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Half-Life (0):
Recent article
Half-Life
Abstract
We established a new limited sampling strategy to assess CYP3A activity and evaluated the time course of reversible (voriconazole) and irreversible (ritonavir) CYP3A inhibition. In this randomized trial, two groups, each with eight healthy participants, received CYP3A inhibitors voriconazole or riton...
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PMID: 21937987
PDF is available here.
PDF is available here.
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Abstract
Biomacromolecules (12)9 2011
Abstract
We investigated the properties of micellar siRNA delivery vehicles prepared with poly(ethylene glycol)-block-poly(l-lysine) (PEG-b-PLL) comprising lysine amines modified to contain amidine and thiol functionality. Lysine modification was achieved using 2-iminothiolane (2-IT) [yielding PEG-b-PLL(N2IM...
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PMID: 21863796
PDF is available here.
PDF is available here.
Abstract
We demonstrate that the proteolysis of human NANOG is regulated by the ubiquitin-proteasomal pathway. The inhibition of proteasome activity by proteasome inhibitor MG132 showed increase in protein levels of endogenous NANOG in a dose-dependent manner in human ESCs (hESCS). We demonstrated that the i...
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PMID: 21299413
PDF is available here.
PDF is available here.
l Orthodontie Française (82)3 2011
Abstract
Bisphosphonates have unique pharmacological characteristics unlike those of any other drug group. Millions of adults take oral bisphosphonates for long-term treatment of osteoporosis and osteopenia; some of these people will most likely also seek orthodontic treatment. Adverse dental effects from bis...
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PMID: 21914435
PDF is available here.
PDF is available here.
Abstract
The pharmacokinetic changes observed in patients with renal impairment are of small magnitude without clinical importance. A dose adjustment or a change in the administration interval of roflumilast is not necessary in patients with renal impairment....
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PMID: 21781649
PDF is available here.
PDF is available here.
Abstract
Efavirenz plasma concentration-time data obtained from 29 HIV-1-infected, treatment-naïve patients were merged with previously reported data from 32 adult healthy subjects. The model identified sex and HIV/AIDS disease as statistically significant categorical predictors of efavirenz pharmacokinetic...
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PMID: 21740076
PDF is available here.
PDF is available here.
Abstract
Based on the dataset evaluated in this study, we demonstrated that human plasma concentration-time profiles and pharmacokinetic parameters could be predicted with the Dedrick and C(ss)-MRT approaches and that if correction factors were implemented, the predictions improved significantly. With the re...
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PMID: 21740074
PDF is available here.
PDF is available here.
Abstract
Our primary aim was to determine the pharmacokinetic parameters of a macrocyclic lactone, moxidectin, to assist in the development of effective treatment protocols. Pharmacokinetic parameters were determined in four female SHNW following a single subcutaneous injection of 0.2 mg/kg moxidectin. Blood...
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PMID: 21719829
PDF is available here.
PDF is available here.
Abstract
Abstract
I multicenter, double-blind, randomized, placebo-controlled, dose escalation, cross-over study of PHY906 as a modulator of the weekly, bolus regimen of irinotecan, 5-FU, and LV (IFL) in the first-line treatment of patients with advanced colorectal cancer (CRC) was conducted. The specific objectives...
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PMID: 21859559
PDF is available here.
PDF is available here.
Abstract
Abstract. This randomized, open-label study of patients in India with visceral leishmaniasis (VL) investigated the effect of food on sitamaquine and desethyl-sitamaquine pharmacokinetics. Patients were randomized to receive oral sitamaquine, 2 mg/kg/day, once a day for 21 days across...
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PMID: 21633025
PDF is available here.
PDF is available here.
Abstract
Abstract. The therapeutic efficacies of 3-day regimens of artesunate-amodiaquine and artemether-lumefantrine during 5 years of adoption as first-line treatments were evaluated in 811 ≤ 12-year-old malarious children. Compared with artemether-lumefantrine, amodiaquine-artesunate sig...
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PMID: 21633031
PDF is available here.
PDF is available here.
Abstract
Objective-To assess the pharmacokinetics of nalbuphine HCl after IV and IM administration to Hispaniolan Amazon parrots (Amazona ventralis). Animals-8 healthy adult Hispaniolan Amazon parrots of unknown sex. Procedures-Nalbuphine HCl (12.5 mg/kg) was administered IV and IM to all birds in a complete...
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PMID: 21627518
PDF is available here.
PDF is available here.
Abstract
Abstract
Temporal changes in indoxacarb and chlorantraniliprole were determined in four midwestern soils by simulating commercial field applications of termiticides. Indoxacarb (0.0625 and 0.125%) and chlorantraniliprole (0.05 and 0.10%) were applied to each soil type in a rotating cement mixer to ensure unif...
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PMID: 21735921
PDF is available here.
PDF is available here.
Abstract
DNA-based techniques have proved to be very useful methods to study trophic relationships between pests and their natural enemies. However, most predators are best defined as omnivores, and the identification of plant-specific DNA should also allow the identification of the plant spe...
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PMID: 21092379
PDF is available here.
PDF is available here.
Abstract
The pharmacokinetics of levetiracetam were determined prospectively in 18 neonates with seizures. Neonates were found to have lower clearance, higher volume of distribution, and a longer half-life as compared with older children and adults. Mild somnolence was the only adverse effect.
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PMID: 21592494
PDF is available here.
PDF is available here.
Abstract
We simultaneously measured absolute mRNA and protein abundance and turnover by parallel metabolic pulse labelling for more than 5,000 genes in mammalian cells. Whereas mRNA and protein levels correlated better than previously thought, corresponding half-lives showed no correlation. Using a quantitat...
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PMID: 21593866
PDF is available here.
PDF is available here.
Veterinary Record (168)22 2011
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.
PDF is available here.
Abstract
We think that after the completion of approximately 3 half-lives, a normal dose of rocuronium can produce the desired effect without the influence of residual sugammadex present in the plasma....
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PMID: 21626868
PDF is available here.
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.
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.
PDF is available here.
Veterinary Record (168)16 2011
Abstract
Abstract
To investigate pharmacokinetic parameters of peoniflorin, albiflorin and amygdaloside after administration of Guizhi Fuling capsule in beagle dogs.
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PMID: 21809575
PDF is available here.
PDF is available here.
Abstract
Blood levels of dioxins in Yusho patients have been measured for 10 years. The purposes of this study were to determine the half-lives of dioxins on the basis of the data obtained from Yusho patients and to compare the half-lives of the compounds. Linear regression analysis was performed using the bi...
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PMID: 21706886
PDF is available here.
PDF is available here.
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.
PDF is available here.
Abstract
3,4-Methylenedioxymethamphetamine (MDMA; ecstasy) is a ring-substituted amphetamine widely used for recreational purposes. MDMA is predominantly O-demethylenated in humans by cytochrome P450 (CYP) 2D6 and is also a potent mechanism-based inhibitor of the enzyme. This study assessed the inhibition and...
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PMID: 21456632
PDF is available here.
PDF is available here.
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.
PDF is available here.
Abstract
Recently a new assay method that can quantify the singlet oxygen absorption capacity (SOAC) of antioxidants was proposed. In the present work, kinetic study of the reaction of singlet oxygen ((1)O(2)) with carotenoids and vegetable extracts has been performed in ethanol/chloroform/D(2)O (50:50:1, v/v...
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PMID: 21395214
PDF is available here.
PDF is available here.
Abstract
The time course of tissue distribution of amphotericin B (AmB) has not been sufficiently characterized despite its therapeutic importance and an apparent disconnect between plasma pharmacokinetics and clinical outcomes. The goals of this work were to develop and evaluate a physiologi...
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PMID: 21431453
PDF is available here.
PDF is available here.
Abstract
Glutaredoxins (Grxs) play important roles in the redox system via reduced glutathione as a reductant. A TcmonoGrx cDNA (1039 bp, EU158772) encoding a putative monothiol Grx was cloned from Taiwanofungus camphorata (formerly named Antrodia camphorata). The deduced amino acid sequence is conserved amon...
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PMID: 21395221
PDF is available here.
PDF is available here.
Abstract
A simple validated LC-UV method for the phytochemical analysis of four bioactive quassinoids, 13alpha(21)-epoxyeurycomanone (EP), eurycomanone (EN), 13alpha,21-dihydroeurycomanone (ED) and eurycomanol (EL) in rat plasma following oral (200 mg/kg) and intravenous administration (10 mg...
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PMID: 21485270
PDF is available here.
PDF is available here.
Audio, Transactions of the IRE Professional Group on (204)6 Suppl 1 2011
Abstract
We estimated the area-under-the-curve, maximum concentration, time-to-maximum concentration, and half-life. There were no significant differences in the pharmacokinetics of oseltamivir by trimester, except for an increased half-life in the first trimester for oseltamivir phosphate and an increased m...
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PMID: 21492824
PDF is available here.
PDF is available here.
Abstract
Polychlorinated biphenyls (PCBs) are considered "persistent organic pollutants;" fat-soluble compounds that bioaccumulate in individuals and bio-magnify in the food chain. PCBs were the first industrial compounds to experience a worldwide ban on production because of their potent toxicity. These comp...
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PMID: 21438643
PDF is available here.
PDF is available here.
Abstract
We studied pharmacokinetics of morphine in SCD to explore if altered disposition could be a factor contributing to increased requirement of morphine in this population. The study subjects were in steady state of health to avoid the effect of hemodynamic changes associated with vaso-occlusion on morp...
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PMID: 21277838
PDF is available here.
PDF is available here.
Abstract
We have genetically fused RGD-P125A-endostatin to Fc of IgG4 isotype and evaluated its antiangiogenic and antitumor effects in athymic mice. Two genetic constructs were made, RGD-P125A-endostatin-Fc (RE-Fc) and P125A-endostatin-RGD-Fc (ER-Fc). Both constructs were cloned and expressed in mammalian c...
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PMID: 21225621
PDF is available here.
PDF is available here.
Abstract
Our results implicate that, when equipped with targeting ligands, liposomes are most suitable for the imaging of plaque-associated endothelial markers due to low background enhancement, whereas micelles, which accumulate extravascularly on a long timescale, are suited for imaging of less abundant ma...
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PMID: 20882509
PDF is available here.
PDF is available here.
Abstract
We have demonstrated that the half-lives of HIV-derived peptides in cytosol from primary human cells were highly variable and sequence dependent, and significantly affected the efficiency of cell recognition by CD8⁺ T cells. Furthermore, multiple clinical isolates of HLA-associated HIV epitope var...
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PMID: 21555856
PDF is available here.
PDF is available here.
Abstract
Meloxicam is a cyclooxygenase-2, preferential inhibitor non-steroidal anti-inflammatory drug (NSAID) and belongs to an enolic acid (oxicam) class used for the treatment of osteoarthritis and rheumatoid arthritis. The purpose of this single dose randomized cross-over study was to assess bioequivalence...
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PMID: 21485709
PDF is available here.
PDF is available here.
Abstract
We show here that IL-17 enhanced the stability of chemokine CXCL1 mRNA and other mRNAs through a pathway that involved the adaptor Act1, the adaptors TRAF2 or TRAF5 and the splicing factor SF2 (also known as alternative splicing factor (ASF)). TRAF2 and TRAF5 were necessary for IL-17 to signal the s...
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PMID: 21822258
PDF is available here.
PDF is available here.
Abstract
We compared the relative potency of these drugs, and also measured pH, PaCO2 and skin temperature....
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PMID: 21786523
PDF is available here.
PDF is available here.
Medicina Clínica (136 Suppl 1) 2011
Abstract
Canakinumab is a fully human monoclonal antibody targeted at IL-1β which has shown to be effective in the control the symptoms of patients affected by CAPS and other autoinflammatory diseases. Its effect is rapid and sustained. In clinical trials conducted up until now, the most common adverse effec...
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PMID: 21596185
PDF is available here.
PDF is available here.
Arzneimittel-Forschung (61)4 2011
Abstract
The present study was performed to compare the bioavailability of two perindopril erbumine (CAS 107133-36-8) 4 mg tablet formulations (test formulation and reference formulation). This study was a randomized, single-blind, two-period, two-sequence cross-over study which included 20 healthy adult male...
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PMID: 21650082
PDF is available here.
PDF is available here.
Arzneimittel-Forschung (61)6 2011
Abstract
I was compared with that of clopidogrel bisulfate form II in 12 male Sprague-Dawley rats. The rats, randomly divided into two groups, received a single oral dose of 8 mg/kg clopidogrel (CP) bisulfate form I and form II, respectively, under fasting condition. The plasma concentrations of CP and its i...
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PMID: 21827046
PDF is available here.
PDF is available here.
Arzneimittel-Forschung (61)6 2011
Abstract
A rapid and specific HPLC method has been developed and validated for the simultaneous determination of liensinine (CAS 2586-96-1), isoliensinine (CAS 6817-41-0) and neferine (CAS 2292-16-2) in rat plasma. The sample was prepared by a liquid-liquid extraction with diethyl ether and the recovery was a...
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PMID: 21827045
PDF is available here.
PDF is available here.
Arzneimittel-Forschung (61)7 2011
Abstract
A simple, sensitive and modified method was developed for determination of low dihydrocodeine (CAS 125-28-0) concentrations in human plasma by high performance-liquid chromatography (HPLC) with diode array detector. Measurement was performed on a Zorbax XDB-C18 analytical column toge...
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PMID: 21899209
PDF is available here.
PDF is available here.
Arzneimittel-Forschung (61)7 2011
Abstract
The aim of this study was to evaluate the pharmacokinetic profiles of betamethasone (BOH, CAS 378-44-9) and betamethasone 17-monopropionate (B17P), the active metabolites of betamethasone phosphate (BSP) and betamethasone dipropionate (BDP), respectively, after administration of beta...
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PMID: 21899210
PDF is available here.
PDF is available here.
Arzneimittel-Forschung (61)2 2011
Abstract
A sensitive and specific liquid chromatography-electrospray ionization mass spectrometry (LC-ESI-MS) method was developed and validated for the identification and quantification of voriconazole (VRC, CAS 137234-62-9) in human plasma. Following liquid-liquid extraction, VRC and lorata...
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PMID: 21428249
PDF is available here.
PDF is available here.
Arzneimittel-Forschung (61)2 2011
Abstract
Two bioequivalence studies were carried out in healthy volunteers in order to compare the rate and extent of absorption of two dosage forms (film-coated tablet and orodispersible tablet) of oral olanzapine (CAS 132539-06-1) 10 mg test formulations and the respective brand formulation...
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PMID: 21428240
PDF is available here.
PDF is available here.
Arzneimittel-Forschung (61)2 2011
Abstract
The present study has been designed to investigate the pharmacokinetic parameters of the novel trioxane antimalarial 97-78 (US Patent 6316493 B1, 2001) in male and female rats after single oral and intravenous administration. The pharmacokinetic profile of 97-78 was investigated in t...
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PMID: 21428247
PDF is available here.
PDF is available here.
Arzneimittel-Forschung (61)3 2011
Abstract
Eplerenone (CAS 107724-20-9) prevents the binding of aldosterone, a key hormone in the renin-angiotensin-aldosterone-system (RAAS), which is involved in the regulation of blood pressure and the pathophysiology of cardiovascular disease and is indicated, in addition to standard therapy including beta-...
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PMID: 21528639
PDF is available here.
PDF is available here.
Arzneimittel-Forschung (61)3 2011
Abstract
Existing methods to determine biapenem (CAS 120410-24-4), a carbapenem, either lacked sensitivity/reproducibility or had no internal standard as a control. Here an improved reversed-phase high-performance liquid chromatographic (RP-HPLC) method was established in human plasma and urine. After adding...
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PMID: 21528646
PDF is available here.
PDF is available here.
Abstract
The aim of our study was to investigate the pharmacokinetics and safety of human tissue urokinase type plasminogen activator (HTUPA) in healthy Chinese subjects after intravenous administration. Thirty-two subjects were given intravenous injection doses of 5-35 mg of HTUPA for safety evaluation. Twen...
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PMID: 21302035
PDF is available here.
PDF is available here.
Abstract
These results indicated that bufotalin could cross the blood-brain barrier and naturally target the lung. Bufotalin might be a promising antitumor candidate for lung cancer....
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PMID: 21302038
PDF is available here.
PDF is available here.
Abstract
Our objective was to evaluate a possible pharmacokinetic interaction between zolpidem and ciprofloxacin in healthy volunteers. The study consisted of two periods: Period 1 (reference), when each volunteer received a single dose of 5 mg zolpidem and Period 2 (test), when each volunteer received a sing...
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PMID: 21302033
PDF is available here.
PDF is available here.
Clinical Nephrology (75)1 2011
Abstract
The purpose of this study was to characterize the pharmacokinetics and tolerability of daptomycin in subjects undergoing hemodialysis (HD) or continuous ambulatory peritoneal dialysis (CAPD).
16 noninfected adults on stable dialysis regimens were enrolled. Daptomycin 6 mg/kg was administered after H...
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PMID: 21176752
PDF is available here.
PDF is available here.
Abstract
We examined the effects of ASL volume expansion on ENaC activity in primary human bronchial epithelial (HBE) cell cultures. We found that ENaC activity increases dramatically after rapid dilution of endogenous ASL. Approximately 35% of the increase in Na(+) absorption was attributable to activation...
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PMID: 20097829
PDF is available here.
PDF is available here.
Abstract
Disulfide bond engineering is an important approach to improve the metabolic half-life of cysteine-containing peptides. Eleven analogues of oxytocin were synthesized including disulfide bond replacements by thioether, selenylsulfide, diselenide, and ditelluride bridges, and their stabilities in huma...
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PMID: 21117646
PDF is available here.
PDF is available here.
Journal of Neurosurgery (113 Suppl) 2010
Abstract
The object of this study was to determine whether the radiation dose rate affects clinical outcomes in patients who undergo stereotactic Gamma Knife surgery (GKS) to manage typical trigeminal neuralgia (TN).
The authors retrospectively studied pain relief in 165 patients with medically intractable T...
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PMID: 21121798
PDF is available here.
PDF is available here.