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The possible clinical impact of risperidone on P ‐glycoprotein‐mediated transport of tacrolimus: A case report and in vitro study
Abstract The authors encountered the case of an 8‐fold increase in the concentration/dose (C/D) ratio of tacrolimus (TAC) following the coadministration of voriconazole (VRCZ) in a hematopoietic stem cell transplantation (HSCT) recipient. The interaction observed was much greater than expected and the patient had also been treated with oral risperidone (RSP). We hypothesized that cytochrome P450 (CYP)3A inhibition of the small intestine by VRCZ and P‐glycoprotein (P‐gp) inhibition of the small intestine by RSP exerted a synergistic effect on the bioavailability of TAC. The aim of the present study was to evaluate the...
Source: Biopharmaceutics and Drug Disposition - October 20, 2017 Category: Drugs & Pharmacology Authors: Nao Watanabe, Hiroki Higashi, Saki Nakamura, Keiko Nomura, Yuichi Adachi, Masato Taguchi Tags: ORIGINAL PAPER Source Type: research

Issue Information
No abstract is available for this article. (Source: Biopharmaceutics and Drug Disposition)
Source: Biopharmaceutics and Drug Disposition - October 8, 2017 Category: Drugs & Pharmacology Tags: ISSUE INFORMATION Source Type: research

Renal vectorial transport of berberine mediated by organic cation transporter 2 (OCT2) and multidrug and toxin extrusion proteins 1 (MATE1) in rats
This study aimed to investigate the renal transport mechanism of berberine using transfected cells, kidney slices, and animal experiments. In Madin‐Darby canine kidney (MDCK) cells stably expressing rat OCT2 (MDCK‐rOCT2) and kidney slices, saturable and non‐saturable uptake of berberine was observed, and corticosterone could inhibit the uptake of berberine, with IC50 values of 0.1 μM and 147.9 μM, respectively. In double‐transfected cells, the cellular accumulation of berberine into MDCK‐rOCT2 and MDCK‐rOCT2‐rMATE1 (MDCK cells stably expressing rOCT2 and rMATE1) cells was significantly higher than the uptak...
Source: Biopharmaceutics and Drug Disposition - October 1, 2017 Category: Drugs & Pharmacology Authors: Rong Shi, Yuanyuan Yang, Zhangyao Xu, Yan Dai, Zheng Min, Tianming Wang, Yuanyuan Li, Yueming Ma Tags: ORIGINAL PAPER Source Type: research

Molecular cloning and tissue distribution of a novel marmoset ABC transporter
In this study, a cDNA of novel ATP‐dependent efflux transporter ABCB1 was cloned from marmoset liver tissue. Marmoset ABCB1 cDNA encodes a protein of 1,279 amino acid residues (MW = 141.4 kDa) containing characteristic regions of an ATP‐binding cassette (ABC) protein, two hydrophobic transmembrane regions, and two cytoplasmic nucleotide‐binding regions, similar to human ABCB1. The deduced amino acid sequences were more highly identical (95%) to those of human ABCB1 compared with non‐primate species such as dogs, pigs, and rodents (79‐90%). A close evolutionary relationship of ABCB1 among marmosets, cynomolgus and...
Source: Biopharmaceutics and Drug Disposition - October 1, 2017 Category: Drugs & Pharmacology Authors: Shotaro Uehara, Yasuhiro Uno, Takashi Inoue, Erika Sasaki, Hiroshi Yamazaki Tags: SHORT COMMUNICATION Source Type: research

Contribution of Equilibrative Nucleoside Transporter(s) to Intestinal Basolateral and Apical Transports of Anticancer Trifluridine
In conclusion, ENTs were responsible for intestinal transepithelial permeation by mediating the basolateral efflux of FTD after its uptake by CNT1 from the apical side, resulting in decreases in its intracellular accumulation and intestinal toxicity in humans. ENTs may also partially contribute to the low‐affinity uptake of FTD across the apical membrane along with high‐affinity CNT1. (Source: Biopharmaceutics and Drug Disposition)
Source: Biopharmaceutics and Drug Disposition - October 1, 2017 Category: Drugs & Pharmacology Authors: Koichi Takahashi, Kunihiro Yoshisue, Masato Chiba, Takeo Nakanishi, Ikumi Tamai Tags: ORIGINAL PAPER Source Type: research

The application of physiologically based pharmacokinetic modelling to assess the impact of antiretroviral ‐mediated drug–drug interactions on piperaquine antimalarial therapy during pregnancy
This study applied mechanistic pharmacokinetic modelling to predict pharmacokinetics in non‐pregnant and pregnant patients, which was validated in distinct customised population groups from Thailand, Sudan and Papua New Guinea. In each population group, no significant differences in day 7 concentrations were observed during different gestational weeks (GW) (weeks 10–40), supporting the notion that piperaquine is safe throughout pregnancy with consistent pharmacokinetics, although possible teratogenicity may limit this. Antiretroviral‐mediated DDIs (efavirenz and ritonavir) had moderate effects on piperaquine during d...
Source: Biopharmaceutics and Drug Disposition - September 29, 2017 Category: Drugs & Pharmacology Authors: Olusola Olafuyi, Michael Coleman, Raj K.S. Badhan Tags: ORIGINAL PAPER Source Type: research

Issue Information
No abstract is available for this article. (Source: Biopharmaceutics and Drug Disposition)
Source: Biopharmaceutics and Drug Disposition - September 7, 2017 Category: Drugs & Pharmacology Tags: Issue Information Source Type: research

Hepatocellular uptake of cyclodextrin ‐complexed curcumin during liver preservation: A feasibility study
Abstract Increasing demand for donor organs and decreasing organ quality is prompting research toward new methods to reduce ischemia reperfusion injury (IRI). Several strategies have been proposed to protect the preserved organ from this injury. Before curcumin/dextrin complex (CDC), a potent antioxidant and anti‐inflammatory agent, can be used clinically we need to better understand the intracellular uptake under hypothermic conditions on rat model of liver donation after circulatory death (DCD) and brain death (DBD). To be able to use the fluorescence of CDC for quantification we investigate the stability of CDC in dif...
Source: Biopharmaceutics and Drug Disposition - September 1, 2017 Category: Drugs & Pharmacology Authors: Saber Abdelkader Saidi, Nicolas Meurisse, Ina Jochmans, Veerle Heedfeld, Tine Wylin, Jaakko Parkkinen, Jacques Pirenne, Diethard Monbaliu, Abdelfattah El Feki, Jos Pelt Tags: ORIGINAL PAPER Source Type: research

Prediction of drug ‐drug interactions using physiologically‐based pharmacokinetic models of CYP450 modulators included in Simcyp software
Abstract In recent years, Physiologically‐Based PharmacoKinetic (PBPK) modeling has received growing interest as a useful tool for assessment of drug PK. It has demonstrated to be informative and helpful to quantify the modification in drug exposure due to specific physio‐pathological conditions, age, genetic polymorphisms, ethnicity and particularly drug‐drug interactions (DDIs). In this paper, the prediction success of DDIs involving various cytochrome P450 isoenzyme (CYP) modulators namely ketoconazole (a competitive inhibitor of CYP3A), itraconazole (a competitive inhibitor of CYP3A), clarithromycin (a mechanism�...
Source: Biopharmaceutics and Drug Disposition - September 1, 2017 Category: Drugs & Pharmacology Authors: Niloufar Marsousi, Jules A. Desmeules, Serge Rudaz, Youssef Daali Tags: ORIGINAL PAPER Source Type: research

Influence of Body Composition on Disposition of the Highly Fat Distributed Compound as Analyzed by Physiologically ‐based Pharmacokinetic (PBPK) Modeling and Simulation
Abstract A recent study suggested that the pharmacokinetics (PK) of highly‐fat distributed compounds can be affected by acute changes in the volume of adipose tissue. The present study investigates possible influences of body composition on the disposition of the highly lipophilic compound TAK‐357 in two rat strains. Physiologically‐based PK (PBPK) modeling and simulation was applied on single and multiple dose PK data of TAK‐357 in obese Wistar fatty rats and Wistar lean rats having approximately 45% and 13% body fat, respectively. The observed effects of an elevated fat mass in Wistar fatty rats on the plasma con...
Source: Biopharmaceutics and Drug Disposition - September 1, 2017 Category: Drugs & Pharmacology Authors: Akihiko Goto, Yoshihiko Tagawa, Yuu Moriya, Sho Sato, Masami Yamamoto, Takeshi Wakabayashi, Tetsuya Tsukamoto, Joost DeJongh, Tamara J. Steeg, Toshiya Moriwaki, Satoru Asahi Tags: ORIGINAL PAPER Source Type: research

Species ‐related exposure of phase II metabolite gemfibrozil 1‐O‐β‐glucuronide between human and mice: a net induction of mouse P450 activity was revealed
In this study, 6 volunteers were recruited and took therapeutic dose of gemfibrozil for 3 days for examination of the gemfibrozil and gem‐glu level in human. Male mice were fed a gemfibrozil diet (0.75%) for 7 days, following which a cocktail‐based inhibitory DDI experiment was performed. Plasma samples and liver tissues from mice were collected for analysis of gemfibrozil, gem‐glu concentration and cytochrome p450 enzyme (P450) induction analysis. In human, the molar ratio of gem‐glu/gemfibrozil was 15% and 10% at the trough concentration and the concentration at 1.5 h after the 6th dose. In contrast, this molar r...
Source: Biopharmaceutics and Drug Disposition - September 1, 2017 Category: Drugs & Pharmacology Authors: Min Luo, Manyun Dai, Hante Lin, Minzhu Xie, Jiao Lin, Aiming Liu, Julin Yang Tags: ORIGINAL PAPER Source Type: research

Multiple organic cation transporters contribute to the renal transport of sulpiride
Abstract Sulpiride, a selective dopamine D2 receptor blocker, is widely used for treatment of schizophrenia, depression, and gastric/duodenal ulcers. Because of the great majority of sulpiride in positive charged at physiological pH7.4, and ~70% of dose recovered in urine in unchanged form after human intravenous administration of sulpiride, we believe transporters play an important role in renal excretion of sulpiride. The aim of the present study was to explore which transporters contribute to the renal disposition of sulpiride. Our results demonstrated sulpiride was a substrate of human carnitine/organic cation transpor...
Source: Biopharmaceutics and Drug Disposition - September 1, 2017 Category: Drugs & Pharmacology Authors: Liping Li, Yayun Weng, Wei Wang, Mengru Bai, Hongmei Lei, Hui Zhou, Huidi Jiang Tags: ORIGINAL PAPER Source Type: research

SGK1/Nedd4 –2 signaling pathway regulates the activity of human organic anion transporters 3
Abstract Human organic anion transporter 3 (hOAT3) is localized at the basolateral membrane of renal proximal tubule cells and facilitates the renal secretion of numerous clinical drugs, including anti‐HIV therapeutics, anti‐tumor drugs, antibiotics, antihypertension drugs and anti‐inflammatories. The present study explored the role of serum and glucocorticoid‐inducible kinase 1 (sgk1) in the regulation of hOAT3. It was shown 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 incre...
Source: Biopharmaceutics and Drug Disposition - August 22, 2017 Category: Drugs & Pharmacology Authors: Haoxun Wang, Guofeng You Tags: ORIGINAL PAPER Source Type: research

Clinical assessment of the lag ‐time and tmax of pellets with controlled release of glucose: in vitro/in vivo comparison using 13C–breath test
Abstract Maintaining a stable glycaemia in diabetes mellitus type 1 requires flexible insulin administration and carbohydrate intake to affected individuals. In real life, there might be some situations limiting the insulin–sugar balance control, e.g. night sleep or prolonged sporting activities. Glucose pellets with a pre‐determined time lag between the pellet administration and glucose release were developed to mimic a ‘snack eaten in advance’. In this article, a 13C–glucose breath test was introduced to translate laboratory dissolution testing to clinical confirmation of the glucose release pattern using 5% δ...
Source: Biopharmaceutics and Drug Disposition - August 9, 2017 Category: Drugs & Pharmacology Authors: David Neumann, Jan Musel ík, Dana Sabadková, Sylvie Pavloková, Jana Špirková, Aleš Franc Tags: ORIGINAL PAPER Source Type: research

Application of physiologically based pharmacokinetic modeling to predict drug disposition in pregnant populations
Abstract 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. The Simcyp pregnanc...
Source: Biopharmaceutics and Drug Disposition - July 13, 2017 Category: Drugs & Pharmacology Authors: Vamshi Krishna Jogiraju, Suvarchala Avvari, Rakesh Gollen, David R. Taft Tags: ORIGINAL PAPER Source Type: research