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Biopharmaceutics&Drug Disposition,Volume 39, Issue 3, Page 135-142, March 2018. (Source: Biopharmaceutics and Drug Disposition)
Source: Biopharmaceutics and Drug Disposition - January 10, 2018 Category: Drugs & Pharmacology Source Type: research

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Biopharmaceutics&Drug Disposition,Volume 39, Issue 3, Page 125-134, March 2018. (Source: Biopharmaceutics and Drug Disposition)
Source: Biopharmaceutics and Drug Disposition - January 10, 2018 Category: Drugs & Pharmacology Source Type: research

Application of a Physiologically ‐Based Pharmacokinetic Model for the Prediction of Bumetanide Plasma and Brain Concentrations in the Neonate
Abstract Bumetanide is a loop diuretic that is proposed to possess a beneficial effect on disorders of the central nervous system, including neonatal seizures. Therefore, prediction of unbound bumetanide concentrations in brain is relevant from a pharmacological prospective. A physiologically‐based pharmacokinetic (PBPK) model was developed for the prediction of bumetanide disposition in plasma and brain in adult and pediatric populations. A compound file was built for bumetanide integrating physicochemical data and in vitro data. Bumetanide concentration profiles were simulated in both plasma and brain using Simcyp PBPK...
Source: Biopharmaceutics and Drug Disposition - January 10, 2018 Category: Drugs & Pharmacology Authors: Maria D. Donovan, Khaled Abduljalil, John F. Cryan, Geraldine B. Boylan, Brendan T. Griffin 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 - January 3, 2018 Category: Drugs & Pharmacology Tags: ISSUE INFORMATION Source Type: research

Bioactivity guided fractionation of methanolic extract of Terminalia arjuna for its CYP3A and CYP2D inhibition in rat liver microsomes
Abstract Terminalia arjuna (T. arjuna) is an Indian medicinal plant belonging to the family combretaceae and possesses numerous therapeutic activities including its immense cardio protective activity. In the present work, methanolic bark extract of T. arjuna was evaluated for the CYP3A and CYP2D inhibition potential in rat liver microsomes (RLM). Further, the methanolic bark extract was fractionated successively using increasing polarity solvents starting with petroleum ether, chloroform, ethyl acetate and n‐butanol. The fractions so obtained were also evaluated for the CYP3A and CYP2D inhibition potential. Probe substra...
Source: Biopharmaceutics and Drug Disposition - January 1, 2018 Category: Drugs & Pharmacology Authors: Alice Varghese, Prachi Saboo, Sarika Wairkar Tags: ORIGINAL PAPER Source Type: research

Inhibitory Effects of Sulfonylureas and Non ‐Steroidal Anti‐Inflammatory Drugs on In‐Vitro Metabolism of Canagliflozin in Human Liver Microsomes
The objective of the present study was to evaluate the possible inhibitory effect of sulfonylureas and non‐steroidal anti‐inflammatory drugs (NSAIDs) on canagliflozin metabolism in vitro. Three sulfonylurea derivatives were evaluated as inhibitors: chlorpropamide, glimepiride, and gliclazide. Two other NSAIDs were used as positive control inhibitors: niflumic acid and diclofenac. The rate of formation of canagliflozin metabolites was determined by HPLC analysis of vitro incubations of canagliflozin as a substrate with and without inhibitors, using human liver microsomes (HLMs). Among sulfonylureas, glimepiride showed t...
Source: Biopharmaceutics and Drug Disposition - January 1, 2018 Category: Drugs & Pharmacology Authors: Sara Algeelani, Dalal Alkhelb, David J. Greenblatt 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 - December 3, 2017 Category: Drugs & Pharmacology Tags: ISSUE INFORMATION Source Type: research

Alterations in Gene Expression in Vitamin D ‐Deficiency: Down‐Regulation of Liver Cyp7a1 and Renal Oat3 in Mice
In conclusion, vitamin D‐deficiency resulted in down‐regulation of liver Cyp7a1 and renal Oat3, conditions that are alleviated upon replenishment of cholecalciferol. (Source: Biopharmaceutics and Drug Disposition)
Source: Biopharmaceutics and Drug Disposition - December 1, 2017 Category: Drugs & Pharmacology Authors: Holly P. Quach, Keumhan Noh, Stacie Y. Hoi, Adrie Bruinsma, Geny M.M. Groothuis, Albert P. Li, Edwin C.Y. Chow, K. Sandy Pang Tags: ORIGINAL PAPER Source Type: research

Human UGT2B7 is the major isoform responsible for the glucuronidation of clopidogrel carboxylate
In this study, the glucuronidation of CCA was screened with pooled human liver microsomes (HLMs) and 7 human recombinant UGT (rUGT) isoforms. Results indicated that rUGT2B7 exhibited the highest catalytical activity for the CCA glucuronidation as measured with a mean Vmax value of 120.9 pmol/min/mg protein, 3‐ to 12‐fold higher than that of the other rUGT isoforms tested. According to relative activity factor approach, the relative contribution of rUGT2B7 to CCA glucuronidation was estimated to be 58.6%, with the minor contributions (3%) from rUGT1A6, rUGT1A9, and rUGT2B4. Moreover, the glucuronidation of CCA followed ...
Source: Biopharmaceutics and Drug Disposition - December 1, 2017 Category: Drugs & Pharmacology Authors: Jin ‐Zi Ji, Bei‐Bei Huang, Tong‐Tong Gu, Ting Tai, Huan Zhou, Yu‐Meng Jia, Qiong‐Yu Mi, Meng‐Ran Zhang, Hong‐Guang Xie Tags: ORIGINAL PAPER Source Type: research

Nonlinear disposition of lithium in rats and saturation of its tubular reabsorption by the sodium ‐phosphate cotransporter as a cause
Abstract We previously reported the contribution of sodium‐phosphate cotransporter to the tubular reabsorption of lithium in rats. In the present study, the dose dependency of the renal handling of lithium was examined in rats. When lithium chloride at 1.25 mg/kg, 2.5 mg/kg and 25 mg/kg was intravenously injected as a bolus, the areas under the plasma concentration‐time curve of lithium until 60 minutes were calculated to be 6.23 mEq·min/l, 8.77 mEq·min/l and 64.6 mEq·min/l, respectively. The renal clearance of lithium and its fractional excretion increased with increments in the dose administered. The renal clearan...
Source: Biopharmaceutics and Drug Disposition - December 1, 2017 Category: Drugs & Pharmacology Authors: Yuichi Uwai, Tatsuya Kawasaki, Tomohiro Nabekura Tags: ORIGINAL PAPER Source Type: research

Influence of body composition on disposition of the highly fat distributed compound as analysed 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 concent...
Source: Biopharmaceutics and Drug Disposition - November 9, 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

Assessment of multiple cytochrome P450 activities in metabolically inactivated human liver microsomes and roles of P450 2C isoforms in reaction phenotyping studies
This study provides important information to help elucidate the different roles of P450 isoforms in metabolite formation at different substrate concentrations. The data obtained allow the fractions metabolized to be calculated for victim drugs. (Source: Biopharmaceutics and Drug Disposition)
Source: Biopharmaceutics and Drug Disposition - November 1, 2017 Category: Drugs & Pharmacology Authors: Norie Murayama, Kanako Yajima, Mikiko Hikawa, Kanami Shimura, Yu Ishii, Masaki Takada, Yasuhiro Uno, Masahiro Utoh, Kazuhide Iwasaki, Hiroshi Yamazaki Tags: SHORT COMMUNICATION Source Type: research

Effect of Status Epilepticus on Expression of Brain UDP ‐glucuronosyltransferase 1a in Rats
This study indicated that SE altered the expression of brain Ugt1a1 and Ugt1a7, which could alter glucuronidation in the brain. (Source: Biopharmaceutics and Drug Disposition)
Source: Biopharmaceutics and Drug Disposition - November 1, 2017 Category: Drugs & Pharmacology Authors: Yuki Asai, Hatsuna Tanaka, Masayuki Nadai, Miki Katoh Tags: ORIGINAL PAPER Source Type: research

A Rule of Unity for Human Intestinal Absorption 3: Application to Pharmaceuticals
Abstract The rule of unity is based on a simple absorption parameter, Π, that can accurately predict whether or not an orally administered drug will be well absorbed or poorly absorbed. The intrinsic aqueous solubility and octanol‐water partition coefficient, along with the drug dose are used to calculate Π. We show that a single delineator value for Π exist that can distinguish whether a drug is likely to be well absorbed (FA ≥ 0.5) or poorly absorbed (FA < 0.5) at any specified dose. The model is shown to give 82.5 percent correct predictions for over 938 pharmaceuticals. The maximum well‐absorbed dose (i.e.,...
Source: Biopharmaceutics and Drug Disposition - November 1, 2017 Category: Drugs & Pharmacology Authors: Raj B. Patel, Samuel H. Yalkowsky 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 - November 1, 2017 Category: Drugs & Pharmacology Tags: ISSUE INFORMATION Source Type: research