Abstract：
:For many drugs administered per os, high variability in the concentration-time (C-T) values from first sampling to the phase of distribution may cause difficulty in pharmacokinetic analysis. Therefore, the aim of this study was to propose a method of transformation of C-T data, which would allow significantly reducing the standard deviation (SD) value of observed concentrations, without a statistically significant influence on the value of the mean for each sampling point in group. In the presented study, the lowest value of relative standard deviation of concentrations observed in the elimination phase and the value of precision of the used analytical method, were used to optimize the arithmetic, geometric means, median, and the value of SD obtained after single oral administration of itraconazole in human subjects. Non-compartmental modeling was used to estimate pharmacokinetic parameters. The analysis of SD pharmacokinetic parameters after C-T value optimization indicated more than twice the lower value of SD. After transforming the itraconazole data, lower variability of concentration data gives more selective pharmacokinetics profile in absorption and early distribution phase.
journal_name
Eur J Drug Metab Pharmacokinetjournal_title
European journal of drug metabolism and pharmacokineticsauthors
Grabowski T,Jaroszewski JJ,Piotrowski W,Sasinowska-Motyl Mdoi
10.1007/s13318-013-0145-xsubject
Has Abstractpub_date
2014-06-01 00:00:00pages
111-9issue
2eissn
0378-7966issn
2107-0180journal_volume
39pub_type
杂志文章abstract：:The inhibitory effects of 17 flavones and flavonols on ethoxy- and pentoxy-resorufin dealkylases of rat liver were investigated. Several findings concerning the relationship between structure and activity can be pointed out. The presence or lack of hydroxyl groups on the flavane nucleus has no influence on the efficie...
journal_title：European journal of drug metabolism and pharmacokinetics
pub_type： 杂志文章
doi：10.1007/BF03190104
更新日期：1989-07-01 00:00:00
abstract：BACKGROUND AND OBJECTIVES:A clinical trial was conducted to measure and analyse the pharmacokinetic parameters of a lipid formulation of risperidone, VAL401. The VAL401 formulation is designed to repurpose risperidone from an antipsychotic to an adenocarcinoma treatment, with the lipid formulation altering the cellular...
journal_title：European journal of drug metabolism and pharmacokinetics
pub_type： 杂志文章
doi：10.1007/s13318-018-00538-4
更新日期：2019-08-01 00:00:00
abstract：:We retrospectively analyzed amikacin pharmacokinetics in 19 critically ill patients who received amikacin intravenously. Fourteen subjects (577 serum amikacin concentrations, 167 urine measurements) were studied to obtain data for population modeling, while 5 patients (267 serum amikacin concentrations, 68 urine measu...
journal_title：European journal of drug metabolism and pharmacokinetics
pub_type： 杂志文章
doi：10.1007/BF03190009
更新日期：1999-01-01 00:00:00
abstract：:Blood loss during cesarean section was calculated based on post-operative decrement of hemoglobin (Hb) and hematocrit (Hct) level. The model used for pregnant women was previously validated for non-pregnant women who underwent gynecological surgery. 1,068 pregnant women who underwent cesarean section and 517 women who...
journal_title：European journal of drug metabolism and pharmacokinetics
pub_type： 杂志文章
doi：10.1007/s13318-011-0042-0
更新日期：2011-09-01 00:00:00
abstract：:The metabolic fate of anti-inflammatory agent 2-(5-ethylpyridin-2-yl)benzimidazole (KB-1043) was studied in rats after oral administration. An average of 12.2 +/- 1.5% of the dose was excreted in the urine in the course of 0-48 h; 56.7 +/- 2.6% with feces. Two metabolites were also detected in the urine and isolated b...
journal_title：European journal of drug metabolism and pharmacokinetics
pub_type： 杂志文章
doi：10.1007/BF03190109
更新日期：1989-10-01 00:00:00
abstract：:The influence of phenobarbital pretreatment on liver concentration of digitoxin and its metabolites was studied in guinea-pigs after i.p. administration of the cardiac glycoside. During the first hour an increase in liver uptake was observed in pretreated animals. The differences detected in the hepatic subcellular di...
journal_title：European journal of drug metabolism and pharmacokinetics
pub_type： 杂志文章
doi：10.1007/BF03189562
更新日期：1982-01-01 00:00:00
abstract：:The metabolism of galanthamine hydrobromide (Nivalin) was investigated in rat and rabbit liver homogenates. Experiments were carried out varying several parameters of incubation: substrate (galanthamine hydrobromide, galanthamine, galanthaminone and epigalanthamine), cofactor enrichment (NADPH, NADP/G-6-P, NAD), pH (7...
journal_title：European journal of drug metabolism and pharmacokinetics
pub_type： 杂志文章
doi：10.1007/BF03189858
更新日期：1987-01-01 00:00:00
abstract：:A rapid and sensitive procedure is described for the quantitation of levamisole in plasma using high-performance liquid chromatography (HPLC). The procedure involves sample preparation using a reverse-phase C18 cartridge prior to chromatography and quantitation using peak area ratios (UV absorbance detection, 225 nm) ...
journal_title：European journal of drug metabolism and pharmacokinetics
pub_type： 杂志文章
doi：10.1007/BF03226369
更新日期：1995-04-01 00:00:00
abstract：:Bioavailability of lansoprazole, a new gastric proton pump inhibitor, was investigated in 12 healthy subjects. Each subject received in random order, lansoprazole (30 mg) alone or associated with standard meal or with antacids (aluminium and magnesium hydroxides) or one hour later than antacids. Lansoprazole and metab...
journal_title：European journal of drug metabolism and pharmacokinetics
pub_type： 临床试验,杂志文章,随机对照试验
doi：
更新日期：1991-01-01 00:00:00
abstract：:A short review on some pharmacokinetic parameters (mean residence time, sojourn time, transit time) is given in relation to compartmental models and some examples and application are discussed. In particular the use of the sojourn time is suggested because this parameter can give useful informations when comparing the...
journal_title：European journal of drug metabolism and pharmacokinetics
pub_type： 杂志文章
doi：
更新日期：1991-01-01 00:00:00
abstract：:Carboxylesterases (CESs) play major roles in catalyzing the hydrolysis of a wide range of ester- and amide-containing compounds. CESs dominate both the biotransformation of numerous therapeutic drugs and the detoxification of environmental toxicants, and the activity alteration of CESs may be a determinant reason for ...
journal_title：European journal of drug metabolism and pharmacokinetics
pub_type： 杂志文章,评审
doi：10.1007/s13318-016-0326-5
更新日期：2016-08-01 00:00:00
abstract：:Currently, macromolecular drugs such as proteins are mainly administered by means of injections due to their low intestinal epithelial permeability and poor stability in the gastrointestinal tract. This study investigated binary combinations of chemical drug absorption enhancers to determine if synergistic drug absorp...
journal_title：European journal of drug metabolism and pharmacokinetics
pub_type： 杂志文章
doi：10.1007/s13318-015-0280-7
更新日期：2016-10-01 00:00:00
abstract：:The aim of the study was to accelerate the dissolution of the sustained release dosage forms using both elevated temperature and high rpm rates. Teokap(®) SR 200 mg pellets were tested by in vitro sustained and accelerated dissolution studies using USP XXIII rotating paddle method. Sustained dissolution studies were c...
journal_title：European journal of drug metabolism and pharmacokinetics
pub_type： 杂志文章
doi：10.1007/s13318-011-0049-6
更新日期：2011-12-01 00:00:00
abstract：:The aim of the present study was to investigate the relative bioavailability and bioequivalence of a new tablet formulation of metformin hydrochloride with reference to a standard product in healthy Chinese adult male volunteers. Two randomized, comparative, two-way crossover studies were therefore conducted. In study...
journal_title：European journal of drug metabolism and pharmacokinetics
pub_type： 杂志文章,随机对照试验
doi：10.1007/BF03190986
更新日期：2007-01-01 00:00:00
abstract：:The aim of this work was to use radiopharmaceuticals such as technetium (99mTc) and indium (DTPA-Ca111In) to visualize, with a gamma-camera, the disintegration area and time of 3 types of enteric coated hard gelatin capsules (obtained by 3 different preparation processes) and thus, to verify that they are really resis...
journal_title：European journal of drug metabolism and pharmacokinetics
pub_type： 临床试验,杂志文章
doi：10.1007/BF03188829
更新日期：1994-04-01 00:00:00
abstract：:A comparative bioavailability study was undertaken between a new formulation of rifampicin 'Famcin' and a standard formulation of rifampicin 'R-cin' in eight healthy male volunteers at two dose levels: 300 mg and 450 mg given orally under both single dose and steady state conditions. Plasma rifampicin was assayed spec...
journal_title：European journal of drug metabolism and pharmacokinetics
pub_type： 杂志文章
doi：10.1007/BF03189964
更新日期：1991-07-01 00:00:00
abstract：:There is current emphasis for extended integration of pharmacokinetics (PK) and pharmacodynamics (PD) into all phases of new drug development, including large-scale clinical trials. In this paper, we focus on study design and data analysis issues for the investigation of pharmacokinetic/pharmacodynamic and blood level...
journal_title：European journal of drug metabolism and pharmacokinetics
pub_type： 杂志文章,评审
doi：10.1007/BF03220009
更新日期：1993-01-01 00:00:00
abstract：:The biotransformation of 1-(3-butoxy-2-carbamoyloxypropyl)-5-ethyl-5-phenyl-(1H,3H,5H)-pyrimidine-2,4,6-trione (febarbamate) has been investigated in man. Human volunteers received a single oral dose of 15 mg/kg febarbamate. Twenty two metabolites found in urine were separated and purified by means of an extraction wi...
journal_title：European journal of drug metabolism and pharmacokinetics
pub_type： 杂志文章
doi：10.1007/BF03188760
更新日期：1983-07-01 00:00:00
abstract：:The development of peptide therapeutics has increased enormously in recent decades. Many of the peptide drugs and antibody fragments that lack Fc backbone have a short half-life in circulation. In general, the half-life supports the design of the dosing regimen and frequency of administration, which are key aspects in...
journal_title：European journal of drug metabolism and pharmacokinetics
pub_type： 杂志文章
doi：10.1007/s13318-020-00664-y
更新日期：2021-01-01 00:00:00
abstract：:It is known that substituted hydrazide hydrazone derivatives have several biological and pharmacological activities; there is limited literature on the metabolism of hydrazide hydrazones in rats. In our previous study, 4-fluorobenzoic acid [(5-nitro-2-furanyl)methylene]hydrazide (S) was found active against Staphyloco...
journal_title：European journal of drug metabolism and pharmacokinetics
pub_type： 杂志文章
doi：10.1007/BF03190075
更新日期：2000-04-01 00:00:00
abstract：:SC-46264 is an antagonist of the alpha 2-adrenergic receptor. Distribution and excretion of [14C]-SC-46264 were studied after single and repeated daily oral administrations to the Cynomolgus monkey at a 1.5 mg/kg dose. After a single oral administration, more than 95% of the administered dose was recovered within 48 h...
journal_title：European journal of drug metabolism and pharmacokinetics
pub_type： 杂志文章
doi：10.1007/BF03188812
更新日期：1993-07-01 00:00:00
abstract：:Hepatic distributional volumes were investigated in the in situ perfused rat liver. Perfusion experiments were conducted using Krebs bicarbonate buffer delivered via the portal vein in single-pass mode at a total flow rate of 15 mL/min. A bolus dose of normal erythrocytes (RBC, vascular marker) and Evans blue (EB, ext...
journal_title：European journal of drug metabolism and pharmacokinetics
pub_type： 杂志文章
doi：10.1007/BF03190469
更新日期：2006-10-01 00:00:00
abstract：:We studied the pharmacokinetics of moguisteine, a racemic non-narcotic peripheral antitussive drug, in 12 healthy male subjects after a single oral administration of 200 mg. The unchanged drug was absent in plasma and urine of all subjects. Moguisteine was immediately and completely hydrolyzed to its main active metab...
journal_title：European journal of drug metabolism and pharmacokinetics
pub_type： 杂志文章
doi：10.1007/BF03190242
更新日期：1995-10-01 00:00:00
abstract：:The disposition of the gonadotropin-releasing hormone (GnRH) agonist buserelin was studied in male rats under conditions of long-term administration. Rats were continuously infused with about 30 pmole [3H]-buserelin/24 h subcutaneously by osmotic minipumps for 4-7 days. After killing the rats, the 3H-activity of the t...
journal_title：European journal of drug metabolism and pharmacokinetics
pub_type： 杂志文章
doi：10.1007/BF03189737
更新日期：1996-10-01 00:00:00
abstract：:A new high performance liquid chromatographic procedure has been developed for the simultaneous quantification of piribedil (PD) and its three main basic metabolites in rat plasma and urine, without and after hydrolysis. The procedure relies on isolation of the compounds from plasma and urine constituents using the Se...
journal_title：European journal of drug metabolism and pharmacokinetics
pub_type： 杂志文章
doi：10.1007/BF03190147
更新日期：1992-07-01 00:00:00
abstract：:This paper deals with press-coated modified release tablets in which the drug dose is situated in the core or is divided between the core and the coat. The coat contains polymer (sodium alginate or hydroxypropylmethyl cellulose, HPMC) to control drug release. The main objective was to investigate how the pharmacokinet...
journal_title：European journal of drug metabolism and pharmacokinetics
pub_type： 临床试验,杂志文章,随机对照试验
doi：10.1007/BF03189338
更新日期：1998-04-01 00:00:00
abstract：:The main objective of this study was to investigate the release and pharmacokinetic profiles of ketoprofen (KP) from developed thermosensitive and mucoadhesive liquid suppositories. Thermosensitive liquid suppositories were prepared using KP, poloxamer 407 (P 407), poloxamer 188 (P 188) and various amounts of differen...
journal_title：European journal of drug metabolism and pharmacokinetics
pub_type： 杂志文章
doi：10.1007/s13318-013-0157-6
更新日期：2014-12-01 00:00:00
abstract：:Following i.v. administration of mono-HR to the beagle, plasma levels of both mono-HR and its glucuronide conjugates fell rapidly, neither being detectable 8 h after injection. Following oral administration of 14C-mono-HR, mono-HR-glucuronide was detected in plasma, confirming the absorption of mono-HR, and low levels...
journal_title：European journal of drug metabolism and pharmacokinetics
pub_type： 杂志文章
doi：10.1007/BF03189428
更新日期：1979-01-01 00:00:00
abstract：:Influence of two newly synthesized bile acids derivates, namely sodium salt of monoketocholic acid MKH-Na and methyl ester of monoketocholic acid MKH-Me on tramadol (12.5 mg/kg oral and intramuscular) analgesic effect was examined in this research. Analgesic effect was measured by antinociceptive hot plate method. Int...
journal_title：European journal of drug metabolism and pharmacokinetics
pub_type： 杂志文章
doi：10.1007/s13318-010-0011-z
更新日期：2010-09-01 00:00:00
abstract：:This study describes an approach permitting the determination of compartmental concentration and drug kinetics in the case of chronobiological variations of elimination rate. ...
journal_title：European journal of drug metabolism and pharmacokinetics
pub_type： 杂志文章
doi：10.1007/BF03190035
更新日期：1999-10-01 00:00:00
