-pharmacokinetic-modelling-to-assess-the-impact-of-antiretroviral-mediated-drug-drug-interactions-on-piperaquine-antimalarial-therapy-during-pregnancy
#3
Olusola Olafuyi, Michael Coleman, Raj K S Badhan
Antimalarial therapy during pregnancy poses important safety concerns due to potential teratogenicity and maternal physiological and biochemical changes during gestation. Piperaquine (PQ) has gained interest for use in pregnancy in response to increasing resistance towards sulfadoxine-pyrimethamine in sub-Saharan Africa. Co-infection with HIV is common in many developing countries, however, little is known about the impact of anti-retroviral (ARV) mediated drug-drug interaction (DDI) on PQ pharmacokinetics during pregnancy...
July 14, 2017: Biopharmaceutics & Drug Disposition
https://www.readbyqxmd.com/read/28670738/clinical-assessment-of-the-lag-time-and-tmax-of-pellets-with-controlled-release-of-glucose-in-vitro-in-vivo-comparison-using-13-c-breath-test
#4
David Neumann, Jan Muselík, Dana Sabadková, Sylvie Pavloková, Jana Špirková, Aleš Franc
Maintaining a stable glycemia in diabetes mellitus type 1 requires flexible insulin application and carbohydrates intake to affected individuals. In real life, there might be some situations limiting the insulin-sugar balance control, e.g. night sleep or prolonged sport activities. Glucose pellets with pre-determined time lag between pellet administration and glucose release were developed to mimic "snack eaten in advance". In this article, (13) C-glucose breath test is introduced to translate the laboratory dissolution testing to clinical confirmation of the glucose release pattern using 5 per cent of δ abundance to differentiate (13) C appearance in exhaled breath...
July 3, 2017: Biopharmaceutics & Drug Disposition
https://www.readbyqxmd.com/read/28656708/letter-to-the-editor-physiologically-based-pharmacokinetic-predictions-of-intestinal-bcrp-mediated-effect-of-telmisartan-on-the-pharmacokinetics-of-rosuvastatin-in-humans
#5
LETTER
Ruben de Kanter, Christopher Kohl
No abstract text is available yet for this article.
June 28, 2017: Biopharmaceutics & Drug Disposition
https://www.readbyqxmd.com/read/28656677/author-s-response-to-letter-to-the-editor-on-physiologically-based-pharmacokinetic-predictions-of-intestinal-bcrp-mediated-effect-of-telmisartan-on-the-pharmacokinetics-of-rosuvastatin-in-humans
#6
https://www.readbyqxmd.com/read/28608515/efavirenz-clearances-in-vitro-and-in-vivo-in-six-cynomolgus-monkeys-associated-with-polymorphic-cytochrome-p450-2c9-and-simulated-by-individual-physiologically-based-pharmacokinetic-models
#7
Masahiro Utoh, Tomonori Miura, Takashi Kusama, Shotaro Uehara, Makiko Shimizu, Yasuhiro Uno, Hiroshi Yamazaki
Cynomolgus monkey cytochrome P450 2C9 (formerly known as P450 2C43) variation was reportedly associated with metabolic clearance of the antiretroviral drug efavirenz in vivo (of three wild-type, one heterozygote, and two homozygote animals), being unlikely in the case of human P450 2B6-dependent efavirenz clearance. In this study, the liver microsomal elimination rates of efavirenz for the same individual animals previously treated with intravenous/oral administrations of efavirenz showed significant reductions associated with the P450 2C9 p...
June 13, 2017: Biopharmaceutics & Drug Disposition
https://www.readbyqxmd.com/read/28608480/sgk1-nedd4-2-signaling-pathway-regulates-the-activity-of-human-organic-anion-transporters-3
#8
Haoxun Wang, Guofeng You
Human organic anion transporter 3 (hOAT3) is localized at the basolateral membrane of renal proximal tubule cells and facilitates renal secretion of numerous clinical drugs, including anti-HIV therapeutics, anti-tumor drugs, antibiotics, antihypertension drugs, and anti-inflammatories. In the present study, we explored the role of serum and glucocorticoid-inducible kinase 1 (sgk1) in the regulation of hOAT3. We showed that over-expression of sgk1 in hOAT3-expressing cells stimulated hOAT3 transport activity by enhancing the transporter expression at the plasma membrane, kinetically reflected as an increased maximal transport velocity Vmax without substantial change in substrate-binding affinity Km ...
June 13, 2017: Biopharmaceutics & Drug Disposition
https://www.readbyqxmd.com/read/28503751/in-vitro-evaluation-of-potential-transporter-mediated-drug-interactions-of-evogliptin
#9
Dae Y Lee, Hye W Chae, Hyun J Shim
To date, little is known about the transporter-mediated drug-drug interaction (DDI) potential of evogliptin, a novel DPP-4 inhibitor. The objective of this study was to evaluate the DDI potential of evogliptin using various in vitro assays in transporter-expressing cell lines. After incubating evogliptin with cells overexpressing OAT1, OAT3, OCT2, OATP1B1 and OATP1B3, there was no notable cellular accumulation of evogliptin (fold accumulation, 0.41-1.86). In bidirectional transport assays using a Caco-2 cell monolayer, a high efflux ratio (ER, 522) of evogliptin was observed, which was significantly decreased (97...
May 14, 2017: Biopharmaceutics & Drug Disposition
https://www.readbyqxmd.com/read/28474821/application-of-physiologically-based-pharmacokinetic-modeling-to-predict-drug-disposition-in-pregnant-populations
#10
Vamshi Krishna Jogiraju, Suvarchala Avvari, Rakesh Gollen, David R Taft
Pregnancy is associated with numerous physiological changes that influence absorption, distribution, metabolism and excretion. Moreover, the magnitude of these effects changes as pregnancy matures. For most medications, there is limited information available about changes in drug disposition that can occur in pregnant patients, yet most women are prescribed one or more medications during pregnancy. In this investigation, PBPK modeling was used to assess the impact of pregnancy on the pharmacokinetic profiles of three medications (metformin, tacrolimus, oseltamivir) using the Simcyp® simulator...
May 5, 2017: Biopharmaceutics & Drug Disposition
https://www.readbyqxmd.com/read/28474789/functional-characterization-and-tissue-expression-of-marmoset-cytochrome-p450-2e1
#11
Shotaro Uehara, Yasuhiro Uno, Etsuko Tomioka, Takashi Inoue, Erika Sasaki, Hiroshi Yamazaki
Common marmosets (Callithrix jacchus) have attracted increasing attention as a useful small non-human primate model in preclinical research. However, studies on marmoset cytochrome P450 (P450) 2E enzyme have scarcely been conducted. In this study, the full-length cDNA encoding P450 2E1 enzyme was isolated from marmoset livers by reverse transcription (RT)-polymerase chain reaction (PCR). Marmoset P450 2E1 amino acid sequences were highly identical (>88%) to those of cynomolgus monkey and human P450 2E1 enzymes...
May 5, 2017: Biopharmaceutics & Drug Disposition
https://www.readbyqxmd.com/read/28425104/inactivation-kinetics-and-residual-activity-of-cyp3a4-after-treatment-with-erythromycin
#12
Yuko Ishikawa, Takeshi Akiyoshi, Ayuko Imaoka, Hisakazu Ohtani
This study aimed to characterize the inactivation kinetics of cytochrome P450 3A4 (CYP3A4) by erythromycin, which involves mechanism-based inhibition (MBI), in detail. In addition to an MBI assay based on the conventional method in which erythromycin and recombinant CYP3A4 were pre-incubated for 15 min, the study also evaluated the long-term MBI kinetics of this reaction by pre-incubation for 120 min. Mechanism-based inhibition profiles were obtained using three typical substrates, testosterone, midazolam and nifedipine...
April 20, 2017: Biopharmaceutics & Drug Disposition
https://www.readbyqxmd.com/read/28374512/pharmacokinetic-analysis-of-inhaled-salmeterol-in-asthma-patients-evidence-from-two-dry-powder-inhalers
#13
Konstantina Soulele, Panos Macheras, Vangelis Karalis
Salmeterol (SAL) is a long-acting β2-adrenergic agonist, which is widely used in the asthma therapy. The aim of this study was to investigate the pharmacokinetics (PK) of inhaled SAL in asthma patients using two different dry powder inhalers. This analysis was based on data from 45 subjects who participated in a two-sequence, four period crossover bioequivalence (BE) study after single administration of the test (T) and reference (R) products. In order to mimic more closely the real treatment conditions, activated charcoal was not co-administered...
April 3, 2017: Biopharmaceutics & Drug Disposition
https://www.readbyqxmd.com/read/28207929/optimization-of-intestinal-microsomal-preparation-in-the-rat-a-systematic-approach-to-assess-the-influence-of-various-methodologies-on-metabolic-activity-and-scaling-factors
#14
Oliver J D Hatley, Christopher R Jones, Aleksandra Galetin, Amin Rostami-Hodjegan
The metabolic capacity of the intestine and its importance as the initial barrier to systemic exposure can lead to underestimation of first-pass, and thus overestimation of oral bioavailability. However, the in vitro tools informing estimates of in vivo intestinal metabolism are limited by the complexity of the in vitro matrix preparation and uncertainty with the scaling factors for in vitro to in vivo extrapolation. A number of methods currently exist in the literature for the preparation of intestinal microsomes; however, the impact of key steps in the preparation procedure has not been critically assessed...
April 2017: Biopharmaceutics & Drug Disposition
https://www.readbyqxmd.com/read/28152562/a-comparative-evaluation-of-models-to-predict-human-intestinal-metabolism-from-nonclinical-data
#15
Estelle Yau, Carl Petersson, Hugues Dolgos, Sheila Annie Peters
Extensive gut metabolism is often associated with the risk of low and variable bioavailability. The prediction of the fraction of drug escaping gut wall metabolism as well as transporter-mediated secretion (Fg ) has been challenged by the lack of appropriate preclinical models. The purpose of this study is to compare the performance of models that are widely employed in the pharmaceutical industry today to estimate Fg and, based on the outcome, to provide recommendations for the prediction of human Fg during drug discovery and early drug development...
April 2017: Biopharmaceutics & Drug Disposition
https://www.readbyqxmd.com/read/28032362/prioritizing-pharmacokinetic-drug-interaction-precipitants-in-natural-products-application-to-oatp-inhibitors-in-grapefruit-juice
#16
Emily J Johnson, Christina S Won, Kathleen Köck, Mary F Paine
Natural products, including botanical dietary supplements and exotic drinks, represent an ever-increasing share of the health-care market. The parallel ever-increasing popularity of self-medicating with natural products increases the likelihood of co-consumption with conventional drugs, raising concerns for unwanted natural product-drug interactions. Assessing the drug interaction liability of natural products is challenging due to the complex and variable chemical composition inherent to these products, necessitating a streamlined preclinical testing approach to prioritize precipitant individual constituents for further investigation...
April 2017: Biopharmaceutics & Drug Disposition
https://www.readbyqxmd.com/read/28294376/influence-of-the-pharmacokinetic-profile-on-the-plasma-glucose-lowering-effect-of-ppar%C3%AE-agonist-pioglitazone-in-wistar-fatty-rats
#17
Akihiko Goto, Yoshihiko Tagawa, Yoshiaki Kimura, Akifumi Kogame, Yuu Moriya, Nobuyuki Amano
Although the mechanism of action for peroxisome proliferator-activated receptor gamma (PPARγ) agonists has been extensively explored, the impact of the pharmacokinetic (PK) profile on the pharmacodynamic (PD) effects of PPARγ agonists has not been elucidated in detail. We evaluated the importance of the PK profile of PPARγ agonist for its PD effect based on population PK/PD analysis. Pioglitazone hydrochloride, the PPARγ agonist, was administered orally to Wistar fatty rats once a day (qd) or once every other day (q2d) as double the amount for the qd treatment...
March 11, 2017: Biopharmaceutics & Drug Disposition
https://www.readbyqxmd.com/read/28256717/impact-of-acute-fat-mobilisation-on-the-pharmacokinetics-of-the-highly-fat-distributed-compound-tak-357-investigated-by-physiologically-based-pharmacokinetic-pbpk-modeling-and-simulation
#18
Akihiko Goto, Yoshihiko Tagawa, Yuu Moriya, Sho Sato, Yoshiyuki Furukawa, Takeshi Wakabayashi, Tetsuya Tsukamoto, Joost DeJongh, Tamara J van Steeg, Toshiya Moriwaki, Satoru Asahi
In a dog toxicokinetic study, an unusual plasma concentration increase of the highly lipophilic compound TAK-357 was observed 2 weeks after termination of a 2-week repeated dosing in one dog with acute body weight loss. The present study investigates the cause of this increase. A physiologically based pharmacokinetic (PBPK) model was constructed using the rat and dog pharmacokinetic data. Using the constructed model, the TAK-357 concentration profile in the case of body weight change was simulated. The PBPK model-derived simulation suggested that redistribution from adipose tissues to plasma due to a loss of body fat caused the observed concentration increase of TAK-357 in dog plasma...
March 3, 2017: Biopharmaceutics & Drug Disposition
https://www.readbyqxmd.com/read/28255999/development-of-a-physiologically-based-pharmacokinetic-model-to-predict-the-effects-of-flavin-containing-monooxygenase-3-fmo3-polymorphisms-on-itopride-exposure
#19
Wangda Zhou, Helen Humphries, Sibylle Neuhoff, Iain Gardner, Eric Masson, Nidal Al-Huniti, Diansong Zhou
Itopride, a substrate of FMO3, has been used for the symptomatic treatment of various gastrointestinal disorders. Physiologically based pharmacokinetic (PBPK) modeling was applied to evaluate the impact of FMO3 polymorphism on itopride pharmacokinetics (PK). The Asian populations within the Simcyp simulator were updated to incorporate information on frequency, activity and abundance of FMO3 enzyme with different phenotypes. A meta-analysis of relative enzyme activities suggested that FMO3 activity in subjects with homozygous Glu158Lys and Glu308Gly mutations (Lys158 and Gly308) in both alleles is ~47% lower than those carrying two wild-type FMO3 alleles...
March 3, 2017: Biopharmaceutics & Drug Disposition
https://www.readbyqxmd.com/read/28317174/revisiting-the-role-of-gut-wall-in-the-fate-of-orally-administered-drugs-why-now-and-to-what-effect
#20
EDITORIAL
Amin Rostami-Hodjegan, Ikumi Tamai, K Sandy Pang
No abstract text is available yet for this article.
March 2017: Biopharmaceutics & Drug Disposition
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