Nano-based drug delivery system enhances the oral absorption of lipophilic drugs with extensive presystemic metabolism.

abstract：:In vitro models of the liver using isolated primary hepatocytes have been used as screens for measuring the metabolism, toxicity and efficacy of xenobiotics, for studying hepatocyte proliferation, and as bioartificial liver support systems. Yet, primary isolated hepatocytes rapidly lose liver specific functions when m...

journal_title：Current drug metabolism

authors： Sivaraman A,Leach JK,Townsend S,Iida T,Hogan BJ,Stolz DB,Fry R,Samson LD,Tannenbaum SR,Griffith LG

更新日期：2005-12-01 00:00:00

abstract：:Currently the major research highlights of bioengineering and medical technology are directed towards development of improved diagnostic techniques to screen complex diseases. Screening requirements are to identify the cause of illnesses, monitor improvement or progression of the state of diseases such as cancer, card...

journal_title：Current drug metabolism

authors： Savaliya R,Shah D,Singh R,Kumar A,Shanker R,Dhawan A,Singh S

更新日期：2015-01-01 00:00:00

abstract：:Ageing is characterized by a progressive decline in the functional reserve of multiple organs and systems, which can influence drug disposition. In addition, comorbidity and polypharmacy are highly prevalent in the elderly. As ageing is associated with some reduction in first-pass metabolism, bioavailability of a few ...

journal_title：Current drug metabolism

authors： Shi S,Klotz U

更新日期：2011-09-01 00:00:00

abstract：:A amyloid-β (Aβ) plaque formation in the brain is known to be the root cause of Alzheimer's disease (AD), which affects the behavior, memory, and cognitive ability in humans. The brain starts undergoing changes several years before the actual appearance of the symptoms. Nanotechnology could prove to be an alternative ...

journal_title：Current drug metabolism

authors： Chauhan PS,Yadav D,Koul B,Mohanta YK,Jin JO

更新日期：2020-01-01 00:00:00

abstract：:Gender differences in drug concentrations, drug response and toxicity have been attributed to various distinct yet interrelated physiological and molecular mechanisms. Drug transporters and metabolising enzymes play an important role in the xenobiotic cascade and are important regulators of drug disposition at the mol...

journal_title：Current drug metabolism

authors： Bebawy M,Chetty M

更新日期：2009-05-01 00:00:00

abstract：BACKGROUND:Nobel laureate Sir James Black's molecule, propranolol, still has broad potential in cardiovascular diseases, infantile haemangiomas and anxiety. A comprehensive and systematic review of the literature for the summarization of pharmacokinetic parameters would be effective to explore the new safe uses of prop...

journal_title：Current drug metabolism

authors： Kalam MN,Rasool MF,Rehman AU,Ahmed N

更新日期：2020-01-01 00:00:00

abstract：BACKGROUND:Overactive bladder syndrome is a broadly occurring urological disorder with a distressing impact on the quality of life. The commonly used antimuscarinic drugs show poor patient compliance because of unsatisfactory potency, tolerability and high occurrence of adverse effects such as dry mouth, blurred vision...

journal_title：Current drug metabolism

authors： Mandpe P,Prabhakar B,Shende P

更新日期：2020-01-01 00:00:00

abstract：:5-methoxy-N,N-dimethyltryptamine (5-MeO-DMT) belongs to a group of naturally-occurring psychoactive indolealkylamine drugs. It acts as a nonselective serotonin (5-HT) agonist and causes many physiological and behavioral changes. 5-MeO-DMT is O-demethylated by polymorphic cytochrome P450 2D6 (CYP2D6) to an active metab...

journal_title：Current drug metabolism

authors： Shen HW,Jiang XL,Winter JC,Yu AM

更新日期：2010-10-01 00:00:00

abstract：BACKGROUND:Bioequivalence studies are a vital part of drug development. The average bioequivalence approach is the standard method of assessment to conclude whether the generic product is bioequivalent to the innovator product. Of late, debates are on whether the average bioequivalence approach adequately addresses dru...

journal_title：Current drug metabolism

authors： Micheal F,Sayana M,Prasad R,Motilal BM

更新日期：2020-01-01 00:00:00

abstract：:Diabetes is associated with an increase risk for cardiovascular disease (CVD). Recently, macrovascular complications of diabetes have been shown to start before the development of diabetes. Indeed, several clinical studies have confirmed the increased risk of CVD in patients with impaired glucose tolerance (IGT). Sinc...

journal_title：Current drug metabolism

authors： Yamagishi S,Matsui T,Ueda S,Fukami K,Okuda S

更新日期：2009-02-01 00:00:00

abstract：:Work on human immortalized cell lines is not considered research on human subjects, but does involve biohazards. It has also been estimated that about 80% of human cell lines are the kind of cells that they are expected. Cells that are cultured directly from a subject are referred to as primary cells. Clonetics is the...

journal_title：Current drug metabolism

authors： Gomase VS,Tagore S,Changbhale SS,Kale KV

更新日期：2008-03-01 00:00:00

abstract：:Infection with the human immunodeficiency virus type 1 (HIV) results in a chronic infection that progressively cripples the host immune defenses. HIV infection is associated with increased tryptophan (trp) catabolism by the cytokine-inducible enzyme indoleamine 2,3-dioxygenase (IDO). IDO has powerful immune suppressiv...

journal_title：Current drug metabolism

authors： Boasso A,Shearer GM

更新日期：2007-04-01 00:00:00

abstract：:In recent years several arylpiperazine derivatives have reached the stage of clinical application, mainly for the treatment of depression, psychosis or anxiety. Examples are the pyrimidinylpiperazine buspirone, the chlorophenylpiperazine derivatives nefazodone and trazodone, the dichlorophenylpiperazine aripiprazole a...

journal_title：Current drug metabolism

authors： Caccia S

更新日期：2007-08-01 00:00:00

abstract：:Decarboxylation, reduction and hydrolysis can yield active metabolites from the parent drug. Major therapeutic indications and metabolic routes of these drugs are reviewed. Changes in the logP values (determined and calculated) from the parent drug to the active metabolite show certain characteristics in comparison to...

journal_title：Current drug metabolism

authors： Hartyánszky I,Kalász H,Adeghate E,Gulyás Z,Hasan MY,Tekes K,Adem A,Sótonyi P

更新日期：2012-07-01 00:00:00

abstract：:Cytochromes P450 of the liver are involved in maintenance of lipid homeostasis (cholesterol, vitamin D, oxysterol and bile acid metabolism) and in detoxification processes of endogenous compounds (i. e. bile acids) and xenochemicals (drugs). This review describes the roles of various CYPs in production of cholesterol ...

journal_title：Current drug metabolism

authors： Hafner M,Rezen T,Rozman D

更新日期：2011-02-01 00:00:00

abstract：:The possibility to treat central nervous system (CNS) disorders is strongly limited by the poor access of many therapeutic agent to the target tissues. This is mainly due to the presence of the blood-brain barrier (BBB), formed by a complex interplay of endothelial cells, astrocyte and pericytes, through which only se...

journal_title：Current drug metabolism

authors： De Rosa G,Salzano G,Caraglia M,Abbruzzese A

更新日期：2012-01-01 00:00:00

abstract：BACKGROUND:Thiopurine antimetabolites are important agents for the treatment of severe diseases, such as acute lymphoblastic leukemia and inflammatory bowel disease. Their pharmacological actions depend on biotransformation into active thioguanine-nucleotides; intracellular metabolism is mediated by enzymes of the salv...

journal_title：Current drug metabolism

authors： Pelin M,De Iudicibus S,Londero M,Spizzo R,Dei Rossi S,Martelossi S,Ventura A,Decorti G,Stocco G

更新日期：2016-01-01 00:00:00

abstract：:Arylamine N-acetyltransferases (NAT) are xenobiotic-metabolizing enzymes responsible for the acetylation of many aromatic arylamine and heterocyclic amines, thereby playing an important role in both detoxification and activation of numerous drugs and carcinogens. Two closely related isoforms (NAT1 and NAT2) have been ...

journal_title：Current drug metabolism

authors： Rodrigues-Lima F,Dairou J,Dupret JM

更新日期：2008-07-01 00:00:00

abstract：:This paper reviews the empirical methods of quantitative microdialysis that have been used to interpret the results obtained from pharmacokinetic studies. The concept of extraction efficiency or recovery and the properties of recovery in vivo (variation with flow rate, time dependency and influence of the mode of admi...

journal_title：Current drug metabolism

authors： Cano-Cebrián MJ,Zornoza T,Polache A,Granero L

更新日期：2005-04-01 00:00:00

abstract：:Pharmacokinetic studies conducted in patients with CRF demonstrate that the nonrenal clearance of multiple drugs is reduced. Although the mechanism by which this occurs is unclear, several studies have shown that CRF affects the metabolism of drugs by inhibiting key enzymatic systems in the liver, intestine and kidney...

journal_title：Current drug metabolism

authors： Pichette V,Leblond FA

更新日期：2003-04-01 00:00:00

abstract：BACKGROUND:Drug-metabolizing enzymes and transporters play key roles in drug disposition and drug interactions. The alterations of their expression will influence drug pharmacokinetics and pharmacodynamics. However, the changes in the expression of enzymes and transporters in the disease state are still unclear. OBJEC...

journal_title：Current drug metabolism

authors： Dong Y,Gong L,Lu X,Ye M,Lin Y,Xie S,Zhang J,Zhou F,Tang L,Zou W,Liu M

更新日期：2020-01-01 00:00:00

abstract：:Cytochrome P450s (P450 or CYPs) comprise a superfamily of enzymes that catalyze the oxidation of a wide variety of xenobiotic chemicals. Although most of P450 inhibitors decrease the metabolic activities mediated by the corresponding P450 forms, unexpected phenomena, which are called as activation or heterotropic coop...

journal_title：Current drug metabolism

authors： Niwa T,Murayama N,Yamazaki H

更新日期：2008-06-01 00:00:00

abstract：:When used at a high dose, many anticancer drugs produce undesirable side effects including hepatotoxicity. Transdermal delivery bypasses first-pass metabolism, allowing the use of a lower dose of drug while decreasing systemic toxicity. In this review, we summarize various advanced technologies for improving anticance...

journal_title：Current drug metabolism

authors： Fang JY,Liu PF,Huang CM

更新日期：2008-09-01 00:00:00

abstract：:Toxicogenomics is defined as an integration of genomics (transcriptomics, proteomics and metabolomics) and toxicology. It is a scientific field that studies how the genome is involved in responses to environmental stressors and toxicants. It combines studies of mRNA expression, cell and tissue-wide protein expression ...

journal_title：Current drug metabolism

authors： Gomase VS,Tagore S

更新日期：2008-03-01 00:00:00

abstract：:This review provides an overview of the in vitro methods currently used in studies of intestinal drug metabolism and active efflux with a special emphasis on the efflux- metabolism interplay. These methods include e.g. expressed enzymes or efflux transporters, fractionated intestinal cells, cell lines, primary cells, ...

journal_title：Current drug metabolism

authors： Siissalo S,Heikkinen AT

更新日期：2013-01-01 00:00:00

abstract：:Maternal antenatal therapy with glucocorticoids (GC) is routinely used to prevent lung immaturity. The potential harmful effects on other organs, including in particular the central nervous system (CNS), are still controversial. In the present review we aimed to investigate: i) the beneficial and detrimental effects o...

journal_title：Current drug metabolism

authors： Gazzolo D,Serpero LD,Frigiola A,Abella R,Dro Giamberti A,Li Volti G,Michetti F

更新日期：2013-02-01 00:00:00

abstract：OBJECTIVE:Tyrosine kinase inhibitors (TKIs) are widely used drugs which have high availability in reducing the activity of BCR-ABL1 tyrosine kinase, therefore they play an indispensable role in the treatment of Chronic myeloid leukemia (CML). Imatinib, dasatinib and nilotinib have been proved to have absolute bioavaila...

journal_title：Current drug metabolism

authors： Wang R,Zhong C,Zhang C,Hua M,Ma D

更新日期：2017-01-01 00:00:00

abstract：:Graphene possesses a wide range of potential biomedical applications because of the unique physical and chemical properties. However, the side effects of grapheme and its derivatives on a number of biological models even on human body are still not very clear. Therefore, to properly assess the potential risk of graphe...

journal_title：Current drug metabolism

authors： Xu C,Wang J,Xu Y,Shang G,Wang R,Lin Y

更新日期：2013-10-01 00:00:00

abstract：:Despite the introduction of newer drugs, the atypical antipsychotic clozapine remains the most effective drug in psychotic patients who are resistant to treatment with conventional agents. Optimal therapeutic responses to clozapine have been reported with serum concentrations between 350 microg/L and 1000 microg/L. Cl...

journal_title：Current drug metabolism

authors： Chetty M,Murray M

更新日期：2007-05-01 00:00:00

abstract：:This review introduces the Noscapine, which is being used as an antitussive drug for a long time has been recently discovered as a novel tubulin-binding, anti-angiogenic anticancer drug that causes cell cycle arrest and induces apoptosis in cancer cells both in vitro as well as in vivo. Noscapine is a multifunctional ...

journal_title：Current drug metabolism

authors： Singh H,Singh P,Kumari K,Chandra A,Dass SK,Chandra R

更新日期：2013-03-01 00:00:00