Abstract
Butorphanol tartrate (2 mg/kg) was injected intravenously in 18 healthy broiler chickens to study its pharmacokinetics. Plasma samples were analysed by a highly sensitive high-performance liquid chromatography with diode-array detection method and pharmacokinetic parameters were calculated from the m...
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PMID: 21628341
PDF is available here.
Abstract
The present study was designed to validate an analytical method based on HPLC for the quantitative measurement of the Apigenin-7-O-β-D-glucoside (AGL) in rat plasma after intravenous administration. HPLC analysis was done using a C18 column, UV detection at 335 nm, and a mobile phase of methanol:0.2...
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PMID: 21656359
PDF is available here.
Abstract
Dihydroartemisinin (DHA) is a poorly water-soluble drug that displays low bioavailability after oral administration. Attempts have been made to improve the solubility of DHA. Yet, no information is available concerning improved bioavailability. This study aimed to improve the water solubility of DHA...
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PMID: 21656361
PDF is available here.
Vikash K VK Sinha,
Karin K Vaarties,
Stefan S SS De Buck,
Luca A LA Fenu,
Marjoleen M Nijsen,
Ron A H J RA Gilissen,
Wendy W Sanderson,
Kelly K Van Uytsel,
Eva E Hoeben,
Achiel A Van Peer,
Claire E CE Mackie and
Johan W JW Smit
Abstract
We have evaluated the use of allometry for prediction of CL/F and AUC. In this paper we describe the evaluation of different allometric scaling approaches for the prediction of C(max), V(z)/F and t(½) after oral drug administration in man....
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PMID: 21456631
PDF is available here.
Hannah M HM Jones,
Iain B IB Gardner,
Wendy T WT Collard,
Phil J PJ Stanley,
Penny P Oxley,
Natilie A NA Hosea,
David D Plowchalk,
Steve S Gernhardt,
Jing J Lin,
Maurice M Dickins,
S Ravi SR Rahavendran,
Barry C BC Jones,
Kenny J KJ Watson,
Henry H Pertinez,
Vikas V Kumar and
Susan S Cole
Abstract
The importance of predicting human pharmacokinetics during compound selection has been recognized in the pharmaceutical industry. To this end there are many different approaches that are applied.
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PMID: 21456633
PDF is available here.
Richard H RH Beigi,
Kelong K Han,
Raman R Venkataramanan,
Gary D GD Hankins,
Shannon S Clark,
Mary F MF Hebert,
Thomas T Easterling,
Anne A Zajicek,
Zhaoxia Z Ren,
Donald R DR Mattison,
Steve N SN Caritis and
Abstract
We sought to delineate the pharmacokinetics (PK) of oseltamivir and its active metabolite oseltamivir carboxylate during pregnancy. Physiologic changes of pregnancy, including increased renal filtration and secretion, may increase the clearance of oseltamivir carboxylate. Sixteen pregnant women takin...
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PMID: 21492826
PDF is available here.
Abstract
The estimation of hepatic clearance, Clh, using in vitro data on metabolic stability of compound, its protein binding and blood–plasma equilibrium concentration ratio is commonly performed using well-stirred, parallel tube or dispersion models. It appears that for ionizable drugs there is a differe...
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PMID: 21355107
PDF is available here.
Abstract
Ronidazole (RDZ) is an effective treatment for feline Tritrichomonas foetus infection, but has produced neurotoxicity in some cats. An understanding of the disposition of RDZ in cats is needed in order to make precise dosing recommendations. Single-dose pharmacokinetics of intravenous (IV) RDZ and im...
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PMID: 21239199
PDF is available here.
Abstract
We addressed the question in the mouse model how the Th1/Th2 bias of primed immune responses by a DNA vaccine influences hepatitis B virus (HBV) clearance.
Plasmids expressing HBV core protein (HBcAg) or HBV e antigen and HBcAg fused to the extracellular domain of CTLA-4 (pCTLA-4-HBc...
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PMID: 21799884
PDF is available here.
Abstract
The use of in vitro metabolism in scaling to predict human clearance of new chemical entities has become a commonplace activity in the research and development of new drugs. The measurement of in vitro lability in human liver microsomes, a rich source of drug metabolizing cytochrome...
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PMID: 21320062
PDF is available here.
Abstract
The radiosynthesis of 99mTc-Prulifloxacin ((99m)Tc-PRN) was assessed in terms of stability, binding with Staphylococcus aureus (S. aureus), biodistribution in rats (RT) and scintigraphic profile in rabbits (RB). ANIMALS, MATERIAL, METHODS: 99mTc-PRN was synthesized by mixing 25 µg of stannous fluori...
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PMID: 21340097
PDF is available here.
Abstract
Daptomycin is a lipopeptide bactericidal antimicrobial indicated in the treatment of skin and soft tissue infections (SSTI), Staphylococcus aureus-related right-sided infective endocarditis (RIE) and bacteremia secondary to these infections. The recommended dosage in patients with previous renal impa...
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PMID: 21477705
PDF is available here.
Victoria A VA Brown,
Ketan R KR Patel,
Maria M Viskaduraki,
James A JA Crowell,
Marjorie M Perloff,
Tristan D TD Booth,
Grygoriy G Vasilinin,
Ananda A Sen,
Anna Maria AM Schinas,
Gianfranca G Piccirilli,
Karen K Brown,
William P WP Steward,
Andreas J AJ Gescher and
Dean E DE Brenner
Abstract
Resveratrol, a naturally occurring polyphenol, has cancer chemopreventive properties in preclinical models. It has been shown to downregulate the levels of insulin-like growth factor-1 (IGF-I) in rodents. The purpose of the study was to assess its safety, pharmacokinetics, and effects on circulating...
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PMID: 20935227
PDF is available here.
Abstract
Ranolazine is a new drug for use in patients with stable angina pectoris. Unlike other antianginal drugs ranolazine does not alter heart rate or systemic blood pressure. Inhibition of the persistent or late sodium current (I(Na,late)) by ranolazine reduces [Na(+) ](i)-dependent Ca(2+) overload and t...
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PMID: 20925013
PDF is available here.
Abstract
Mean clearance of inulin and iohexol for the reference method was 2.72 and 2.48 mL/min/kg, respectively. The mean difference between clearance of these 2 markers for the reference method was 0.24 mL/min/kg. In general, use of the limited-sample strategies yielded clearance values similar to those fo...
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PMID: 20807152
PDF is available here.
Abstract
In order to lower the costs for second generation bioethanol from lignocellulosic biomass anaerobic digestion of the effluent from ethanol fermentation was implemented using an upflow anaerobic sludge blanket (UASB) reactor system in a pilot-scale biorefinery plant. Both thermophilic (53 degrees C)...
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PMID: 20506521
PDF is available here.
Abstract
We also demonstrated that glutamine was a major carbon source to supply the TCA cycle in Vero cells and that a reduction of lactate production did not necessary improve the efficiency of the Vero cell metabolism. Thus, to adapt the formulation of the medium to the Vero cell needs, it is important to...
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PMID: 20506276
PDF is available here.
Abstract
Chronic kidney disease is one of the most common disorders in dogs and cats. The plasma urea nitrogen (P-UN) and creatinine (P-Cre) concentrations are not sufficiently sensitive for early diagnosis of renal dysfunction. Although urine and plasma clearance methods allow earlier detection of reduction...
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PMID: 20410678
PDF is available here.
Abstract
Studies conducted in humans or in animals explored the presence, nature and potential causes of 3,4-methylenedioxymethamphetamine (MDMA) toxicity. According to literature, there are four principal types of such serious toxicity: hepatic, cardiovascular, cerebral and hyperpyrexic. The molecular mecha...
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PMID: 20420577
PDF is available here.
Abstract
We can conclude that for post-mortem quantitation of amphetamine and derivatives, and MDMA in particular, peripheral blood sampling (e.g. femoral vein) remains compulsory. However, if the latter is impossible, MDMA quantification in a few alternative matrices such as vitreous humour and iliopsoas mu...
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PMID: 20420573
PDF is available here.
Abstract
We conducted a study in an in vivo animal model to evaluate the cellular morphological alterations related to the biological response between MDMA administration and inflammatory cytokines (tumor necrosis factor-alpha, IL-1beta, IL-6, 8, 10, and monocyte chemotactic protein-1). A total of 25 male ra...
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PMID: 20420568
PDF is available here.
Takashi Hirose,
Ken-Ichi Fujita,
Kazuko Nishimura,
Hiroo Ishida,
Keishi Yamashita,
Yu Sunakawa,
Keiko Mizuno,
Keisuke Miwa,
Fumio Nagashima,
Yusuke Tanigawara,
Mitsuru Adachi and
Yasutsuna Sasaki
Abstract
We developed a population pharmacokinetic (PPK) model of S-1 including the cytochrome P450 (CYP) 2A6 genotype and then used this PPK model to assess the influence of the CYP2A6 genotype on PK parameters of S-1 and the relationship between toxicity and the individual maximum concentrations (Cmax) or...
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PMID: 20596643
PDF is available here.
Abstract
We propose to estimate the total contrast agent-accessible volume fraction of tumor, including blood plasma, v(pe), and an average transfer rate constant across all tumor compartments, K(trans.av), by fitting a three-compartment tumor model and then calculating the area under the tumor impulse-respo...
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PMID: 20665785
PDF is available here.
Abstract
During Rhizopus oryzae-mediated methanolysis of triglycerides for biodiesel production, the amount of 1,2-DG and 2-MG as well as the ratio of 1,2-DG/1,3-DG and 2-MG/1-MG differed significantly in different reaction medium, which indicated that solvent might be a crucial factor that would influence t...
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PMID: 20307973
PDF is available here.
Abstract
Metabolic inhibition of Clostridium thermocellum, when grown in a high solids environment, was investigated by comparing submerged fermentation (SmF), solid-substrate cultivation (SSC) and solid-substrate cultivation with media replacement by periodic flushing (FSSC). Cellulose conversion extent and...
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PMID: 20362436
PDF is available here.
Abstract
Although activated sludge (AS)-biofilm system has many advantages, it lacks in the mathematical concepts for its design. This paper deals with deducing a mathematical model for the simulation of ammonical nitrogen in such systems starting from the basic mass balance equations. Monod kinetic equation...
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PMID: 20338756
PDF is available here.
Abstract
These studies demonstrated that Danshen aqueous extract affected the metabolism of CYP1A2 substrates through competitive inhibition and altered their clearance....
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PMID: 20663043
PDF is available here.
Abstract
The inhibition for the metabolism of docetaxel via hepatic and intestinal CYP3A subfamily, and inhibition of P-glycoprotein-mediated efflux of docetaxel in the intestine by tesmilifene were almost negligible. The extremely low value of F for docetaxel was due to the incomplete absorption from the ga...
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PMID: 20663044
PDF is available here.
Abstract
Clearance mechanisms for recombinant activated human FVII (rFVIIa; NovoSeven), a heterogeneously glycosylated protein, have yet to be fully elucidated, but may involve the liver. The effects of the gamma-carboxy glutamic acid (Gla) domain and the sialic acid content of the protein on rFVIIa clearance...
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PMID: 20508904
PDF is available here.
Abstract
We focus on the evidence-based use of prasugrel or prasugrel versus clopidogrel in clinical practice.
Georg Thieme Verlag KG Stuttgart, New York....
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PMID: 20665417
PDF is available here.
Abstract
These results suggested a modest reduction in the rate and extent of nilotinib absorption by esomeprazole. Nilotinib is a TKI that may be used concurrently with esomeprazole or other proton pump inhibitors....
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PMID: 20498287
PDF is available here.
Abstract
It is important to distinguish between the two GFR estimates and use separate reference intervals for pregnant females....
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PMID: 20334586
PDF is available here.
Abstract
We found that mGFRs had stable mean values, but substantial variability across visits. Of all mGFRs collected a mean of 62 days apart from the reference visit, 8.0% were outside 30% of the single reference mGFR (1 - P(30)). Estimation equations were less accurate because 12.1%, 17.1%, and 8.3% of eG...
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PMID: 20537455
PDF is available here.
Abstract
We investigated the use of contrast-enhanced ultrasonography (CEUS) with quantitative measurements to assess the stages of liver fibrosis in patients with chronic hepatitis B. One-hundred twenty-two patients with chronic hepatitis B were divided into three groups according to the Scheuer scoring sys...
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PMID: 20620694
PDF is available here.
Abstract
Pharmacokinetics and therapeutic efficacy of submicron/nanoscale, intracranial implants were evaluated for treating malignant glioblastoma in mice. 9.1% (w/w) paclitaxel-loaded polylactide-co-glycolide (PLGA) nanofiber discs (F3) were fabricated and characterized for morphology and size distribution...
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PMID: 20350766
PDF is available here.
Abstract
HPA axis dysregulation seems to be associated with low cognitive performance in the elderly. Slower cortisol elimination rates could predict cognitive decline affecting principally non-verbal functioning in men and verbal functioning in women. The effects are independent of environmental context, ap...
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PMID: 19814852
PDF is available here.
Abstract
Gemcitabine was rapidly cleared from plasma and undetectable after 3 h. The allele frequency of the 79A>C polymorphism was 0.40. Diplotypes were distributed as A/A n = 8, A/C n = 8 ,and C/C n = 4. No significant differences were found between the different CDA genotypes and gemcitabine or dFdU AUC,...
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PMID: 20213492
PDF is available here.
Abstract
In preterm infants and neonates, pantoprazole granules were generally well tolerated, mean exposures with pantoprazole 2.5 mg were slightly higher than that in adults who received 40 mg. While the half-life was longer, accumulation did not occur....
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PMID: 20306184
PDF is available here.
Abstract
There is a relationship between the pharmacokinetics and pharmacodynamics of omeprazole, with the latter depending in part on the duration of administration as evidenced by a higher AUC or C(max) and intragastric pH resulting from repeated dosing....
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PMID: 20414645
PDF is available here.
Abstract
87 of 90 nodules showed the typical coin-like hyperechogenicity in the arterial phase. The remaining three nodules were all in the same patient and were diagnosed as FNH after resection. Contrast started to appear within the lesions after a mean of 15.7 +/- 4.6 seconds (range 7 - 27 s) and reached p...
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PMID: 19941252
PDF is available here.
Abstract
The concept of personalized drug therapy on the basis of genetic investigations has become a major issue in psychopharmacology. Pharmacogenetic studies have focused on polymorphisms in liver cytochrome P450 isoenzymes that metabolize many antidepressant and antipsychotic medications. The most signif...
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PMID: 20562776
PDF is available here.
Abstract
This study was first conducted to characterize the intravenous and oral pharmacokinetics of magnolin, a major pharmacologically active ingredient of Magnolia fargesii, at various doses in rats. Magnolin was administered to rats by intravenous injection (0.5, 1 and 2 mg/kg doses) and oral administrat...
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PMID: 20607499
PDF is available here.
C Ronco,
R Bellomo,
PA McCullough,
Rinaldo Bellomo,
Paul M Palevsky,
Sean M Bagshaw,
Noel Gibney,
Finlay A McAlister,
Patrick M Honore,
Olivier Joannes-Boyau,
John Prowle,
Michael Haase,
Dinna N Cruz and
Claudio Ronco
Abstract
I evidence to guide the practice of RRT in critically ill patients and to better define the optimal intensity of such RRT in this setting. Clinicians practicing in the field of critical care nephrology need to be aware of these trials, their details, their findings or design or current recruitment r...
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PMID: 20427981
PDF is available here.
Abstract
Subtotal (5/6) nephrectomy was performed in APN-knockout (KO) mice and wild-type (WT) mice. The procedure in WT mice resulted in the significant increase of plasma APN and cystatin C levels. The clearance rate of APN was measured by injecting plasma from WT mice into KO mice. The clearance rate was...
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PMID: 20035033
PDF is available here.
Abstract
The overall difference between rest (201)Tl and poststress (201)Tl MPS was - 15.4%. Normal and ischemic patients showed 16.2 and 14.0% (P =0.17) washout, respectively. Visual assessment by two independent observers revealed no regional differences between rest (201)Tl and delayed or poststress (201)...
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PMID: 20429095
PDF is available here.
Abstract
In this short-term study in healthy adult male Japanese volunteers, multiple oral doses of linagliptin inhibited plasma DPP-4 activity and elevated active GLP-1 concentrations in a dose-dependent manner, with no episodes of hypoglycemia. Multiple dosing of linagliptin for 12 days was well tolerated...
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PMID: 20637971
PDF is available here.
Abstract
Lack of dose adjustment for renally cleared drugs in the presence of poor renal function is a common problem in the hospital setting. The absence of a clinical decision support system (CDSS) from direct clinician workflows such as computerized provider order entry (CPOE) hinders the uptake of CDSS....
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PMID: 20442149
PDF is available here.
Abstract
Metal tritide has been used for different areas such as research, purification, compression, and storage of tritium. Current radiation protection guidelines for tritium compounds describe the behavior of the metal tritide as the same as that of organically bound tritium. However, the biokinetic beha...
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PMID: 20386197
PDF is available here.
Abstract
The effect of surfactant administration for respiratory distress syndrome (RDS) on indomethacin (INDO) pharmacodynamics and dosing requirements for patent ductus arteriosus (PDA) closure and renal toxicity was evaluated. A 22-year prospective cohort study including 442 INDO-treated patients given 46...
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PMID: 20063159
PDF is available here.
Abstract
In intoxications with psychoactive agents, the presence of an enzyme defect in the P450 system should be considered as an additional possible cause....
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PMID: 20225176
PDF is available here.
Abstract
We found renal impairment in 32% (97/301) of medical admissions. There were 615 prescription entries for the 97 patients with renal impairment. Dose adjustment was required in 19% (117/615) of prescription entries, and only 32% (37/117) of these prescription entries were correctly dose adjusted. Of...
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PMID: 20460024
PDF is available here.
Abstract
Critically ill patients are at an increased risk to develop drug-drug interactions (DDIs). DDIs that increase the risk of QT prolongation, and ultimately torsades de pointes, can result in a medical emergency. Many clinicians are unaware of the risk of certain drug combinations that may precipitate...
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PMID: 20377471
PDF is available here.
Abstract
We evaluated factors possibly influencing serum concentrations of levetiracetam (LEV-SC). The study included 163 patients with epilepsy (91 men, 72 women; mean age 39.6 years). The duration of treatment on first analysis was 226 days; the mean daily dose amounted to 2,434 mg. In each patient between...
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PMID: 20111854
PDF is available here.
Abstract
We hypothesised that, in young trained swimmers, training status-related adaptations in the V(O)(2) and heart rate (HR) kinetics would be more evident during upper body (arm cranking) than during leg cycling exercise. Eight swim-trained (T; 11.4 +/- 0.7 years) and eight untrained (UT; 11.5 +/- 0.6 y...
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PMID: 20033206
PDF is available here.
Abstract
We performed serum pharmacokinetic studies in patients with multiple sclerosis after a single oral dose of 1200 mg lipoic acid. Patients received one of the three different racemic formulations randomly: tablet (Formulation A) and capsules (Formulations B and C). Mice pharmacokinetic studies were pe...
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PMID: 20150394
PDF is available here.