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Application of a method used to deconstruct a single dose pharmacokinetic profile from multiple dose data
This article is protected by copyright. All rights reserved. (Source: Biopharmaceutics and Drug Disposition)
Source: Biopharmaceutics and Drug Disposition - March 12, 2015 Category: Drugs & Pharmacology Authors: Chris Stockmann, Michael G. Spigarelli, Daniel Healy, Michele M. Gottschlich, Richard Kagan, Alfred H. Balch, Catherine Sherwin Tags: Short Communication Source Type: research

Impact of nutritional status on the pharmacokinetics of erlotinib in rats
This article is protected by copyright. All rights reserved. (Source: Biopharmaceutics and Drug Disposition)
Source: Biopharmaceutics and Drug Disposition - March 12, 2015 Category: Drugs & Pharmacology Authors: A. Pérez‐Pitarch, A. Nácher, V. Merino, A. Catalán‐Latorre, N. V. Jiménez‐Torres, M. Merino‐Sanjuán Tags: Original Paper Source Type: research

Bioactivation of loxoprofen to a pharmacologically active metabolite and its disposition kinetics in human skin
This article is protected by copyright. All rights reserved. (Source: Biopharmaceutics and Drug Disposition)
Source: Biopharmaceutics and Drug Disposition - March 12, 2015 Category: Drugs & Pharmacology Authors: Ryoko Sawamura, Hidetaka Sakurai, Naoya Wada, Yumi Nishiya, Tomoyo Honda, Miho Kazui, Atsushi Kurihara, Akira Shinagawa, Takashi Izumi Tags: Original Paper Source Type: research

Impact of sampling time deviations on the prediction of the area under the curve using regression limited sampling strategies
This article is protected by copyright. All rights reserved. (Source: Biopharmaceutics and Drug Disposition)
Source: Biopharmaceutics and Drug Disposition - March 1, 2015 Category: Drugs & Pharmacology Authors: S. Sarem, F. Nekka, I. S. Ahmed, C. Litalien, J. Li Tags: Original Paper Source Type: research

Absorption and cleavage of enalapril, a carboxyl ester prodrug, in the rat intestine: In vitro, in situ intestinal perfusion, and portal vein cannulation models
This article is protected by copyright. All rights reserved. (Source: Biopharmaceutics and Drug Disposition)
Source: Biopharmaceutics and Drug Disposition - March 1, 2015 Category: Drugs & Pharmacology Authors: Vinay K. Holenarsipur, Nilesh Gaud, Jaydeep Sinha, Sankara Sivaprasad, Priyadeep Bhutani, Murali Subramanian, Sheelendra Pratap Singh, Rambabu Arla, Sundeep Paruchury, Tarun Sharma, Punit Marathe, Sandhya Mandlekar Tags: Original Paper Source Type: research

In vitro inhibition and induction of human cytochrome P450 enzymes by SIPI5357, a potential antidepressant
In conclusion, SIPI5357 might cause drug–drug interaction via induction of CYP2B6. The in vivo drug‐drug interaction potential deserves further investigation. This article is protected by copyright. All rights reserved. (Source: Biopharmaceutics and Drug Disposition)
Source: Biopharmaceutics and Drug Disposition - March 1, 2015 Category: Drugs & Pharmacology Authors: Gaoning Fan, Yun Cao, Jin Yang Tags: Original Paper Source Type: research

Characterization of in vitro metabolites of cudratricusxanthone A in human liver microsomes
This article is protected by copyright. All rights reserved. (Source: Biopharmaceutics and Drug Disposition)
Source: Biopharmaceutics and Drug Disposition - March 1, 2015 Category: Drugs & Pharmacology Authors: Juhee Sim, Eunhwa Choi, Gil‐Saeng Jeong, Sangkyu Lee Tags: Original Paper Source Type: research

Dealing with the complex drug–drug interactions: Towards mechanistic models
ABSTRACT Unmanageable severe adverse events caused by drug‐drug interactions (DDIs), leading to market withdrawals or restrictions in the clinical usage, are increasingly avoided with the improvement in our ability to predict such DDIs quantitatively early in drug development. However, significant challenges arise in the evaluation and/or prediction of complex DDIs caused by inhibitor drugs and/or metabolites that affect not one but multiple pathways of drug clearance. This review summarizes the discussion topics at the 2013 AAPS symposium on “Dealing with the complex drug‐drug interactions: towards mechanistic model...
Source: Biopharmaceutics and Drug Disposition - February 10, 2015 Category: Drugs & Pharmacology Authors: Manthena V. Varma, K. Sandy Pang, Nina Isoherranen, Ping Zhao Tags: Invited Review Source Type: research

In vitro–in vivo extrapolations to evaluate the effect of concomitant drugs on tacrolimus (FK506) exposure
In this study, the IC50 values of concomitant drugs on the formation of M‐I, the major metabolite of tacrolimus, were determined, and the effect on oral exposure (AUCp.o.) of tacrolimus was assessed from static models. When an absorbed fraction (Fa) of 0.97, intestinal wall availability (Fg) of 0.27 and fraction metabolized by CYP3A (fm(CYP3A)) of 0.8 were used, the least bias was observed for the prediction of the AUCp.o. of tacrolimus. The relationship of the IC50 values of 11 inhibitors between tacrolimus and typical CYP3A substrates (midazolam and testosterone) was also analysed. A strong correlation was found betwee...
Source: Biopharmaceutics and Drug Disposition - February 4, 2015 Category: Drugs & Pharmacology Authors: Kazuo Oda, Katsuhiro Yamano, Yukio Otsuka Tags: Original Paper Source Type: research

The guinea‐pig expresses functional CYP2C and P‐glycoprotein: further validation of its usefulness in drug biotransformation/transport studies
Conclusion: The guinea‐pig expresses functional CYP2C and P‐gp, thus suggesting its usefulness for further validating data obtained with other animal models in drug biotransformation/transport studies. Copyright © 2014 John Wiley & Sons, Ltd. (Source: Biopharmaceutics and Drug Disposition)
Source: Biopharmaceutics and Drug Disposition - February 1, 2015 Category: Drugs & Pharmacology Authors: Ibrahim Hasibu, Dany Patoine, Sylvie Pilote, Benoit Drolet, Chantale Simard Tags: Original Paper Source Type: research

Does age affect gastric emptying time? A model‐based meta‐analysis of data from premature neonates through to adults
ConclusionsThese findings challenge the assertion that GE is different in neonates, as compared with older children and adults due to age, and they reinforce the significance of food type in modulating GE. This article is protected by copyright. All rights reserved. (Source: Biopharmaceutics and Drug Disposition)
Source: Biopharmaceutics and Drug Disposition - January 19, 2015 Category: Drugs & Pharmacology Authors: Jennifer J. Bonner, Pavan Vajjah, Khaled Abduljalil, Masoud Jamei, Amin Rostami‐Hodjegan, Geoffrey T. Tucker, Trevor N. Johnson Tags: Original Paper Source Type: research

Pharmacokinetic modeling of tranexamic acid for patients undergoing cardiac surgery with normal renal function and model simulations for patients with renal impairment
This article is protected by copyright. All rights reserved. (Source: Biopharmaceutics and Drug Disposition)
Source: Biopharmaceutics and Drug Disposition - January 1, 2015 Category: Drugs & Pharmacology Authors: Qi Yang, Angela Jerath, Robert R. Bies, Marcin Wąsowicz, K. Sandy Pang Tags: Original Paper Source Type: research

Investigation of omeprazole and phenacetin first pass metabolism in humans using a microscale bioreactor and pharmacokinetic models
This article is protected by copyright. All rights reserved. (Source: Biopharmaceutics and Drug Disposition)
Source: Biopharmaceutics and Drug Disposition - January 1, 2015 Category: Drugs & Pharmacology Authors: Thibault Bricks, Jérémy Hamon, Marie José Fleury, Rachid Jellali, Franck Merlier, Yves Edouard Herpe, Alexandre Seyer, Jean‐Marc Regimbeau, Frédéric Bois, Eric Leclerc Tags: Original Paper Source Type: research

In vitro‐in vivo extrapolations to evaluate the effect of concomitant drugs on the exposure of tacrolimus (FK506)
This article is protected by copyright. All rights reserved. (Source: Biopharmaceutics and Drug Disposition)
Source: Biopharmaceutics and Drug Disposition - January 1, 2015 Category: Drugs & Pharmacology Authors: Kazuo Oda, Katsuhiro Yamano, Yukio Otsuka Tags: Original Paper Source Type: research

Modeling of the pharmacokinetic/pharmacodynamic interaction between irbesartan and hydrochlorothiazide in normotensive subjects
ConclusionA limited potential for clinically significant interactions between IRB and HCT at the given doses were observed; therefore, no dosage adjustments were recommended for either drug when used together. This article is protected by copyright. All rights reserved. (Source: Biopharmaceutics and Drug Disposition)
Source: Biopharmaceutics and Drug Disposition - December 27, 2014 Category: Drugs & Pharmacology Authors: Mohsen A. Hedaya, Sally A. Helmy Tags: Original Paper Source Type: research