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Sample records for antipyrine

  1. The determination of antipyrine elimination in saliva by liquid chromatography.

    Science.gov (United States)

    Gartzke, J; Jäger, H

    1991-01-01

    A simple, fast and reliable liquid chromatographic method for the determination of antipyrine in saliva is described. The elimination of antipyrine is a good indicator for general evaluation of the liver function for dispositional purposes for example in occupational and environmental medicine. The described LC method was compared with a more extensive photometric procedure. The results obtained from both methods show very good correlation. Only one measurement is necessary to determine the antipyrine clearance. Furthermore the antipyrine dosage can be minimized, because of the sensitivity of the HPLC-method.

  2. Endothelial cell permeability to water and antipyrine

    International Nuclear Information System (INIS)

    Garrick, R.A.

    1986-01-01

    The endothelium provides a structural barrier between plasma constituents and the tissues. The permeability characteristics of the the endothelial cells regulate the transcellular movement of materials across this barrier while other movement is paracellular. In this study the permeability of the endothelial cells to tritiated water ( 3 HHO) and 14 C-labeled antipyrine (AP) was investigated. The cells were isolated non-enzymatically from calf pulmonary artery and were maintained in culture and used between the seventh and fifteenth passage. The cells were removed from the T-flasks with a rubber policeman, titurated with a 22g needle and centrifuged. The cells were mixed with an extracellular marker, drawn into polyethylene tubing and packed by centrifugation for use in the linear diffusion technique. All measurements were made at 37 C. The diffusion coefficients for 3 HHO through the packed cells (D), the intracellular material (D 2 ), and the extracellular material (D 1 ) were 0.682, 0.932 and 2.45 x 10 -5 cm 2 s -1 and for AP were 0.273, 0.355 and 1.13 x 10 -5 cm 2 s -1 respectively. The permeability coefficient calculated by the series-parallel pathway model for 3 HHO was higher than that for AP and for both 3 HHO and AP were lower than those calculated for isolated lung cells and erythrocytes

  3. The Influence of Alcohol on the Pharmacokinetics of Antipyrine ...

    African Journals Online (AJOL)

    The filtrate was injected into a high pressure liquid chromatography using reversed phase Bondesil C18 (0.5um) column, with benzoic acid (as internal standard) and acetonitrile: acetic acid (in 1% water) (35:65) as mobile phase. The concentrations of the antipyrine were determined from the chromatographic calibration ...

  4. Antipyrine clearance during experimental and occupational exposure to toluene

    DEFF Research Database (Denmark)

    Døssing, M; Bælum, Jesper; Lundqvist, G R

    1983-01-01

    into four groups. Eighteen printers and 21 controls were exposed to 100 ppm of toluene during 6.5 hours in an exposure chamber. The remaining 18 printers and 18 controls were exposed to 0 ppm of toluene under similar conditions. The salivary clearance of antipyrine was measured immediately after the stay...

  5. Spectrophotometric study of lanthanoid complexes with antipyrine and salicylic acid

    Energy Technology Data Exchange (ETDEWEB)

    Tishchenko, M A; Gerasimenko, G I; Poluehktov, N S [AN Ukrainskoj SSR, Odessa. Fiziko-Khimicheskij Inst.

    1981-01-01

    The extraction-spectrophotometric method has been used to study lanthanoid ion complexing (Pr, Nd, Ho and Er) with antipyrine (Ant) and salicylic acid (Sal). The component relationship in different-ligand compounds Ln:Ant:Sal=2:3:6 and solvate number equal to 5 are determined; molar extinction coefficients of binary and different-ligand compounds are calculated. Oscillator strengths of absorption bands corresponding to supersensitive transitions of neodymium, holmium, erbium and some most intensive praseodymium bands are calculated. The study of IR spectra of investigated compounds allows to conclude on formation of coordination bonds of the central atom with the antipyrine molecule through the oxygen of the carbonyl group as well as on carboxyl group hydrogen substitution for metal and formation of coordination bond with OH group in salicylic acid molecules.

  6. Spectrophotometric study of lanthanoid complexes with antipyrine and salicylic acid

    International Nuclear Information System (INIS)

    Tishchenko, M.A.; Gerasimenko, G.I.; Poluehktov, N.S.

    1981-01-01

    The extraction-spectrophotometric method has been used to study lanthanoid ion complexing (Pr, Nd, Ho and Er) with antipyrine (Ant) and salicylic acid (Sal). The component relationship in different-ligand compounds Ln:Aut:Sal=2:3:6 and solvate number equal to 5 are determined; molar extinction coefficients of binary and different-ligand compounds are calculated. Oscillator strengths of absorption bands corresponding to supersensitive transitions of neodymium, holmium, erbium and some most intensive praseodymium bands are calculated. The study of IR spectra of investigated compounds allows to conclude on formation of coordination bonds of the central atom with the antipyrine molecule through the oxygen of the carbonyl group as well as on carboxyl group hydrogen substitution for metal and formation of coordination bond with OH group in salicylic acid molecules [ru

  7. Antipyrine metabolite formation and excretion in patients with chronic renal failure

    NARCIS (Netherlands)

    Teunissen, M W; Kampf, D; Roots, I; Vermeulen, N P; Breimer, D D

    1985-01-01

    In the present study the influence of chronic renal insufficiency on antipyrine clearance, metabolite formation and excretion was investigated in 8 patients. After oral administration of antipyrine, the parent compound, its metabolites and their conjugates were assayed in plasma and urine. Besides

  8. Solar photo-Fenton mineralization of antipyrine in aqueous solution.

    Science.gov (United States)

    Durán, A; Monteagudo, J M; Sanmartín, I; Carrasco, A

    2013-11-30

    The mineralization of an aqueous solution of antipyrine (C11H12N2O), an emerging contaminant, using a solar photocatalytic oxidation process assisted with ferrioxalate was evaluated in a compound parabolic collector (CPC) pilot plant. Under the selected operating conditions ([H2O2] = 250 ppm, [Fe] = 14 ppm, pH = 2.7, and [(COOH)2·2H2O] = 80 ppm), 60% of TOC is removed just 5 min after treating an aqueous solution containing 50 ppm of antipyrine. The addition of oxalic acid up to a maximum concentration of 80 ppm significantly increases the mineralization rate during the first 15 min of the reaction. The synergism between the solar and dark H2O2/ferrioxalate process was quantified at 79%, calculated from the pseudo first-order mineralization rate constants. The operational costs due to the consumption of electrical energy, reagents and catalysts were calculated from the optimal conditions and compared with a novel sono-photocatalytic process using artificial UV-light. The results showed that the ferrioxalate-assisted solar photo-Fenton process was economically feasible, being able to achieve up to 60% mineralization with a total cost of 4.5 cent €/g TOC removed (1.1 €/m(3)). Copyright © 2013 Elsevier Ltd. All rights reserved.

  9. Albendazole metabolism in patients with neurocysticercosis: antipyrine as a multifunctional marker drug of cytochrome P450

    Directory of Open Access Journals (Sweden)

    M.P. Marques

    2002-02-01

    Full Text Available The present study investigates the isoform(s of cytochrome P450 (CYP involved in the metabolism of albendazole sulfoxide (ASOX to albendazole sulfone (ASON in patients with neurocysticercosis using antipyrine as a multifunctional marker drug. The study was conducted on 11 patients with neurocysticercosis treated with a multiple dose regimen of albendazole for 8 days (5 mg/kg every 8 h. On the 5th day of albendazole treatment, 500 mg antipyrine was administered po. Blood and urine samples were collected up to 72 h after antipyrine administration. Plasma concentrations of (+-ASOX, (--ASOX and ASON were determined by HPLC using a chiral phase column and detection by fluorescence. The apparent clearance (CL/f of ASON and of the (+ and (--ASOX enantiomers were calculated and compared to total antipyrine clearance (CL T and the clearance for the production of the three major antipyrine metabolites (CLm. A correlation (P<=0.05 was obtained only between the CL T of antipyrine and the CL/f of ASON (r = 0.67. The existence of a correlation suggests the involvement of CYP isoforms common to the metabolism of antipyrine and of ASOX to ASON. Since the CL T of antipyrine is a general measure of CYP enzymes but with a slight to moderate weight toward CYP1A2, we suggest the involvement of this enzyme in ASOX to ASON metabolism in man. The study supports the establishment of a specific marker drug of CYP1A2 in the study of the in vivo metabolism of ASOX to ASON.

  10. Liver volume, portal vein flow, and clearance of indocyanine green and antipyrine in hyperthyroidism before and after antithyroid treatment

    DEFF Research Database (Denmark)

    Andersen, Vibeke; Sonne, J; Court-Payen, M

    1999-01-01

    The aim of the study was to examine liver volume, portal vein flow, and indocyanine green (ICG) and antipyrine clearance in hyperthyroidism before and after antithyroid drug treatment.......The aim of the study was to examine liver volume, portal vein flow, and indocyanine green (ICG) and antipyrine clearance in hyperthyroidism before and after antithyroid drug treatment....

  11. Antipyrine, oxazepam, and indocyanine green clearance in patients with chronic pancreatitis and healthy subjects

    DEFF Research Database (Denmark)

    Andersen, Vibeke; Sonne, J; Larsen, S

    1999-01-01

    Hepatic drug metabolism was examined in patients with chronic pancreatitis and healthy controls by using a cocktail design with three different model compounds: antipyrine to express phase-I oxidation, oxazepam to express phase-II conjugation, and indocyanine green (ICG), a high-clearance compound....

  12. Correlation between the in vivo metabolism of hexobarbital and antipyrine in rats

    NARCIS (Netherlands)

    van der Graaff, M; Vermeulen, N P; Joeres, R P; Vlietstra, T; Breimer, D D

    1983-01-01

    Two model substrates for oxidative hepatic enzyme activity, viz. hexobarbital (HB) and antipyrine (AP), were given simultaneously to rats by the oral route of administration. Blood concentrations of HB and AP were measured simultaneously by a gas chromatographic method and the urinary excretion of

  13. Correlation between the in vivo metabolism of hexobarbital and antipyrine in rats with a portacaval shunt

    NARCIS (Netherlands)

    van der Graaff, M; Vermeulen, N P; Joeres, R P; Breimer, D D

    1984-01-01

    To investigate how hepatic malfunction affects the disposition of hexobarbital (HB), an intermediate 'high-clearance' compound, and antipyrine (AP), a low-clearance compound, as well as the correlation between the rates of elimination of these drugs, their pharmacokinetics, were studied in control

  14. Synthesis, spectral and thermal studies of some dioxouranium(VI) coordination compounds of 4[N -( 4- hydroxy -3- methoxybenzalidene ) amino] antipyrine semicarbazone and 4[N-(3,4,5- trimethoxybenzalidene) amino] antipyrine semicarbazone

    International Nuclear Information System (INIS)

    Singh, Lakshman; Singh, U.P.; Chakraborti, Indranil

    2001-01-01

    In view of high coordination compounds formed by actinide metal ions, the present work describes the 8, 9 and 10-coordinated compounds of dioxouranium(IV) with 4[N-(4-hydroxy-3-methoxy-benzalidene) amino] antipyrine semicarbazone (HMBAAPS) and 4[N-(3,4,5-trimethoxybenzalidene) amino] antipyrine semicarbazone (TMBAAPS) with the general composition UO 2 X 2 .L (X = Br - , I - , NCS - or ClO 4 ) and UO 2 X 2 .L (X = NO 3 - or CH 3 COO - , and L HMBAAPS or TMBAAPS). All these complexes were characterized through elemental, spectral and thermal studies. (author)

  15. Studies on 4-[N-(furfural) amino] antipyrine complexes of thorium (IV) and dioxouranium (VI)

    International Nuclear Information System (INIS)

    Agarwal, R.K.; Arora, Kishore; Dutt, Prashant

    1997-01-01

    Thorium (IV) and dioxouranium (VI) complexes of Schiff base 4-[N-(furfural) amino] antipyrine (FFAP) derived from furfural and 4-aminoantipyrine having general composition ThX 4 .nL (X = Cl - , Br - , NCS - or NO 3 - , n = 2; x = I - or ClO 4 - n = 3, L = FFAP) and UO 2 X 2. nL (X Br - , I - , NCS - ,NO 3 - or CH 3 COO - , n = 2; X = ClO 4 - n = 3, L = FFAP) have been synthesized and characterized by molecular weight, conductivity, IR spectral and thermoanalytical studies. (author)

  16. Fluconazole is a potent inhibitor of antipyrine metabolism in vivo in mice

    Energy Technology Data Exchange (ETDEWEB)

    La Delfa, I.; Zhu, Q.M.; Mo, Z.; Blaschke, T.F.

    1989-01-01

    Fluconazole, a bis-triazole antifungal, is distinguished from imidazole antifungals (e.g. ketoconazole) by its potency and pharmacokinetic characteristics. Imidazole-containing compounds are well documented to inhibit the hepatic cytochrome P-450-dependent enzyme system; whether this effect occurs with a bis-triazole agent is unknown. The (/sup 14/C)antipyrine breath test was employed to investigate the effects of fluconazole on this enzyme system in CD-1 male mice. Control, ketoconazole (100 mg/kg), and fluconazole (1 and 10 mg/kg) were studied in single- and multiple-dose experiments. Fluconazole had potent inhibitory effects on the total (mean = -73% +/- 2%), demethylase (mean = -90% +/- 2%), and nondemethylase (mean = -60% +/- 4%) elimination rate constants (all p less than 0.001). The fraction of the administered radioactivity excreted as /sup 14/CO/sub 2/ was decreased by 50-80% in the fluconazole groups (p less than 0.001). These effects were seen after single- and multiple-dose studies; however, return to baseline occurred more quickly in the multiple-dose group. These effects were significantly more pronounced than those observed with equipotent doses of ketoconazole. These results provide evidence that fluconazole is a potent, partially selective, and reversible inhibitor of the cytochrome P-450-dependent enzyme system in mice. Future studies will be required to assess this property and possible interactions with drugs metabolized by this enzyme system in humans.

  17. Effect of antipyrine on the gastric emptying of liquid in rats

    Directory of Open Access Journals (Sweden)

    A.C.F. Soares

    2006-11-01

    Full Text Available Antipyrine (At and dipyrone (Dp delay gastric emptying (GE in rats. The objective of the present study was to assess the effects of intravenous (iv and intracerebroventricular (icv administration of At and Dp on the GE of liquid by rats. GE was assessed in male Wistar rats (5-10 in each group 10 min after the icv or iv drug injection by measuring percent gastric retention (%GR of a saline test meal labeled with phenol red 10 min after administration by gavage. The At iv group was significantly higher (64.4 ± 2.6% compared to control (33.4 ± 1.5% but did not differ from the Dp group (54.3 ± 3.8%. After icv administration of At, %GR (34.2 ± 2% did not differ from control (32.6 ± 1.9%, but was significantly higher after Dp (54.5 ± 2.3%. Subdiaphragmatic vagotomy significantly reduced %GR in the At group (30.2 ± 0.7% compared to the sham group, but was significantly higher than in the controls (23.0 ± 0.5%. In the animals treated with At iv, baclofen significantly reduced %GR (28.3 ± 2.4% compared to vehicle-treated animals (55.2 ± 3.2%. The same occurred in the animals treated iv with vehicle and icv with baclofen. Although vagotomy and baclofen reduced %GR per se, the reduction was twice more marked in the animals treated with At. The results suggest that At administered iv, but not icv, delays GE of liquid in rats with the participation, at least in part, of the vagus nerve and that this phenomenon is blocked by the activation of GABA B receptors in the central nervous system.

  18. Inhibition effect of 4-amino-antipyrine on the corrosion of copper in 3 wt.% NaCl solution

    Energy Technology Data Exchange (ETDEWEB)

    Hong Song; Chen Wen; Luo Hongqun [Key Laboratory of Eco-environments in Three Gorges Reservoir Region (Ministry of Education), School of Chemistry and Chemical Engineering, Southwest University, Chongqing 400715 (China); Li Nianbing, E-mail: linb@swu.edu.cn [Key Laboratory of Eco-environments in Three Gorges Reservoir Region (Ministry of Education), School of Chemistry and Chemical Engineering, Southwest University, Chongqing 400715 (China)

    2012-04-15

    Highlights: Black-Right-Pointing-Pointer 4-Amino-antipyrine (AAP) has inhibition behaviour for copper corrosion in 3.0 wt.% NaCl. Black-Right-Pointing-Pointer AAP acted as a mixed-type inhibitor with anodic predominance. Black-Right-Pointing-Pointer Adsorption of AAP on the copper surface obeys the Langmuir isotherm. Black-Right-Pointing-Pointer Quantum chemical calculations were applied to explain the experimental results. - Abstract: The effect of 4-amino-antipyrine (AAP) on the corrosion of copper in 3.0 wt.% NaCl was investigated using weight loss, potentiodynamic polarisation, and electrochemical impedance spectroscopy. The results revealed that AAP acts as a mixed-type inhibitor with more pronounced effect on anodic domain and the inhibition efficiency decreases with increasing the temperature. The adsorption of AAP was found to obey the Langmuir isotherm. Surface characterisation was performed using scanning electron microscope and Fourier transform infrared spectrometer. Quantum chemical calculations show that AAP has large negative charge in nitrogen and oxygen atoms, which facilitates the adsorption of AAP on the copper surface.

  19. Determination of phenolic derivatives of antipyrine in plasma with solid-phase extraction and high-performance liquid chromatography-atmospheric-pressure chemical ionization mass spectrometry

    NARCIS (Netherlands)

    Coolen, S.A.J.; Ligor, T.; Lieshout, van H.P.M.; Huf, F.A.

    1999-01-01

    This manuscript describes a method to determine antipyrine and its phenolic derivatives in plasma by reversed-phase high-performance liquid chromatography–mass spectrometry (RP-HPLC–MS). The sample pretreatment consisted of a C18 solid-phase extraction (SPE), to remove the salts and proteins. The

  20. The influence of aging on the metabolism of simultaneously administered hexobarbital enantiomers and antipyrine before and after phenobarbital induction in male rats: A longitudinal study

    NARCIS (Netherlands)

    Groen, K.; Breimer, D.D.; Jansen, E.J.; Bezooijen, C.F.A. van

    1994-01-01

    The influence of aging on the metabolism of antipyrine (AP) and hexobarbital enantiomers (R-HB and S-HB) with and without phenobarbital (PB) induction was investigated in a longitudinal study in rats aged 6, 12, 24 and 30 months. The metabolic clearances of AP (Cl(m AP)), R-HB (Cl(m R-HB)) and S-HB

  1. Determination of the tissue-to-blood partition coefficient for 131iodo-antipyrine in human subcutaneous adipose tissue

    DEFF Research Database (Denmark)

    Jelnes, R; Astrup, A

    1985-01-01

    131Iodo-antipyrine (131I-AP) is commonly used for blood flow measurements in adipose tissue. These estimations have been based on the assumption of the tissue-to-blood partition coefficient being 1 ml g-1. No exact determination of the tissue-to-blood partition coefficient for 131I-AP in adipose...... tissue has been carried out. In the present study a partition coefficient of 1.12 +/- 0.06 (mean +/- S.D.) for 131I-AP in adipose tissue has been determined based on the partition coefficient for 131I-AP between lipid-saline (1.24 ml g-1), red blood cells-plasma (0.64 ml g-1), protein-saline (0.19 ml g-1...

  2. A fully automated effervescence assisted dispersive liquid–liquid microextraction based on a stepwise injection system. Determination of antipyrine in saliva samples

    International Nuclear Information System (INIS)

    Medinskaia, Kseniia; Vakh, Christina; Aseeva, Darina; Andruch, Vasil; Moskvin, Leonid; Bulatov, Andrey

    2016-01-01

    A first attempt to automate the effervescence assisted dispersive liquid–liquid microextraction (EA-DLLME) has been reported. The method is based on the aspiration of a sample and all required aqueous reagents into the stepwise injection analysis (SWIA) manifold, followed by simultaneous counterflow injection of the extraction solvent (dichloromethane), the mixture of the effervescence agent (0.5 mol L"−"1 Na_2CO_3) and the proton donor solution (1 mol L"−"1 CH_3COOH). Formation of carbon dioxide microbubbles generated in situ leads to the dispersion of the extraction solvent in the whole aqueous sample and extraction of the analyte into organic phase. Unlike the conventional DLLME, in the case of EA-DLLME, the addition of dispersive solvent, as well as, time consuming centrifugation step for disruption of the cloudy state is avoided. The phase separation was achieved by gentle bubbling of nitrogen stream (2 mL min"−"1 during 2 min). The performance of the suggested approach is demonstrated by determination of antipyrine in saliva samples. The procedure is based on the derivatization of antipyrine by nitrite-ion followed by EA-DLLME of 4-nitrosoantipyrine and subsequent UV–Vis detection using SWIA manifold. The absorbance of the yellow-colored extract at the wavelength of 345 nm obeys Beer's law in the range of 1.5–100 µmol L"−"1 of antipyrine in saliva. The LOD, calculated from a blank test based on 3σ, was 0.5 µmol L"−"1. - Highlights: • First attempt to automate the effervescence assisted dispersive liquid–liquid microextraction. • Automation based on Stepwise injection analysis manifold in flow batch system. • Counterflow injection of extraction solvent and the effervescence agent. • Phase separation performed by gentle bubbling of nitrogen. • Application for the determination of antipyrine in saliva samples.

  3. A fully automated effervescence assisted dispersive liquid–liquid microextraction based on a stepwise injection system. Determination of antipyrine in saliva samples

    Energy Technology Data Exchange (ETDEWEB)

    Medinskaia, Kseniia; Vakh, Christina; Aseeva, Darina [Department of Analytical Chemistry, Institute of Chemistry, Saint Petersburg State University, RU-198504 Saint Petersburg (Russian Federation); Andruch, Vasil, E-mail: vasil.andruch@upjs.sk [Department of Analytical Chemistry, University of P.J. Šafárik, SK-04154 Košice (Slovakia); Moskvin, Leonid [Department of Analytical Chemistry, Institute of Chemistry, Saint Petersburg State University, RU-198504 Saint Petersburg (Russian Federation); Bulatov, Andrey, E-mail: bulatov_andrey@mail.ru [Department of Analytical Chemistry, Institute of Chemistry, Saint Petersburg State University, RU-198504 Saint Petersburg (Russian Federation)

    2016-01-01

    A first attempt to automate the effervescence assisted dispersive liquid–liquid microextraction (EA-DLLME) has been reported. The method is based on the aspiration of a sample and all required aqueous reagents into the stepwise injection analysis (SWIA) manifold, followed by simultaneous counterflow injection of the extraction solvent (dichloromethane), the mixture of the effervescence agent (0.5 mol L{sup −1} Na{sub 2}CO{sub 3}) and the proton donor solution (1 mol L{sup −1} CH{sub 3}COOH). Formation of carbon dioxide microbubbles generated in situ leads to the dispersion of the extraction solvent in the whole aqueous sample and extraction of the analyte into organic phase. Unlike the conventional DLLME, in the case of EA-DLLME, the addition of dispersive solvent, as well as, time consuming centrifugation step for disruption of the cloudy state is avoided. The phase separation was achieved by gentle bubbling of nitrogen stream (2 mL min{sup −1} during 2 min). The performance of the suggested approach is demonstrated by determination of antipyrine in saliva samples. The procedure is based on the derivatization of antipyrine by nitrite-ion followed by EA-DLLME of 4-nitrosoantipyrine and subsequent UV–Vis detection using SWIA manifold. The absorbance of the yellow-colored extract at the wavelength of 345 nm obeys Beer's law in the range of 1.5–100 µmol L{sup −1} of antipyrine in saliva. The LOD, calculated from a blank test based on 3σ, was 0.5 µmol L{sup −1}. - Highlights: • First attempt to automate the effervescence assisted dispersive liquid–liquid microextraction. • Automation based on Stepwise injection analysis manifold in flow batch system. • Counterflow injection of extraction solvent and the effervescence agent. • Phase separation performed by gentle bubbling of nitrogen. • Application for the determination of antipyrine in saliva samples.

  4. Permeability of ferret trachea in vitro to 99m Tc-DTPA and [14C]antipyrine

    International Nuclear Information System (INIS)

    Hanafi, Z.; Webber, S.E.; Widdicombe, J.G.

    1994-01-01

    Platelet-activating factor (PAF) and vasoactive drugs were tested on permeability of ferret trachea in vitro by measuring fluxes of 99m T c -diethylenetriamine pentaacetic acid ( 99m T c -DTPA; hydrophilic) and [ 14 C]antipyrine ([ 14 C]AP; lipophilic) across the tracheal wall. Tracheae were bathed on both sides with Krebs-Henseleit buffer, with luminal buffer containing either 99m T c -DTPA or [ 14 C]AP. Luminal and abluminal radioactivities, potential difference, and tracheal smooth muscle tone were measured. Baseline 99m T c -DTPA and [ 14 C]AP permeability coefficients were - 4.7 ± 0.6 (SE) x 10 -7 and -2.2 ± 0.1 x 10 -5 cm/s, respectively. PAF (10 μM) increased permeability to 99m T c -DTPA to -35.3 ± 7.6 x 10 -7 cm/s (P 14 C]AP did not change, suggesting that paracellular but not transcellular transport was affected. Abluminal and luminal applications of methacholine (MCh, 20 μM), phenylephrine (PE, 100 μM), and albuterol (Alb, 100 μM) caused no change in permeability to 99m T c -DTPA before or after exposure to luminal PAF, but abluminal histamine (Hist, 10 μM) significantly increased permeability. Abluminal Hist decreased permeability to [ 14 C]AP before and after exposure to PAF. MCh, PE, and Hist increased smooth muscle tone; Alb and PAF had no effect. Thus, only PAF and Hist altered permeability to 99m T c -DTPA, and MCh, PE, and Hist changed smooth muscle tone. Tracheal permeability changes were greater for the hydrophilic than for the lipophilic agent. 37 refs., 11 figs., 1 tab

  5. A new recycling technique for human placental cotyledon perfusion: application to studies of the fetomaternal transfer of glucose, inulin, and antipyrine

    International Nuclear Information System (INIS)

    Brandes, J.M.; Tavoloni, N.; Potter, B.J.; Sarkozi, L.; Shepard, M.D.; Berk, P.D.

    1983-01-01

    A previously described technique has been modified to permit the continuously recirculating perfusion of the separate maternal and fetal circulations of an isolated cotyledon of human placenta. Viability of the perfused cotyledons was established by measurements of oxygen consumption (average, 0.18 ml/gm/hr), glucose utilization (average, 1.0 mg/gm/hr), and lactate production (less than 0.01 mumol/gm/hr), and integrity of the placental barrier by the failure of India ink, 125I-albumin, or 35S-sulfobromophthalein to cross from fetal to maternal circulation. Clearance of 3H-inulin from the fetal circuit, 0.0059 +/- 0.0005 (SE) ml/min/gm, corresponded to 2.5% of its clearance by the adult human kidney. Clearance of 14C-antipyrine was 0.013 +/- 0.003 ml/min/gm. After introduction into the fetal circuit, the observed appearance of both inulin and antipyrine in the maternal circuit closely paralleled curves predicted by a simple mathematical model. The use of a continuously recirculating perfusion system is technically feasible, and has advantages over the single-pass technique for studying transplacental transfer of metabolites with a low efficiency of extraction

  6. Characterization of 60 Co y-radiation induced radical products of antipyrine by means of high performance liquid chromatography, mass spectrometry, capillary zone electrophoresis, micellar electrokinetic capillary chromatography and nuclear magnetic resonance spectrometry

    NARCIS (Netherlands)

    Coolen, S.A.J.; Everaerts, F.M.; Huf, F.A.

    1997-01-01

    Monitoring the amount of oxidative damage, caused by free radicals, is a major problem in free radical and aging research. Antipyrine is proposed as an exogenous marker for the biomolecular monitoring of oxidative stress. In this paper the characterization of the 60Co γ-radiation products of

  7. Characterization of 60Co gamma-radiation induced radical products of antipyrine by means of high-performance liquid chromatography, mass spectrometry, capillary zone electrophoresis, micellar electrokinetic capillary chromatography and nuclear magnetic resonance spectrometry

    NARCIS (Netherlands)

    Coolen, S.A.J.; Everaerts, F.M.; Huf, F.A.

    1997-01-01

    Monitoring the amount of oxidative damage, caused by free radicals, is a major problem in free radical and aging research. Antipyrine is proposed as an exogenous marker for the biomolecular monitoring of oxidative stress. In this paper the characterization of the 60Co ¿-radiation products of

  8. The 14C-monomethylamino-antipyrine breath test as in vivo parameter for characterizing the induction of the drug catabolizing enzyme system in the guinea pig

    International Nuclear Information System (INIS)

    Gramatzki, S.

    1981-01-01

    The aim of these investigations was to help clarify the following questions: 1) Does MAAP, following 14 C labelling of the exocyclic aminomethyl group, offer a suitable substrate for a breath test in guinea pigs. 2) Which procedures for evaluating the 14 C exhalation curves of the breath test are especially valid. 3) Can an induction of the drug catabolizing enzyme system following pre-treatment with various inducing substances be detected by the 14 C-MAAP breath test. 4) Do inducer-specific differences arise in response to the 14 C-MAAP breath test by which the inducers can be characterized. 5) Is monomethylamino-antipyrine similar to amidopyrine in that it is a suitable independent in vivo parameter for the drug metasbolizing enzyme system in the liver of guinea pigs. (orig./MG) [de

  9. Estimation of rare earth elements in uranium matrix after solvent extraction of uranium as uranium-antipyrine-anion complex using chloroform as solvent

    International Nuclear Information System (INIS)

    Bose, Roopa; Murthy, D.S.R.; Malhotra, R.K.

    1999-01-01

    The neutron economy in a nuclear reactor dictates the occurrence of neutron absorbers at very low levels. Hence the determination of lanthanides especially Sm, Eu, Gd and Dy is one of the most difficult and complicated analytical tasks particularly in high uranium matrix. Solvent extraction is a potent and versatile technique for the separation of lanthanides. The systems generally used for lanthanide extraction are TBP-nitrate, TBP-chloride, TBP-thiocyanate TOPO, DEHPA-nitrate etc. However, these methods of extraction of lanthanides fail to give a clear cut separation for their determination from uranium matrix. Hence analytical procedures have been standardised for extraction of uranium matrix into the organic phase leaving lanthanides unextracted in the aqueous phase. In this direction Cyanex-923 a mixture of 4 trialkyl phosphine oxides, TBP- TOPO and trioctylamine in xylene have been used for extraction of uranium and consequent determination of lanthanides by ICP-AES in the aqueous phase. In this paper the authors have investigated uranium -antipyrine -anion, a different combination other than the well known phosphine oxides and tertiary amines for extraction of uranium

  10. Evidence for the involvement of peripheral β-adrenoceptors in delayed liquid gastric emptying induced by dipyrone, 4-aminoantipyrine, and antipyrine in rats

    Energy Technology Data Exchange (ETDEWEB)

    Vinagre, A.M. [Núcleo de Medicina e Cirurgia Experimental, Faculdade de Ciências Médicas, Universidade Estadual de Campinas, Campinas, SP (Brazil); Collares, E.F. [Departamento de Pediatria, Faculdade de Ciências Médicas, Universidade Estadual de Campinas, Campinas, SP (Brazil); Núcleo de Medicina e Cirurgia Experimental, Faculdade de Ciências Médicas, Universidade Estadual de Campinas, Campinas, SP (Brazil)

    2013-09-27

    Dipyrone (Dp), 4-aminoantipyrine (AA), and antipyrine (At) delay liquid gastric emptying (GE) in rats. We evaluated adrenergic participation in this phenomenon in a study in male Wistar rats (250-300 g) pretreated subcutaneously with guanethidine (GUA), 100 mg·kg{sup −1}·day{sup −1}, or vehicle (V) for 2 days before experimental treatments. Other groups of animals were pretreated intravenously (iv) 15 min before treatment with V, prazosin (PRA; 1 mg/kg), yohimbine (YOH; 3 mg/kg), or propranolol (PRO; 4 mg/kg), or with intracerebroventricular (icv) administration of 25 µg PRO or V. The groups were treated iv with saline or with 240 µmol/kg Dp, AA, or At. GE was determined 10 min later by measuring the percentage of gastric retention (%GR) of saline labeled with phenol red 10 min after gavage. %GR (mean±SE, n=8) indicated that GUA abolished the effect of Dp (GUA vs V=31.7±1.6 vs 47.1±2.3%) and of At (33.2±2.3 vs 54.7±3.6%) on GE and significantly reduced the effect of AA (48.1±3.2 vs 67.2±3.1%). PRA and YOH did not modify the effect of the drugs. %GR (mean±SE, n=8) indicated that iv, but not icv, PRO abolished the effect of Dp (PRO vs V=29.1±1.7 vs 46.9±2.7%) and At (30.5±1.7 vs 49±3.2%) and significantly reduced the effect of AA (48.4±2.6 vs 59.5±3.1%). These data suggest activation of peripheral β-adrenoceptors in the delayed GE induced by phenylpyrazolone derivatives.

  11. Iodine 123-antipyrine. A diffusible tracer for brain exploration

    International Nuclear Information System (INIS)

    Dantonel-Mathieu, Evelyne.

    1978-09-01

    Iodine 123-labelled iodoantipyrine is a liposoluble diffusible tracer which crosses the blood-brain barrier intact. Its build-up in brain tissue is proportional to the regional blood flow. Its behavior was studied in undervascularised brain lesions and in cases where research with traditional radioactive tracers (99mTc and its different vectors for example) has proved limited. Because of the great diffusibility of iodoantipyrine a brain parenchyma image is obtained within minutes after its injection, and this by the use of a non-invasive technique and under good gamma-camera exploration conditions. 81 brain explorations including 11 standards have been carried out on subjects averaging 51,2 years old; these examinations took place in three nuclear medicine centres. The 123 I iodoantipyrine used in each nuclear medicine centre is supplied by the CEA. Iodoantipyrine is labelled with a good yield (>98%) checked by chromatography by means of a CEA kit. After intraveinous injection of 4 to 6 mCi iodine-123 iodoantipyrine, a dynamic study (from 0 to 60 seconds) of the tracer passage in the brain tissue may be followed by static images taken in the next minutes according to a standard procedure. The table of results shows the major interest of this tracer for the exploration of vascular accidents with ischemic lesions, especially in the early phase of the accident. The lesion appears as a hypoactive zone and this lack of perfusion lasts for some minutes after the injection [fr

  12. Extraction of thorium(IV) as perchlorate and chloroacetate complexes with 1-phenyl-2,3-dimethyl-5-pyrazolone (antipyrine)

    International Nuclear Information System (INIS)

    Roopa Bose; Murty, D.S.R.; Chakrapani, G.

    2005-01-01

    Thorium was extracted quantitatively with the neutral ligand 1-phenyl-2,3-dimethyl-5-pyrazolone (Apy) in the presence of perchlorate (ClO 4 - )and di/trichloroacetates (DCA/TCA) at pH 2.5 into an organic solvent. Optimization of experimental parameters like pH, equilibration time, solvents, reactant concentrations, best suited conditions for back extraction, interference due to the presence of different anions and cations and effect of metal ion concentration were studied. The composition of the complexes has been established using log-log plots and are represented as [Th(Apy) 2 (ClO 4 ) 4 ], [Th(Apy) 2 (TCA) 4 ], [Th(Apy)(H 2 O)(DCA) 4 ]. The respective conditional stability constants of the effectively extracted complexes have also been calculated as 9.4 ± 0.03 and 10.4 ± 0.04, respectively . The method has been extended for the separation of thorium from a number of cations in binary and multicomponent mixtures. The method is simple, rapid, selective and has a good reproducibility (±0.5%). (author)

  13. Determination of phenolic derivatives of antipyrine in plasma with HPLC-Tandem MS using ESI and Turbo ion spray as interfaces

    NARCIS (Netherlands)

    Coolen, S.A.J.; Lieshout, van H.P.M.; Reijenga, J.C.; Huf, F.A.

    1999-01-01

    Free radical damage plays an important role in biology and medicine, especially in the aging process of human beings. In the field of free radical products, determining the degree of this free radical damage is still a major problem. Several determination methods exist, most of which involve the use

  14. Dissociation of brain edema induced by cold injury in rat model. MR imaging and perfusion studies with 14C-iodo-antipyrine

    International Nuclear Information System (INIS)

    Itabashi, Yoko; Prado, G.L.M.; Abo, Mitsuru; Miura, Hiroyuki; Abe, Yoshinao

    2001-01-01

    The purpose of this study is to confirm whether T2-weighted imaging and perfusion imaging, i.e. autoradiogram of 14 C-iodoantipyrine, on the course of brain edema correspond to each other or not. Cold injured rat brains were used as a model and were sequentially examined by both methods and compared with each other and with histological specimens. Special focus relies on the time changes in the lesions. High SI of T2-weighted images were observed and the percentages in the high SI area to the total brain area in the same slice were 4.7±0.31, 5.6±0.46 and 3.4±0.42 for 6, 24 and 48 hours, respectively. By contrast, low perfusion areas were indicated in the perfusion study and their percentages were 4.6±0.55, 5.6±0.86 and 2.4±0.35 for 6, 24 and 48 hours, respectively. At 48 hours after cold injury, low perfusion areas were smaller than high SI areas. Moreover, high accumulation areas consisting of macrophages were observed surrounding necrosis. It is concluded that there is dissociation between perfusion and T2-weighted MR imaging, where the collection of macrophages surrounding edema lesions and necrosis had the same appearance on MRI and different accumulations on perfusion studies. (author)

  15. Investigations into the post-natal development of demethylating enzyme systems by determination of carbon dioxide 14 in the air exhaled by mice after applications of carbon 14 dimethyl amino-antipyrine

    International Nuclear Information System (INIS)

    Schmidt, H.

    1982-01-01

    Albino mice were subcutaneously injected with carbon 14 dimethyl aminopyrines, the methyl group of which can be metabolised in the organism into carbon dioxide 14. The following results were obtained: In the carbon dioxide 14 exhalation of neonate, young and adult animals after administration of carbon 14 aminopyrine, distinct differences were noted. The maximum of elimination via the lungs occurs after 20-30 minutes in grown-up mice, in neonates or young animals distinctly later (60-90 min). The carbon dioxide 14 exhalation was also measured after additional subcutaneous application of methrotrexate. In mice aged 8 and 10 days a distinct decrease in carbon dioxide 14 exhalation was found. By contrast, a rise in carbon dioxide 14 exhaled was found in mice aged 2 days. The orientating experiments with folic acid and carbon 14 dimethyl aminopyrine show that leucovorin leads to a distinct increase in carbon dioxide 14 exhalation during the first 30 minutes. As a cause of the different degrees of stimulation respectively inhibition of demethylation, different biochemical ways of formaldehyde formation are pointed out. One of these probably includes the folate-dependent reaction. (orig./MG) [de

  16. Transplacental diffusion and blood flow of gravid bovine uterus

    International Nuclear Information System (INIS)

    Reynolds, L.P.; Ferrell, C.L.; Ford, S.P.

    1985-01-01

    Electromagnetic blood flow transducers and uterine arterial, uterine venous, umbilical venous, fetal femoral arterial, and fetal femoral venous catheters were implanted in 11 cows on day 161 +/- 4 of gestation. Antipyrine (0.66 M) plus NaCl (0.16 M) dissolved in deuterium oxide (D 2 O), or H 2 O, was infused at a constant rate into the fetal femoral vein catheter. Concentrations of antipyrine and D 2 O in uterine arterial and venous blood and antipyrine in fetal arterial and umbilical venous blood, as well as middle uterine arterial blood flow (electromagnetic transducer), were determined. Antipyrine and D 2 O gave similar estimates (steady-state diffusion method) of gravid uterine blood flow. In addition, the slope of the regression of D 2 O on antipyrine estimates was not different from one. Electromagnetic transducers gave estimates of uterine blood flow that were 32-42% of those obtained with steady-state diffusion but were correlated with estimates obtained by use of both antipyrine and D 2 O. The transplacental clearance rate of antipyrine was similar (per kg placenta) to that observed in ewes. It was suggested that the maternal and fetal microvasculatures of the bovine placenta could have a concurrent arrangement with vascular shunts or maldistribution of flows, as has been suggested for the ewe

  17. 2002 Chemical Science Archive

    Indian Academy of Sciences (India)

    Suresh

    Synergism in the extraction of uranium in presence of antipyrine. R K Malhotra, M ... Exchange interactions in some low-dimensional metal dithiolene complexes ... Asymmetric reductionof carbonyl compounds with chiral alkoxy aluminium and ...

  18. Synthesis and kinetics of [18F]4'-fluoroantipyrine in normal mice

    International Nuclear Information System (INIS)

    Robbins, P.J.; Fortman, D.L.; Scholz, K.L.; Fusaro, G.A.; Sodd, V.J.

    1978-01-01

    Antipyrine labeled with radioiodine has proven useful for studying the symmetry of human brain perfusion by gamma-camera techniques. The feasibility of preparing F-18-labeled antipyrine for eventual use with a positron camera was investigated. The preparation of [ 18 F] 4'-fluoroantipyrine and its distribution in normal mice were used to evaluate this potential. 4'-Fluoroantipyrine was prepared in 7 to 20% chemical yield by the pyrolysis of the 4'-diazonium fluoroborate salt of antipyrine. This Schiemann salt was prepared by a five-step synthesis from 1-(4'-nitrophenyl)-3-methyl-5-chloro-pyrazole. Fluorine-18 labeling of the diazonium fluoroborate salt by exchange with aqueous F-18 and pyrolysis of the dried labeled salt produced [ 18 F] 4'-fluoroantipyrine with specific activities of 0.83 to 2.7 μCi/mg. The incorporated F-18 activity ranged from 0.53 to 1.9%. The labeling procedure took about 3 hr. The labeled antipyrine was administered by tail vein to fasting female Swiss-Cox mice. Distribution of F-18 at 12, 30, 60, and 120 sec, and 10 min, after injection showed that radioactivity persisted in the brain up to 120 sec at a level greater than that of the skin and the bone. (Skin and bone samples were chosen as representative of activities in the scalp and skull surrounding the brain.) Thus, perfusion imaging of the CNS should be possible when greater quantities of high-specific-activity F-18-labeled antipyrine becomes available

  19. Kinetics of silica nanoparticles in the human placenta

    DEFF Research Database (Denmark)

    Poulsen, Marie Sønnegaard; Mose, Tina; Maroun, Lisa Leth

    2015-01-01

    choriocarcinoma cell line and the ex vivo perfused human placenta. Nanotoxicity in BeWo cells was examined by the MTT assay which demonstrated decreased cell viability at concentrations >100 µg/mL. In the placental perfusion experiments, antipyrine crossed the placenta rapidly, with a foetal:maternal ratio of 0...

  20. Wound healing in below-knee amputations in relation to skin perfusion pressure

    DEFF Research Database (Denmark)

    Holstein, P; Sager, P; Lassen, N A

    1979-01-01

    In 60 below-knee amputations the healing of the stumps was correlated with the local skin perfusion pressure (SPP) measured preoperatively as the external pressure required to stop isotope washout using 131I- or 125I--antipyrine mixed with histamine. Of the eight cases with an SPP below 20 mm...

  1. Modeling placental transport: correlation of in vitro BeWo cell permeability and ex vivo human placental perfusion

    DEFF Research Database (Denmark)

    Poulsen, Marie Sønnegaard; Rytting, Erik; Mose, Tina

    2009-01-01

    across the BeWo cells was observed in the rank order of caffeine>antipyrine>benzoic acid>glyphosate in terms of both the apparent permeability coefficient and the initial slope, defined as the linear rate of substance transferred to the fetal compartment as percent per time, a parameter used to compare...

  2. Effect of isolated hepatic ischemia on organic anion clearance and oxidative metabolism.

    Science.gov (United States)

    Minard, G; Bynoe, R; Wood, G C; Fabian, T C; Croce, M; Kudsk, K A

    1992-04-01

    Hepatic failure is frequently seen following severe hemorrhagic shock, sepsis, and trauma. Clearance of various drugs has been used to evaluate hepatocellular dysfunction, including indocyanine green (ICG), an organic anionic dye that is transported similarly to bilirubin, and antipyrine (AP), a marker of oxidative phosphorylation. Previous investigators have noted a decrease in ICG excretion following systemic hemorrhage. The effect of isolated hepatic ischemia on the clearances of ICG and AP was studied in 16 pigs after 90 minutes of vascular occlusion to the liver. Antipyrine clearance decreased almost 50% from baseline values at 24 and 72 hours after the ischemia procedure, indicating a significant depression in the cytochrome P-450 system. On the other hand, ICG clearance did not change significantly. In conclusion, ICG clearance is not depressed after isolated hepatic ischemia in pigs. Changes in organic anion clearance after systemic hemorrhage may be because of release of toxic products from ischemic peripheral tissue.

  3. Age dependence of rat liver function measurements

    DEFF Research Database (Denmark)

    Fischer-Nielsen, A; Poulsen, H E; Hansen, B A

    1989-01-01

    Changes in the galactose elimination capacity, the capacity of urea-N synthesis and antipyrine clearance were studied in male Wistar rats at the age of 8, 20 and 44 weeks. Further, liver tissue concentrations of microsomal cytochrome P-450, microsomal protein and glutathione were measured. All...... liver function measurements increased from the age of 8 to 44 weeks when expressed in absolute values. In relation to body weight, these function measurements were unchanged or reduced from week 8 to week 20. At week 44, galactose elimination capacity and capacity of urea-N synthesis related to body...... weight were increased by 10% and 36%, respectively, and antipyrine plasma clearance was reduced to 50%. Liver tissue concentrations of microsomal cytochrome P-450 and microsomal protein increased with age when expressed in absolute values, but were unchanged per g liver, i.e., closely related to liver...

  4. Meta-analysis of data from human ex vivo placental perfusion studies on genotoxic and immunotoxic agents within the integrated European project NewGeneris

    DEFF Research Database (Denmark)

    Mose, T; Mathiesen, L; Karttunen, V

    2012-01-01

    highly ranked no matter which parameter was used. Antipyrine normalization resulted in the following ranking order of compounds according to AUC(120NORM) values: NDMA = EtOH = BPA = IQ =AA = GA = PCB180 = PhIP = AFB1 > DON = BP = PCB52 = TCDD. As the variance in all parameters within a study decreased...

  5. Ischaemic wound complications in above-knee amputations in relation to the skin perfusion pressure

    DEFF Research Database (Denmark)

    Holstein, P

    1980-01-01

    Healing of the stumps in 59 above-knee amputations was correlated with the local skin perfusion pressure (SPP) measured preoperatively as the external pressure required to stop isotope washout using 131I-(-) or 125I-(-) antipyrine mixed with histamine. Out of the 11 cases with an SPP below 30 mm...... ischaemic wound complications in above-knee amputations as has previously been shown to be the case in below-knee amputations....

  6. Application of solar photocatalytic ozonation for the degradation of emerging contaminants in water in a pilot plant

    OpenAIRE

    Beltrán, F.J.; Contreras, S.; Rey, A.; Álvarez, P.M.; Quiñones, D.H.

    2015-01-01

    10.1016/j.cej.2014.08.067 Aqueous mixtures of six commonly detected emerging contaminants (acetaminophen, antipyrine, bisphenol A, caffeine, metoprolol and testosterone), selected as model compounds, were treated by different solar-driven photochemical processes including photolysis, photocatalytic oxidation with Fe(III) or TiO2, photo-Fenton and single, photolytic and photocatalytic ozonations. Experiments were carried out in a compound parabolic collector photoreactor. It was found that...

  7. 1,5-Dimethyl-4-(1-methyl-3-oxo-3-phenylprop-1-enylamino-2-phenyl-1H-pyrazol-3(2H-one

    Directory of Open Access Journals (Sweden)

    Hualing Zhu

    2011-07-01

    Full Text Available In the title compound, C21H21N3O2, an intramolecular N—H...O interaction generates an S(6 ring, which stablizes the enamine–keto tautomer. The S(6 ring makes dihedral angles of 33.07 (7, 56.50 (8 and 38.59 (8°, respectively, with the benzoylacetone benzene ring and the antipyrine pyrazole and benzene rings.

  8. New prospects in radioiodine production technologies and radioiodination

    Energy Technology Data Exchange (ETDEWEB)

    Miller, J [Magyar Tudomanyos Akademia, Budapest. Izotopintezete

    1984-01-01

    A new economical dry distillation procedure was developed to produce /sup 131/I or /sup 125/I from irradiated TeO/sub 2/ melt and xenon gas, respectively. The method can be applied to the thermodesorptive radioiodination of different types of water soluble or insoluble organic compounds: oleic acid, prostaglandin, insulin, ACTH, antipyrine. The labelling procedure is based on the thermolysis of the stable Pt(I) surface compound.

  9. The effect of diminazene aceturate on cholinesterase activity in dogs with canine babesiosis

    Directory of Open Access Journals (Sweden)

    R.J. Milner

    1997-07-01

    Full Text Available A clinical trial was designed to evaluate the effects of diminazene aceturate and its stabiliser antipyrine on serum pseudocholinesterase (PChE and red blood cell acetylcholinesterase (RBC AChE in dogs with babesiosis. The trial was conducted on naturally occurring, uncomplicated cases of babesiosis (n = 20 that were randomly allocated to groups receiving a standard therapeutic dose of diminazene aceturate with antipyrine stabiliser (n = 10 or antipyrine alone (n = 10. Blood was drawn immediately before and every 15 minutes for 1 hour after treatment. Plasma PChE showed a 4 % decrease between 0 and 60 min within the treatment group (p < 0.05. No statistically significant differences were found between the treatment and control groups at any of the time intervals for PChE. There was an increase in RBC AChE activity at 15 min in the treatment group (p < 0.05. No significant differences were found between the treatment and control groups at any time interval for RBC AChE. In view of the difference in PChE, samples from additional, new cases (n = 10 of canine babesiosis were collected to identify the affect of the drug over 12 hours. No significant depression was identified over this time interval. The results suggests that the underlying mechanism in producing side-effects, when they do occur, is unlikely to be through cholinesterase depression.

  10. Transplacental pharmacokinetics of diclofenac in perfused human placenta.

    Science.gov (United States)

    Shintaku, Kyohei; Hori, Satoko; Tsujimoto, Masayuki; Nagata, Hideaki; Satoh, Shoji; Tsukimori, Kiyomi; Nakano, Hitoo; Fujii, Tomoyuki; Taketani, Yuji; Ohtani, Hisakazu; Sawada, Yasufumi

    2009-05-01

    The aims of this study were to evaluate the transplacental transfer properties of diclofenac and to determine the effect of L-lactic acid on the transplacental transfer of diclofenac. The maternal and fetal vessels of human placenta were perfused in a single-pass mode with a solution containing diclofenac and antipyrine. The transplacental pharmacokinetic model was fitted to the time profiles of the drug concentrations in the effluent and placenta to obtain transplacental pharmacokinetic parameters. In addition, chloride ion in the perfusate was partially replaced with L-lactic acid to see the change in the transplacental transfer properties of diclofenac. The TPT(ss) value (ratio of the rate of amount transferred across the placenta to that infused in the steady state) of diclofenac was 2.22%, which was approximately one-third that of antipyrine and was significantly reduced in the presence of L-lactic acid. The transplacental pharmacokinetic model could adequately explain the transplacental transfer of diclofenac with influx clearances from maternal and fetal perfusates to placental tissue of 0.276 and 0.0345 ml/min/g cotyledon and efflux rate constants from placental tissue to maternal and fetal perfusates of 0.406 and 0.0337 min(-1), respectively. By taking into account protein binding, the placental tissue/plasma concentration ratio in humans for diclofenac was estimated to be 0.108 ml/g of cotyledon and was smaller than that of antipyrine. In conclusion, human placental perfusion and transplacental pharmacokinetic modeling allowed us to determine the transplacental transfer properties of diclofenac quantitatively. Diclofenac may share transplacental transfer system(s) with L-lactic acid.

  11. CriticalSorb™ promotes permeation of flux markers across isolated rat intestinal mucosae and Caco-2 monolayers.

    Science.gov (United States)

    Brayden, D J; Bzik, V A; Lewis, A L; Illum, L

    2012-09-01

    CriticalSorb™ is a novel absorption enhancer based on Solutol(®) HS15, one that has been found to enhance the nasal transport. It is in clinical trials for nasal delivery of human growth hormone. The hypothesis was that permeating enhancement effects of the Solutol(®)HS15 component would translate to the intestine. Rat colonic mucosae were mounted in Ussing chambers and Papp values of [(14)C]-mannitol, [(14)C]-antipyrine, FITC-dextran 4000 (FD-4), and TEER values were calculated in the presence of CriticalSorb™. Tissues were fixed for H & E staining. Caco-2 monolayers were grown on Transwells™ for similar experiments. CriticalSorb™(0.01% v/v) significantly increased the Papp of [(14)C]-mannitol, FD-4 [(14)C]-antipyrine across ileal and colonic mucosae, accompanied by a decrease in TEER. In Caco-2 monolayers, it also increased the Papp of [(14)C]-mannitol FD-4 and [(14)C]-antipyrine over 120 min. In both monolayers and tissues, it acted as a moderately effective P-glycoprotein inhibitor. There was no evidence of cytotoxicity in Caco-2 at concentrations of 0.01% for up to 24 h and histology of tissues showed intact epithelia at 120 min. Solutol(®) HS15 is the key component in CriticalSorb™ that enables non-cytotoxic in vitro intestinal permeation and its mechanism of action is a combination of increased paracellular and transcellular flux.

  12. Structural studies of 4-aminoantipyrine derivatives

    Science.gov (United States)

    Cunha, Silvio; Oliveira, Shana M.; Rodrigues, Manoel T.; Bastos, Rodrigo M.; Ferrari, Jailton; de Oliveira, Cecília M. A.; Kato, Lucília; Napolitano, Hamilton B.; Vencato, Ivo; Lariucci, Carlito

    2005-10-01

    Reaction of 4-aminoantipyrine with acetylacetone, ethyl acetoacetate, benzoyl isothiocyanate, phenyl isothiocyanate, maleic anhydride and methoxymethylene Meldrum's acid afforded a series of new antipyrine derivatives. The antibacterial activity of the synthesized compounds against Micrococcus luteus ATCC 9341, Staphilococcus aureus ATCC 29737, and Escherichia coli ATCC 8739 was evaluated and the minimal inhibitory concentration determined. Modest activity was found only to the maleamic acid obtained from the reaction of 4-aminoantipyrine and maleic anhydride. 1H NMR investigation of this maleamic acid showed that it is slowly converted to the corresponding toxic maleimide. The structures of three derivatives were determined by X-ray diffraction analysis.

  13. Effect of organic bases on extraction of gadolinium carboxylates

    International Nuclear Information System (INIS)

    Sukhan, V.V.; Frankovskij, V.A.

    1982-01-01

    The effect of pyridine, 2-aminopyridine, benzylamine, antipyrine and o-phenanthroline on the extraction of capronates and bromocapronates of gadolinium with chloroform is studied. Out of the studied organic bases benzylamine produces the highest synergetic effect. In the absence of organic bases gadolinium carboxylates, solvated by three molecules of carbonic acids, are extracted into organic phase. A possihility of extractional separation of gadolinium from comparable amounts of iron with the mixture of 1 M solutions of caproic or bromocaproic acids with 1 M benzylamine from 0.1 M solution of tartaric acids is shown [ru

  14. Wound healing in above-knee amputations in relation to skin perfusion pressure

    DEFF Research Database (Denmark)

    Holstein, P; Dovey, H; Lassen, N A

    1979-01-01

    In 59 above-knee amputations healing of the stumps was correlated with the local skin perfusion pressure (SPP) measured preoperatively as the external pressure required to stop isotope washout using 1318-- or 125I--antipyrine mixed with histamine. Out of the 11 cases with an SPP below 30 mm...... on the stumps was on average only slightly and insignificantly higher than the preoperative values, explaining why the preoperative values related so closely to the postoperative clinical course. We conclude that the SPP can be used to predict ischaemic wound complications in above-knee amputations as has...... previously been shown to be the case in below-knee amputations....

  15. Application of the Microwave Discharge Modification of the Wilzbach Technique for the Tritium Labelling of some Organics of Biological Interest

    International Nuclear Information System (INIS)

    Gosztonyi, T.

    1969-01-01

    The modification of the Wilzbach technique using microwave discharge has been routinely used in our laboratory for rapid tritium labellings. The applicability of the method and the effects of some of the reaction parameters were studied and published previously. The main advantage of the method is its simplicity and rapidity and the low extent of decomposition of the compound to be labelled during the reaction. Specific activities obtained, however, are not high enough for some investigations. In this paper the labelling of dihydrostreptomycine, tetracycline and antipyrine will be described

  16. Determination of organic bases in non-aqueous solvents by catalytic thermometric titration.

    Science.gov (United States)

    Vajgand, V J; Kiss, T A; Gaál, F F; Zsigrai, I J

    1968-07-01

    Catalytic thermometric titrations have been developed for bases (brucine, diethylaniline, potassium acetate and triethylamine) in acetic acid by continuous and discontinuous addition of the standard solution and automatic temperature recording. The determination of weak bases, e.g., antipyrine, unsuccessful in acetic acid by catalytic thermometric titration, has been achieved by using nitromethane or acetic anhydride as solvent. Catalytic thermometric titrations were also performed by coulometric generation of hydrogen ions for the determination of micro amounts of weak bases in a mixture of acetic anhyride and acetic acid.

  17. Application of the Microwave Discharge Modification of the Wilzbach Technique for the Tritium Labelling of some Organics of Biological Interest

    Energy Technology Data Exchange (ETDEWEB)

    Gosztonyi, T

    1969-01-15

    The modification of the Wilzbach technique using microwave discharge has been routinely used in our laboratory for rapid tritium labellings. The applicability of the method and the effects of some of the reaction parameters were studied and published previously. The main advantage of the method is its simplicity and rapidity and the low extent of decomposition of the compound to be labelled during the reaction. Specific activities obtained, however, are not high enough for some investigations. In this paper the labelling of dihydrostreptomycine, tetracycline and antipyrine will be described.

  18. The effects of estrus cycle on drug metabolism in the rat.

    Science.gov (United States)

    Brandstetter, Y; Kaplanski, J; Leibson, V; Ben-Zvi, Z

    1986-01-01

    The effect of the female rat estral cycle on microsomal drug metabolism in-vivo and in-vitro has been studied. Two microsomal enzymes, aminopyrine-N-demethylase and aniline hydroxylase showed a greater specific activity (p less than 0.01) in the diestrus phase of the estral cycle while the oxidative enzyme aryl hydrocarbon hydroxylase and the conjugative enzyme, glucuronyl transferase, were not affected. In vivo studies which included theophylline and antipyrine metabolism, and hexobarbital sleeping times showed no difference between the different phases of the estral cycle. Conflicting evidence about the effect of steroid sex hormones on hepatic drug metabolism is discussed.

  19. Assessment of drug disposition in the perfused rat brain by statistical moment analysis

    International Nuclear Information System (INIS)

    Sakane, T.; Nakatsu, M.; Yamamoto, A.; Hashida, M.; Sezaki, H.; Yamashita, S.; Nadai, T.

    1991-01-01

    Drug disposition in the brain was investigated by statistical moment analysis using an improved in situ brain perfusion technique. The right cerebral hemisphere of the rat was perfused in situ. The drug and inulin were injected into the right internal carotid artery as a rapid bolus and the venous outflow curve at the posterior facial vein was obtained. The infusion rate was adjusted to minimize the flow of perfusion fluid into the left hemisphere. The obtained disposition parameters were characteristics and considered to reflect the physicochemical properties of each drug. Antipyrine showed a small degree of initial uptake. Therefore, its apparent distribution volume (Vi) and apparent intrinsic clearance (CLint,i) were small. Diazepam showed large degrees of both influx and efflux and, thus, a large Vi. Water showed parameters intermediate between those of antipyrine and those of diazepam. Imipramine, desipramine, and propranolol showed a large CLint,i compared with those of the other drugs. The extraction ratio of propranolol significantly decreased with increasing concentrations of unlabeled propranolol in the perfusion fluid. These findings may be explained partly by the tissue binding of these drugs. In conclusion, the present method is useful for studying drug disposition in the brain

  20. Development and validation of an HPLC method for simultaneous determination of trimethoprim and sulfamethoxazole in human plasma.

    Science.gov (United States)

    Sayar, Esin; Sahin, Selma; Cevheroglu, Semsettin; Hincal, A Atilla

    2010-09-01

    The combination of trimethoprim (TMP) and sulfamethoxazole (SMX) is used in the treatment of many common infections such as urinary, respiratory and gastrointestinal tract infections. The aim of this study was to determine TMP and SMX simultaneously in human plasma samples by high performance liquid chromatography (HPLC) using antipyrine as the internal standard. Separation of the compounds was achieved on a reverse-phase C8 column packed with 5 microm dimethyl octadecylsilyl bonded amorphous silica (4.6 mm x 250 mm) column using a mobile phase consisted of potassium hydrogen phosphate, acetonitrile, methanol and water adjusted to pH 6.2. The mobile phase was delivered at a flow rate of 1 mL min- and the effluent was monitored using Max plot technique at 25 derees C. Retention times were 5 min for TMP, 7 min for antipyrine and 9 min for SMX. Quantitation limits were 10 ng mL(-1) for TMP and 50 ng mL(-1) for SMX. Our findings indicated that the developed HPLC method was precise, accurate, specific and sensitive for simultaneous determination of TMP and SMX. Proposed HPLC method was successfully applied for the analysis of TMP and SMX in human plasma after oral administration of a co-trimoxazole tablet to human volunteers.

  1. Influence of nutrition on liver oxidative metabolism.

    Science.gov (United States)

    Jorquera, F; Culebras, J M; González-Gallego, J

    1996-06-01

    The liver plays a major role in the disposition of the majority of drugs. This is due to the presence of several drug-metabolizing enzyme systems, including a group of membrane-bound mixed-function oxidative enzymes, mainly the cytochrome P450 system. Hepatic oxidative capacity can be assessed by changes in antipyrine metabolism. Different drugs and other factors may induce or inhibit the cytochrome P450-dependent system. This effect is important in terms of the efficacy or toxicity of drugs that are substrates for the system. Microsomal oxidation in animals fed with protein-deficient diets is depressed. The mixed-function oxidase activity recovers after a hyperproteic diet or the addition of lipids. Similar findings have been reported in patients with protein-calorie malnutrition, although results in the elderly are conflicting. Different studies have revealed that microsomal oxidation is impaired by total parenteral nutrition and that this effect is absent when changing the caloric source from carbohydrates to a conventional amino acid solution or after lipid addition, especially when administered as medium-chain/long-chain triglyceride mixtures. Peripheral parenteral nutrition appears to increase antipyrine clearance.

  2. Increase in the penetration of tracer compounds into the rat brain during 2-methyl-4-chlorophenoxyacetic acid (MCPA) intoxication

    International Nuclear Information System (INIS)

    Elo, H.A.; Ylitalo, P.; Kyoettilae, J.; Hervonen, H.

    1982-01-01

    The penetration of different intravenous tracer molecules such as 14 C-labelled 2-methyl-4-chlorophenoxyacetic acid ( 14 C-MCPA), 14 C-p-aminobenzoic acid ( 14 C-PABA), 14 C-sucrose, 14 C-antipyrine and iodinated ( 125 I) human albumin ( 125 I-HA) into the brain and cerebrospinal fluid (CSF) was studied in MCPA-intoxicated and control rats. Toxic subcutaneous doses of sodium salt of MCPA (200-500 mg/kg) increased highly the brain/plasma and CSF/plasma ratios of 14 C-MCPA and 14 C-PABA, as compared to the muscle/plasma ratio. Probenecid (200 mg/kg) did not affect the cerebral MCPA concentration in the intoxicated animals. The tissue/plasma ratios of 14 C-sucrose, 14 C-antipyrine and 125 I-HA were also increased in the brain and CSF of intoxicated animals, but the increases were less pronounced than those of 14 C-MCPA or 14 C-PABA. The results indicate that MCPA intoxication caused a selective damage of the blood-brain barrier in the brain areas studied. (author)

  3. Lung damage and pulmonary uptake of serotonin in intact dogs

    International Nuclear Information System (INIS)

    Dawson, C.A.; Christensen, C.W.; Rickaby, D.A.; Linehan, J.H.; Johnston, M.R.

    1985-01-01

    The authors examined the influence of glass bead embolization and oleic acid, dextran, and imipramine infusion on the pulmonary uptake of trace doses of [ 3 H]serotonin and the extravascular volume accessible to [ 14 C]antipyrine in anesthetized dogs. Embolization and imipramine decreased serotonin uptake by 53 and 61%, respectively, but no change was observed with oleic acid or dextran infusion. The extravascular volume accessible to the antipyrine was reduced by 77% after embolization and increased by 177 and approximately 44% after oleic acid and dextran infusion, respectively. The results suggest that when the perfused endothelial surface is sufficiently reduced, as with embolization, the uptake of trace doses of serotonin will be depressed. In addition, decreases in serotonin uptake in response to imipramine in this study and in response to certain endothelial toxins in other studies suggest that serotonin uptake can reveal certain kinds of changes in endothelial function. However, the lack of a response to oleic acid-induced damage in the present study suggests that serotonin uptake is not sensitive to all forms of endothelial damage

  4. Transfer of PAMAM dendrimers across human placenta: prospects of its use as drug carrier during pregnancy.

    Science.gov (United States)

    Menjoge, Anupa R; Rinderknecht, Amber L; Navath, Raghavendra S; Faridnia, Masoud; Kim, Chong J; Romero, Roberto; Miller, Richard K; Kannan, Rangaramanujam M

    2011-03-30

    Dendrimers offer significant potential as nanocarriers for targeted delivery of drugs and imaging agents. The objectives of this study were to evaluate the transplacental transport, kinetics and biodistribution of PAMAM dendrimers ex-vivo across the human placenta in comparison with antipyrine, a freely diffusible molecule, using dually perfused re-circulating term human placental lobules. The purpose of this study is to determine if dendrimers as drug carriers can be used to design drug delivery systems directed at selectively treating either the mother or the fetus. The transplacental transfers of fluorescently (Alexa 488) tagged PAMAM dendrimer (16 kDa) and antipyrine (188 Da) from maternal to fetal circulation were measured using HPLC/dual UV and fluorescent detector (sensitivity of 10 ng/mL for dendrimer and 100 ng/mL for antipyrine respectively). C(max) for the dendrimer-Alexa (DA) in maternal perfusate (T(max)=15 min) was 18 times higher than in the fetal perfusate and never equilibrated with the maternal perfusate during 5.5 h of perfusion (n=4). DA exhibited a measurable but low transplacental transport of 2.26±0.12 μg/mL during 5.5h, where the mean transplacental transfer was 0.84±0.11% of the total maternal concentration and the feto-maternal ratio as percent was 0.073%±0.02. The biochemical and physiological analysis of the placentae perfused with DA demonstrated normal function throughout the perfusion. The immunofluorescence histochemistry confirmed that the biodistribution of DA in perfused placenta was sparsely dispersed, and when noted was principally seen in the inter-villous spaces and outer rim of the villous branches. In a few cases, DA was found internalized and localized in nuclei and cytoplasm of syncytiotrophoblast and inside the villous core; however, DA was mostly absent from the villous capillaries. In conclusion, the PAMAM dendrimers exhibited a low rate of transfer from maternal to the fetal side across the perfused human placenta

  5. Acid-base properties of complexes of 3 group elements with tetra-4-tert. butylphthalocyanine. [Elements: Al, Ga, In, Sc

    Energy Technology Data Exchange (ETDEWEB)

    Borovkov, N Yu; Akopov, A S

    1987-01-01

    Step-like constants of pKn complex ionization of In and Sc with tetra-4-tert.butylphthalocyanine in CH/sub 3/COOH-H/sub 2/SO/sub 4/ and B-CH/sub 3/COOH-H/sub 2/SO/sub 4/, where B is antipyrine or urea are determined. They have the next values at n equalling 1, 2, 3, 4: +2.70+-0.30; -0.26+-0.09; -3.70+-0.20; -6.10+-0.20 for HOIn phthalocyanine substituted correspondingly. Effect of the methane atom nature on the basicity of phthalocyanine nitrogen mesonic atoms is considered. Using the conductometry method, it is established that phthalocyanines in concentrated H/sub 2/SO/sub 4/ form both completely protonated shapes and contact ion pairs.

  6. In Situ Formation of Steroidal Supramolecular Gels Designed for Drug Release

    Directory of Open Access Journals (Sweden)

    Hana Bunzen

    2013-03-01

    Full Text Available In this work, a steroidal gelator containing an imine bond was synthesized, and its gelation behavior as well as a sensitivity of its gels towards acids was investigated. It was shown that the gels were acid-responsive, and that the gelator molecules could be prepared either by a conventional synthesis or directly in situ during the gel forming process. The gels prepared by both methods were studied and it was found that they had very similar macro- and microscopic properties. Furthermore, the possibility to use the gels as carriers for aromatic drugs such as 5-chloro-8-hydroxyquinoline, pyrazinecarboxamide, and antipyrine was investigated and the prepared two-component gels were studied with regard to their potential applications in drug delivery, particularly in a pH-controlled drug release.

  7. Synthesis, physicochemical studies and biological evaluation of unimetallic and heterobimetallic complexes of hexadentate dihydrazone ligands

    Directory of Open Access Journals (Sweden)

    Fathy A. El Saied

    2017-03-01

    Full Text Available A new coordination unimetallic and heterobimetallic complexes of hexadentate N2O4 donor dihydrazone ligands were prepared by the condensation of 4-formyl antipyrine with adipic dihydrazide and succinic dihydrazide. The ligands (1 and (11 and their complexes thoroughly characterized using various analytical, physical and spectroscopic techniques, which indicate a distorted octahedral geometry around the metal ions. The ESR spectra of solid copper(II complexes (2–4 and (12–14 showed axial symmetry with g||>g⊥ > ge, indicating distorted octahedral structure and the presence of the unpaired electron in a d(x2−y2 orbital with significant covalent bond character. The antimicrobial activity results of the metal compounds (2–5, (7, (10, (12–15 and (17 show that, all these complexes exhibit inhibitory moderate to mild effects towards Bacillus subtilis, Escherichia coli and Aspergillus niger.

  8. Copper(II Complexes with Ligands Derived from 4-Amino-2,3-dimethyl-1-phenyl-3-pyrazolin-5-one: Synthesis and Biological Activity

    Directory of Open Access Journals (Sweden)

    Raluca Cernat

    2006-11-01

    Full Text Available The synthesis of Cu(II complexes derived from Schiff base ligands obtainedby the condensation of 2-hydroxybenzaldehyde or terephtalic aldehyde with 4-amino-antipyrine (4-amino-2,3-dimethyl-1-phenyl-3-pyrazolin-5-one is presented. The newlyprepared compounds were characterized by 1H-NMR, UV-VIS, IR and ESRspectroscopy. The determination of the antimicrobial activity of the ligands and of thecomplexes was carried out on samples of Escherichia coli, Klebsiella pneumoniae,Acinetobacter boumanii, Pseudomonas aeruginosa, Staphylococcus aureus and Candidasp. The qualitative and quantitative antimicrobial activity test results proved that all theprepared complexes are very active, especially against samples of Ps. aeruginosa, A.Boumanii, E. coli and S. aureus.

  9. Determination of phenol in locally grown fruits and vegetable by spectrophotometric method

    International Nuclear Information System (INIS)

    Iqbal, M.; Khan, F.A.; Farooqui, Z.H.; Ifrahim, A.F.K.

    2005-01-01

    Spectrophotometric method for the determination of phenol in the sample of locally grown fruits apple, pear, sweet orange and vegetable radish of Quetta, Hyderabad and Nawabshah are described juices from these fruits and vegetable were squeezed, filtered and decolorized with charcoal. The antipyrine dye formed by reaction between phenol and 4-aminoantipyrine was analyzed. The calibration graphs were prepared in the range of 0.5 to 4 ppm of phenol. Phenol in apple, pear and sweet orange was found to be in the range of 1-1.2 ppm and in radish was found to be 0.5 ppm. Possible source of organic pollutant were pointed out and were discussed. Limits of detection of the method was investigated and was found to be 0.2 mu g/ml

  10. Determination of etoricoxib in human plasma using automated on-line solid-phase extraction coupled with LC-APCI/MS/MS

    Directory of Open Access Journals (Sweden)

    Sérgio Luiz Dalmora

    2008-01-01

    Full Text Available A liquid chromatography-tandem mass spectrometry method with atmospheric pressure chemical ionization (LC-APCI/MS/MS was validated for the determination of etoricoxib in human plasma using antipyrin as internal standard, followed by on-line solid-phase extraction. The method was performed on a Luna C18 column and the mobile phase consisted of acetonitrile:water (95:5, v/v/ammonium acetate (pH 4.0; 10 mM, run at a flow rate of 0.6 mL/min. The method was linear in the range of 1-5000 ng/mL (r²>0.99. The lower limit of quantitation was 1 ng/mL. The recoveries were within 93.72-96.18%. Moreover, method validation demonstrated acceptable results for the precision, accuracy and stability studies.

  11. Phenobarbital treatments lower DDT body burden in rhesus monkeys

    Energy Technology Data Exchange (ETDEWEB)

    Ferguson, P.W.; Clark, C.R.; Gee, S.J.; Krieger, R.I.

    1981-01-01

    Decreased DDT, DDD, DDE in blood and DDA in urine followed phenobarbital treatments (10 mg/kg/day, 11 days, intramuscular (im)) in three male rhesus monkeys (Macaca mulatta). Animals were fed DDT diets containing up to 500 ppm DDT during a 3-year period. Induction of liver monooxygenases was confirmed by reduced in vivo antipyrine plasma half-life and increased in vitro oxidation rates of dihydroisodrin, p-nitroanisole and benz(alpha)pyrene by homogenates of liver obtained from closed needle biopsy. Chlorohydrocarbon blood levels significantly decreased during the induction period (days 1-11). Concentrations on day 28 were at or below pre-DDT exposure levels. Urine DDA gradually decreased in all monkeys from days 16 to 28.

  12. Osler on migraine.

    Science.gov (United States)

    Boes, Christopher J

    2015-03-01

    William Osler's 1892 textbook The Principles and Practice of Medicine became the dominant medical text in the English-speaking world. Osler was labeled a therapeutic nihilist by some. The topic of migraine, including treatment, was succinctly covered in his text. The objectives of this study were to review Osler's thoughts on migraine, and outline his therapeutic recommendations. Preventively Osler mentioned bromides, iron, arsenic, nitroglycerin, and cannabis. Acutely he recommended coffee, chloroform, cannabis, antipyrin, antifebrin, phenacetin, caffeine citrate, nux vomica, or ergot. He thought cannabis was the most satisfactory remedy. Osler was not a therapeutic nihilist when it came to migraine, and his treatment recommendations were similar to other writers of his time. Osler did not draw upon his personal experience to contribute new knowledge about migraine. Regardless, given the popularity and clarity of his text, Osler's well-summarized migraine chapter had a great influence on practicing physicians.

  13. The Use of 4-(3,4-Dichlorophenyl-4-Oxo-2-(4-Antipyrinyl-Butanoic Acid in the Preparation of Some New Heterocyclic Compounds With Expected Biological Activity

    Directory of Open Access Journals (Sweden)

    M. Shafik

    2003-03-01

    Full Text Available Reaction of 4-oxo-4-(3,4-dichlorophenyl-2-butenoic acid (1 with antipyrin (2 gave the corresponding butanoic acid 3. Reaction of 3 with hydrazines gave the pyridazinone derivatives 5a,b. Compounds 5a,b were used to prepare the corresponding dithio derivatives. Reaction of 5a with POCl3 unexpectedly gave the chloropyridazine derivative 7, which is used to prepare the corresponding thio derivative. The hitherto unknown reactions of this chloro derivative with 2-amino-3-carbethoxy-4,5-dimethylthiophene and 2-amino-3-carbethoxy tetrahydrobenzothiophene have now been described. The behaviour of the chloro derivative toward hydrazine hydrate, sodium azide and anthranilic acid was also studied. Some of the new compounds showed antimicrobial and antifungal activities .

  14. Design and evaluation of radiotracers for determination of regional cerebral blood flow with PET

    International Nuclear Information System (INIS)

    Lambrecht, R.M.; Duncan, C.C.; Shiue, C.Y.

    1982-01-01

    The tracer kinetics of 4-Fluoro( 18 F)-, 4-Bromo( 82 Br)- and 4-Iodo( 125 I)-antipyrine and 15 O-water were compared in a cat or baboon animal model. First-pass cerebral extraction and clearance with alterations in PaCO 2 were measured for whole brain. The Renkin/Crone model was used to evaluate brain capillary permeability-surface area product for 4- 18 FAP in cats. Positron-emission-tomographic measurements required development of an instrument and technique for control of the arterial concentration of the radiotracer as a ramp function, so that tracer concentration changes due to radioactive decay or altered physiological processes could be accurately described with PET. Pharmacokinetic and tissue-distribution studies in cats were used to determine dosimetry for 4- 18 FAP. 4-Bromoantipyrine labeled with 78 Br (t = 6.5 m) is suggested as a tracer for determination of rCBF with PET

  15. The double isotope technique for in vivo determination of the tissue-to-blood partition coefficient for xenon in human subcutaneous adipose tissue--an evaluation

    DEFF Research Database (Denmark)

    Jelnes, Rolf; Astrup, A; Bülow, J

    1985-01-01

    the partition coefficient found by the double isotope technique, significantly lower values are obtained than if the in vitro determined coefficient is used. This difference is explained mainly by local dilution when injecting xenon subcutaneously. In short-term studies, utilization of the double isotope...... technique reduces the coefficient of variation on average flow determinations, thus an improvement in accuracy of local blood flow estimation can be obtained compared to the method in which an average partition coefficient is used. For long-term studies a partition coefficient of 7.5 ml g-1 seems valid.......Local subcutaneous 133xenon (133Xe) elimination was registered in the human forefoot in 34 patients. The tissue/blood partition coefficient for Xe was estimated individually by simultaneous registration of 133Xe and [131I]antipyrine ([131I]AP) washout from the same local depot. When measured...

  16. 1,5-Dimethyl-2-phenyl-1H-pyrazol-3(2H-one–4,4′-(propane-2,2-diylbis[1,5-dimethyl-2-phenyl-1H-pyrazol-3(2H-one] (1/1

    Directory of Open Access Journals (Sweden)

    Krzysztof Lyczko

    2013-01-01

    Full Text Available The asymmetric unit of the title compound, C11H12N2O·C25H28N4O2, contains two different molecules. The smaller is known as antipyrine [systematic name: 1,5-dimethyl-2-phenyl-1H-pyrazol-3(2H-one] and the larger is built up from two antypirine molecules which are connected through a C atom of the pyrazolone ring to a central propanyl part [systematic name: 4,4′-(propane-2,2-diylbis[1,5-dimethyl-2-phenyl-1H-pyrazol-3(2H-one]. Intramolecular C—H...O hydrogen bonds occur in the latter molecule. In the crystal, C—H...O hydrogen bonds link the molecules into a two-dimensional network parallel to (001.

  17. Variations of some parameters of enzyme induction in chemical workers

    Energy Technology Data Exchange (ETDEWEB)

    Dolara, P. (Univ. of Florence, Italy); Lodovici, M.; Buffoni, F.; Buiatti, E.; Baccetti, S.; Ciofini, O.; Bavazzano, P.; Barchielli, S.; Vannucci, V.

    1982-01-01

    Several parameters related to mono-oxygenase activity were followed in a population of chemical workers and controls. Workers exposed to toluene and xylene had a significant increase of urinary glucaric acid, that was correlated with hippuric acid excretion. On the other hand, workers exposed to pigments showed a marked increase of antipyrine half-life. A dose-related decrease of liver N-demethylase was induced in rats by the administration of a mixture of three of the pigments in use in the plant. Serum gamma-glutamyltranspeptidase was decreased in the workers exposed to pigments, but this variation was not statistically significant. The exposure to different chemicals in the workplace seemed to induce a complicated variation of mono-oxygenase levels, some enzyme being inhibited and others induced in the same group of workers. The sensitivity of these workers to toxic effects of chemicals, carcinogenic compounds and drugs seems to differ markedly from the control population.

  18. On the pathogenesis of bedsores. Skin blood flow cessation by external pressure on the back

    DEFF Research Database (Denmark)

    Larsen, B; Holstein, P; Lassen, N A

    1979-01-01

    This paper is devoted to elucidation of the question: Which external pressure is required to stop skin blood flow at the skin - support interface in humans lying on the back in the supine position? Cessation of blood flow was recorded as cessation of washout of an intracutaneous depot of 131I......-antipyrine mixed with histamine. The external pressure was measured by a small airfilled plastic cushion connected to a mercury manometer. In 11 normal subjects, eight patients with hypertension and seven patients with tetra- or paraplegia the "flow cessation external pressure" (FCEP) was strongly correlated...... to the auscultatory brachial mean blood pressure (p less than or equal to 0.001). The difference mean blood pressure - FCEP was on average 4 mmHg (range (-11) - (+20) mmHg) and there was no significant difference between the three groups studied. Thus external pressure exceeding the actual mean blood pressure...

  19. Extraction-differential-photometric method to determine rare earths of cerium subgroup

    International Nuclear Information System (INIS)

    Askerov, D.N.; Gusejnov, I.K.; Melikov, A.A.

    1985-01-01

    The extraction - photometric method to determine great quantities of rare earths of the cerium subgroup as a complex with antipyrine A and diphenylguanidine is developed. Isobutyl and n-butyl alcohols are used as extractants. It is established that proportional dependence between relative optical density and concentration of rare earths of the cerium subgroup in the solution takes place in the concentration interval of 10.3-14.7 μg of rare earths in 1 ml of the solution. Determination error is+-1.12%. The technique is used to determine rare earths of the cerium subgroup in rare earth oxides of a mixed composition, as well as in monozite and loparite

  20. /sup 123/I production at the Milan AVF cyclotron

    Energy Technology Data Exchange (ETDEWEB)

    Acerbi, E; Birattari, C; Castiglioni, M; Resmini, F [Milan Univ. (Italy). Istituto di Fisica

    1976-01-01

    A program is described to make available quantities of at least 20 mCi of /sup 123/I per irradiation, on a weekly routine basis to medical users at the Clinical Physiology Laboratory of Pisa. Contaminants such as /sup 124/I should be kept below 3%. The isotope, or compounds of it, like iodo-antipyrine and ortho-iodohippuric acid, were to be used as scanning agents for pancreas, kidneys, thyroid and for the detection of the aqueous content in the pulmonary region. The production of /sup 123/I from enriched /sup 124/Te is described. Preliminary experiments on a distillation separation of iodine from the Te target have been performed and the method seems promising in comparison to the time-consuming chemical separation technique.

  1. Research review. Interactions between environmental chemicals and drug biotransformation in man.

    Science.gov (United States)

    Alvares, A P

    1978-01-01

    Many factors influence the metabolism of drugs in man. Besides genetic factors, environmental factors may play a significant role in explaining the variation observed in the rates of drug metabolism between different individuals. Intentional or unintentional exposure to environmental chemicals could enhance or inhibit the activity of hepatic mixed function oxidases that metabolise drugs and other foreign chemicals, as well as endogenous substrates such as steroid hormones. A major source of such exposure may be occupational. Exposure to the heavy metal, lead, has been shown to inhibit drug metabolism; whereas intensive exposure to chlorinated insecticides, and other halogenated hydrocarbons such as polychlorinated biphenyls, has been shown to enhance the metabolism of test drugs such as antipyrine and phenylbutazone. An intentional source of exposure to foreign chemicals is cigarette smoke. Cigarette smoke contains polycyclic hydrocarbons, which are known inducers of hepatic mixed function oxidases. A number of studies have shown that cigarette smoking can alter the pharmacological action and/or the metabolism of some drugs. Pharmacokinetic studies have shown that cigarette smoking decreases the bioavailability of phenacetin and increases dosage requirements of theophylline by enhancing their rate of metabolism. Data, which are not very conclusive, indicate that heavy marijuana use may have an inhibitory effect on metabolism of some drugs and an inducing effect on others such as theophylline. Dietary factors may also play a significant role in the regulation of drug metabolism. Charcoal broiling which introduces polycyclic hydrocarbons into foods has been shown to enhance the metabolism of the test drug, antipyrine, and of such commonly used drugs as phenacetin and theophylline. Such intentional or unintentional exposure to environmental chemicals which may alter the rates of drug metabolism in man indicates the importance of individualisation of drug therapy.

  2. A novel combined solar pasteurizer/TiO2 continuous-flow reactor for decontamination and disinfection of drinking water.

    Science.gov (United States)

    Monteagudo, José María; Durán, Antonio; Martín, Israel San; Acevedo, Alba María

    2017-02-01

    A new combined solar plant including an annular continuous-flow compound parabolic collector (CPC) reactor and a pasteurization system was designed, built, and tested for simultaneous drinking water disinfection and chemical decontamination. The plant did not use pumps and had no electricity costs. First, water continuously flowed through the CPC reactor and then entered the pasteurizer. The temperature and water flow from the plant effluent were controlled by a thermostatic valve located at the pasteurizer outlet that opened at 80 °C. The pasteurization process was simulated by studying the effect of heat treatment on the death kinetic parameters (D and z values) of Escherichia coli K12 (CECT 4624). 99.1% bacteria photo-inactivation was reached in the TiO 2 -CPC system (0.60 mg cm -2 TiO 2 ), and chemical decontamination in terms of antipyrine degradation increased with increasing residence time in the TiO 2 -CPC system, reaching 70% degradation. The generation of hydroxyl radicals (between 100 and 400 nmol L -1 ) was a key factor in the CPC system efficiency. Total thermal bacteria inactivation was attained after pasteurization in all cases. Chemical degradation and bacterial photo-inactivation in the TiO 2 -CPC system were improved with the addition of 150 mg L -1 of H 2 O 2 , which generated approximately 2000-2300 nmol L -1 of HO ● radicals. Finally, chemical degradation and bacterial photo-inactivation kinetic modelling in the annular CPC photoreactor were evaluated. The effect of the superficial liquid velocity on the overall rate constant was also studied. Both antipyrine degradation and E. coli photo-inactivation were found to be controlled by the catalyst surface reaction rate. Copyright © 2016 Elsevier Ltd. All rights reserved.

  3. Transit time dispersion in pulmonary and systemic circulation: effects of cardiac output and solute diffusivity.

    Science.gov (United States)

    Weiss, Michael; Krejcie, Tom C; Avram, Michael J

    2006-08-01

    We present an in vivo method for analyzing the distribution kinetics of physiological markers into their respective distribution volumes utilizing information provided by the relative dispersion of transit times. Arterial concentration-time curves of markers of the vascular space [indocyanine green (ICG)], extracellular fluid (inulin), and total body water (antipyrine) measured in awake dogs under control conditions and during phenylephrine or isoproterenol infusion were analyzed by a recirculatory model to estimate the relative dispersions of transit times across the systemic and pulmonary circulation. The transit time dispersion in the systemic circulation was used to calculate the whole body distribution clearance, and an interpretation is given in terms of a lumped organ model of blood-tissue exchange. As predicted by theory, this relative dispersion increased linearly with cardiac output, with a slope that was inversely related to solute diffusivity. The relative dispersion of the flow-limited indicator antipyrine exceeded that of ICG (as a measure of intravascular mixing) only slightly and was consistent with a diffusional equilibration time in the extravascular space of approximately 10 min, except during phenylephrine infusion, which led to an anomalously high relative dispersion. A change in cardiac output did not alter the heterogeneity of capillary transit times of ICG. The results support the view that the relative dispersions of transit times in the systemic and pulmonary circulation estimated from solute disposition data in vivo are useful measures of whole body distribution kinetics of indicators and endogenous substances. This is the first model that explains the effect of flow and capillary permeability on whole body distribution of solutes without assuming well-mixed compartments.

  4. Zr-doped TiO{sub 2} supported on delaminated clay materials for solar photocatalytic treatment of emerging pollutants

    Energy Technology Data Exchange (ETDEWEB)

    Belver, C., E-mail: carolina.belver@uam.es; Bedia, J.; Rodriguez, J.J.

    2017-01-15

    Highlights: • Novel Zr-doped TiO{sub 2} delaminated clay materials were prepared by a sol-gel process. • Zr is incorporated into the anatase lattice. • Zr-TiO{sub 2} nanoparticles are homogenously distributed over the delaminated clay. • Zr doping enhances the photoactivity by reducing the band gap. • Degradation rates were favored at low concentrations and high radiation intensities. - Abstract: Solar light-active Zr-doped TiO{sub 2} nanoparticles were successfully immobilized on delaminated clay materials by a one-step sol-gel route. Fixing the amount of TiO{sub 2} at 65 wt.%, this work studies the influence of Zr loading (up to 2%) on the photocatalytic activity of the resulting Zr-doped TiO{sub 2}/clay materials. The structural characterization demonstrates that all samples were formed by a delaminated clay with nanostructured anatase assembled on its surface. The Zr dopant was successfully incorporated into the anatase lattice, resulting in a slight deformation of the anatase crystal and the reduction of the band gap. These materials exhibit high surface area with a disordered mesoporous structure formed by TiO{sub 2} particles (15–20 nm) supported on a delaminated clay. They were tested in the solar photodegradation of antipyrine, usually used as an analgesic drug and selected as an example of emerging pollutant. High degradation rates have been obtained at low antipyrine concentrations and high solar irradiation intensities with the Zr-doped TiO{sub 2}/clay catalyst, more effective than the undoped one. This work demonstrates the potential application of the synthesis method for preparing novel and efficient solar-light photocatalysts based on metal-doped anatase and a delaminated clay.

  5. Heterogeneous distribution of a diffusional tracer in the aortic wall of normal and atherosclerotic rabbits

    International Nuclear Information System (INIS)

    Tsutsui, H.; Tomoike, H.; Nakamura, M.

    1990-01-01

    Tracer distribution as an index of nutritional support across the thoracic and abdominal aortas in rabbits in the presence or absence of atherosclerotic lesions was evaluated using [ 14 C]antipyrine, a metabolically inert, diffusible indicator. Intimal plaques were produced by endothelial balloon denudation of the thoracic aorta and a 1% cholesterol diet. After a steady intravenous infusion of 200 microCi of [ 14 C]antipyrine for 60 seconds, thoracic and abdominal aortas and the heart were excised, and autoradiograms of 20-microns-thick sections were quantified, using microcomputer-aided densitometry. Regional radioactivity and regional diffusional support, as an index of nutritional flow estimated from the timed collections of arterial blood, was 367 and 421 nCi.g-1 (82 and 106 ml.min-1.100 g-1) in thoracic aortic media of the normal and atherosclerotic rabbits, respectively. Radioactivity at the thickened intima was 179 nCi.g-1 (p less than 0.01 versus media). The gruel was noted at a deeper site within the thickened intima, and diffusional support here was 110 nCi.g-1 (p less than 0.01 versus an average radioactivity at the thickened intima). After ligating the intercostal arteries, regional tracer distribution in the media beneath the fibrofatty lesion, but not the plaque-free intima, was reduced to 46%. Thus, in the presence of advanced intimal thickening, the heterogeneous distribution of diffusional flow is prominent across the vessel wall, and abluminal routes are crucial to meet the increased demands of nutritional requirements

  6. LC-QTOF MS screening of more than 1,000 licit and illicit drugs and their metabolites in wastewater and surface waters from the area of Bogotá, Colombia.

    Science.gov (United States)

    Hernández, Félix; Ibáñez, María; Botero-Coy, Ana-María; Bade, Richard; Bustos-López, Martha Cristina; Rincón, Javier; Moncayo, Alejandro; Bijlsma, Lubertus

    2015-08-01

    A large screening of around 1,000 emerging contaminants, focused on licit and illicit drugs and their metabolites, has been made in urban wastewaters (both influent and effluent) and surface waters from the area of Bogotá, Colombia. After a simple generic solid-phase extraction (SPE) step with Oasis hydrophilic-lipophilic balanced (HLB) cartridges, analyses were made by ultra high-performance liquid chromatography coupled to quadrupole time-of-flight mass spectrometry (UHPLC-QTOF MS) under MS(E) mode (sequential acquisition of mass spectra at low energy (LE) and high collision energy (HE)). Accurate mass measurements and the information provided by MS(E) on the presence of the (de)protonated molecule and fragment ions allowed the reliable identification of the compounds detected, even without reference standards being available in some cases (tentative identification). The compounds most frequently found were acetaminophen/paracetamol, carbamazepine and its dihydro-dihydroxylated metabolite, clarithromycin, diclofenac, ibuprofen, gemfibrozil, lincomycin, losartan, valsartan, the two metabolites of metamizole (4-acetamido-antipyrine and 4-formylamino-antipyrine), sucralose, and cocaine and its main metabolite benzoylecgonine. Caffeine, the sweetener saccharin, and two hydroxylated metabolites of losartan were tentatively identified in almost all samples analyzed. Pharmaceutical lidocaine was tentatively identified and subsequently confirmed with reference standard. For the first time, a general overview of the occurrence of drugs and their metabolites in the aquatic environment of Colombia has been reported. In the near future, target methodologies, typically based on liquid chromatography coupled to tandem mass spectrometry (LC-MS/MS), will need to be set up for accurate and sensitive quantification of the contaminants selected on the basis on the information provided in the present paper.

  7. Influence of type of ration on the growth rate and carcass quality of young goat

    International Nuclear Information System (INIS)

    Kumar, P.; Singh, U.B.; Ranjhan, S.K.

    1976-01-01

    Twelve young goats (six males and six females) weighing about 10 kg in body weight were divided into two groups and were offered the following rations: (A) all forage diet ad lib consisting of berseem hay and mineral supplements and (B) diet A + 250 gm concentrate mixture (per animal) consisting of 3 parts of maize and one part of wheat bran and mineral supplements. After a preliminary feeding period of 60 days a metabolism trial was conducted to determine nutrient utilization. The animals were continued further on the same ration for another 120 days; a feeding trial was conducted and the body composition was studied in six animals by injecting 5 ml of 10% antipyrine solution and the animals were sacrificed to study carcass characteristics. 50 μci of 14 C tyrosine was injected 24 hours before slaughter and its incorporation into muscle proteins was determined. It has been observed that supplementation of the concentrate to the ration improved the performance of animals. The supplementation has improved growth rate to 38.5 g/day from 13 g/day of the forage fed group of animals. The results of the study are discussed. (author)

  8. Cerebrospinal fluid ionic regulation, cerebral blood flow, and glucose use during chronic metabolic alkalosis

    International Nuclear Information System (INIS)

    Schroeck, H.K.; Kuschinsky, W.

    1989-01-01

    Chronic metabolic alkalosis was induced in rats by combining a low K+ diet with a 0.2 M NaHCO3 solution as drinking fluid for either 15 or 27 days. Local cerebral blood flow and local cerebral glucose utilization were measured in 31 different structures of the brain in conscious animals by means of the iodo-[14C]antipyrine and 2-[14C]deoxy-D-glucose method. The treatment induced moderate [15 days, base excess (BE) 16 mM] to severe (27 days, BE 25 mM) hypochloremic metabolic alkalosis and K+ depletion. During moderate metabolic alkalosis no change in cerebral glucose utilization and blood flow was detectable in most brain structures when compared with controls. Cerebrospinal fluid (CSF) K+ and H+ concentrations were significantly decreased. During severe hypochloremic alkalosis, cerebral blood flow was decreased by 19% and cerebral glucose utilization by 24% when compared with the control values. The decrease in cerebral blood flow during severe metabolic alkalosis is attributed mainly to the decreased cerebral metabolism and to a lesser extent to a further decrease of the CSF H+ concentration. CSF K+ concentration was not further decreased. The results show an unaltered cerebral blood flow and glucose utilization together with a decrease in CSF H+ and K+ concentrations at moderate metabolic alkalosis and a decrease in cerebral blood flow and glucose utilization together with a further decreased CSF H+ concentration at severe metabolic alkalosis

  9. Blood flow and blood volume in a transplanted rat fibrosarcoma

    International Nuclear Information System (INIS)

    Tozer, G.M.; Morris, C.C.

    1990-01-01

    Blood flow measurements following i.v. infusion of iodi-antipyrine labelled with 14 C ( 14 C-IAP) and blood volume measurements following i.v. injection of 125 I human serum albumin and 51 Cr-labelled red blood cells were made in a transplanted rat fibrosarcoma for comparison with various normal tissues. The tumour-blood partition co-efficient for 14 C-IAP w as found to be 0.79 ± 0.07 which is similar to most of the normal tissues studied. The solubility of 14 C-IAP in plasma was found to be higher than that in whole blood. Blood flow to tumours 3 was found to be 17.9 ± 4.0 ml blood 100 g tissue -1 xmin -1 . These values were considered to be primarily measurements of nutritive flow. Blood in the tumours was found to occupy around 1% of the tissue space which was similar to that found for normal muscle and skin. There was no direct correlation between % blood volume and blood flow for the different tissues studied. Th haematocrit of blood contained in tumour tissue was calculated to be significantly lower than that of blood contained in the normal tissues. It was suspected that permeability of tumour blood vessel walls to 125 I-HSA could have accounted for this difference. (author). 41 refs.; 2 figs.; 3 tabs

  10. A modified scintigrafic technique for amputation level selection in diabetics

    International Nuclear Information System (INIS)

    Dwars, B.J.; Rauwerda, J.A.; Broek, T.A.A. van den; Rij, G.L. van; Hollander, W. den; Heidendal, G.A.K.

    1989-01-01

    A modified 123 I-antipyrine cutaneous washout technique for the selection of amputation levels is described. The modifications imply a reduction of time needed for the examination by simultaneous recordings on different levels, and a better patient acceptance by reducing inconvenience. Furthermore, both skin perfusion pressure (SPP) and skin blood flow (SBF) are determined from each clearance curve. In a prospective study among 26 diabetic patients presenting with ulcers or gangrene of the foot, both SPP and SBF were determined preoperatively on the selected level of surgery and on adjacent amputation sites. These 26 patients underwent 12 minor foot amputations and 17 major lower limb amputations. Two of these amputations failed to heal. SBF values appeared indicative for the degree of peripheral vascular disease, as low SBF values were found with low SPP values. SPP determinations revealed good predictive values: All surgical procedures healed when SPP>20 mmHg, but 2 out of 3 failed when SPP<2 mmHg. If SPP values would have been decisive, the amputation would have been converted to a lower level in 6 out of 17 cases. This modified scintigrafic technique provides accurate objective information for amputation level selection. (orig.)

  11. Estimate of body composition by Hume's equation: validation with DXA.

    Science.gov (United States)

    Carnevale, Vincenzo; Piscitelli, Pamela Angela; Minonne, Rita; Castriotta, Valeria; Cipriani, Cristiana; Guglielmi, Giuseppe; Scillitani, Alfredo; Romagnoli, Elisabetta

    2015-05-01

    We investigated how the Hume's equation, using the antipyrine space, could perform in estimating fat mass (FM) and lean body mass (LBM). In 100 (40 male ad 60 female) subjects, we estimated FM and LBM by the equation and compared these values with those measured by a last generation DXA device. The correlation coefficients between measured and estimated FM were r = 0.940 (p LBM were r = 0.913 (p LBM, though the equation underestimated FM and overestimated LBM in respect to DXA. The mean difference for FM was 1.40 kg (limits of agreement of -6.54 and 8.37 kg). For LBM, the mean difference in respect to DXA was 1.36 kg (limits of agreement -8.26 and 6.52 kg). The root mean square error was 3.61 kg for FM and 3.56 kg for LBM. Our results show that in clinically stable subjects the Hume's equation could reliably assess body composition, and the estimated FM and LBM approached those measured by a modern DXA device.

  12. Labelling of some organic compounds with radioactive iodine for medical uses

    International Nuclear Information System (INIS)

    El-tawoosy, M.E.M.

    1997-01-01

    Among all radioisotopes, radioiodine(i.e. 122 I, 123 I, 125 I. 131 I) is the most available tagging element when considering new radiopharmaceutical compounds intended for nuclear medicine uses for in -Vitro and in - vivo measurements. The aim of this work is to optimize and developed new methods of radioiodination of some organic molecules for use in nuclear medicine as diagnostic agents. Some trials for labelling of meta - iodo benzyl guanidine (MIBG), antipyrine (AP) and 3,5,3- tri - iodothyronine (T 3 ) will be done. In the present study, we will try to get easier, short time, high yield, high specific activity, high radiochemical purity and economic methods for the preparation of the following radiopharmaceutical compounds: 1- (m- 131 I) meat - iodo benzyl guanidine (m- 131 I) MIBG for adrenal medulla and myocardial measurements. 2-(4- 131 I) iodoantipyrine (4- 131 I) IAP for brain measurements. 3-( 131 I) tetra -iodothyronine ( 131 I) T 4 for thyroid gland function studies. The influence of substrate conc., reaction time, different oxidizing agents and catalyst concentrations will be investigated to elucidate the optimum methods suitable for preparation of these compounds. Chromatographic techniques such as paper chromatography, thin layer chromatography (TLC), column chromatography and high pressure liquid chromatography (HPLC) will be used for the identification, quality control, purification and quality assurance of the final product. 4.2 tabs., 4.5 figs., 204 refs

  13. Degradation of fifteen emerging contaminants at microg L(-1) initial concentrations by mild solar photo-Fenton in MWTP effluents.

    Science.gov (United States)

    Klamerth, N; Rizzo, L; Malato, S; Maldonado, Manuel I; Agüera, A; Fernández-Alba, A R

    2010-01-01

    The degradation of 15 emerging contaminants (ECs) at low concentrations in simulated and real effluent of municipal wastewater treatment plant with photo-Fenton at unchanged pH and Fe=5 mg L(-1) in a pilot-scale solar CPC reactor was studied. The degradation of those 15 compounds (Acetaminophen, Antipyrine, Atrazine, Caffeine, Carbamazepine, Diclofenac, Flumequine, Hydroxybiphenyl, Ibuprofen, Isoproturon, Ketorolac, Ofloxacin, Progesterone, Sulfamethoxazole and Triclosan), each with an initial concentration of 100 microg L(-1), was found to depend on the presence of CO(3)(2-) and HCO(3)(-) (hydroxyl radicals scavengers) and on the type of water (simulated water, simulated effluent wastewater and real effluent wastewater), but is relatively independent of pH, the type of acid used for release of hydroxyl radicals scavengers and the initial H(2)O(2) concentration used. Toxicity tests with Vibrio fisheri showed that degradation of the compounds in real effluent wastewater led to toxicity increase. (c) 2009 Elsevier Ltd. All rights reserved.

  14. Application of photo-fenton as a tertiary treatment of emerging contaminants in municipal wastewater.

    Science.gov (United States)

    Klamerth, N; Malato, S; Maldonado, M I; Agüera, A; Fernández-Alba, A R

    2010-03-01

    This work focuses on the treatment of real effluents from a municipal wastewater treatment plant (RE) with solar photo-Fenton (5 mg and 20 mg L(-1) Fe, pH approximately 3 and 50 mg L(-1) initial H(2)O(2) concentration) at pilot plant scale. In some experiments RE was spiked with 15 different (acetaminophen, antipyrine, atrazine, caffeine, carbamazepine, diclofenac, flumequine, hydroxybiphenyl, ibuprofen, isoproturon, ketorolac, ofloxacin, progesterone, sulfamethoxazole, and triclosan) emerging contaminants (ECs) at 100 and 5 microg L(-1) each which were added directly into RE prior to treatment. All experiments showed successful degradation of ECs in real effluents from different municipal wastewater treatment plants at low iron concentration (5 mg L(-1)). Although the most degradation took place during the Fenton process, photo-Fenton was necessary to degrade all ECs below their limit of detection (LOD). In the case of the RE containing 52 ECs (determined by HPLC-QTRAP-MS), four of them could not be degraded to their LOD and were still present, although at extremely low concentrations (nicotine 47 ng L(-1), cotinine 11 ng L(-1), chlorfenvinphos 99 ng L(-1), and caffeine 8 ng L(-1)). ECs were easily degraded by (*)OH without substantial competition with the organic content of the RE.

  15. Determination of the subcutaneous tissue to blood partition coefficient in patients with severe leg ischaemia by a double isotope washout technique

    DEFF Research Database (Denmark)

    Bjerre-Jepsen, K; Faris, I; Henriksen, O

    1982-01-01

    Knowledge of the tissue to blood partition coefficient (lambda) is essential for calculation of the perfusion coefficient in a single tissue based on measurements of the washout of locally injected isotopes. No measurements of lambda for Xenon in subcutaneous tissue in the leg have been done...... in patients with occlusive arterial disease. In 12 patients with occlusive arterial disease in the legs lambda for Xenon was determined in subcutaneous tissue in the calf region and foot as the ratio between the washout rate constant of 131I-Antipyrine and 133Xe. A mixture of the two indicators was injected....... Mean value was 3.7 ml X g-1 (range: 1 X 7-10 X 7) in the calf and 2 X 7 ml X g-1 (range: 1 X 2-4 X 9) in the foot. It is concluded that lambda measurements are necessary for determination of subcutaneous blood flow from 133Xe washout curves in these patients. Determination of lambda is especially...

  16. Microbial degradation of pharmaceuticals in estuarine and coastal seawater

    Energy Technology Data Exchange (ETDEWEB)

    Benotti, Mark J. [Marine Sciences Research Center, Stony Brook University, Stony Brook, NY 11794-5000 (United States); Brownawell, Bruce J. [Marine Sciences Research Center, Stony Brook University, Stony Brook, NY 11794-5000 (United States)], E-mail: bruce.brownawell@sunysb.edu

    2009-03-15

    Microbial degradation rates were measured for 19 pharmaceuticals in estuarine and coastal surface water samples. Antipyrine, carbamazepine, cotinine, sulfamethoxazole, and trimethoprim were the most refractory (half-lives, t{sub 1/2} = 35 to >100 days), making them excellent candidates for wastewater tracers. Nicotine, acetaminophen, and fluoxetine were labile across all treatments (t{sub 1/2} = 0.68-11 days). Caffeine, diltiazem, and nifedipine were also and relatively labile in all but one of the treatments (t{sub 1/2} = 3.5-13 days). Microbial degradation of caffeine was further confirmed by production {sup 14}CO{sub 2}. The fastest decay of non-refractory compounds was always observed in more sewage-affected Jamaica Bay waters. Degradation rates for the majority of these pharmaceuticals are much slower than reported rates for small biomolecules, such as glucose and amino acids. Batch sorption experiments indicate that removal of these soluble pharmaceuticals from the water column to sediments is a relatively insignificant removal process in these receiving waters. - Microbial degradation rates were measured for 19 structurally variable pharmaceuticals in wastewater-impacted estuarine and coastal seawater.

  17. Validation of an immortalized human (hBMEC) in vitro blood-brain barrier model.

    Science.gov (United States)

    Eigenmann, Daniela Elisabeth; Jähne, Evelyn Andrea; Smieško, Martin; Hamburger, Matthias; Oufir, Mouhssin

    2016-03-01

    We recently established and optimized an immortalized human in vitro blood-brain barrier (BBB) model based on the hBMEC cell line. In the present work, we validated this mono-culture 24-well model with a representative series of drug substances which are known to cross or not to cross the BBB. For each individual compound, a quantitative UHPLC-MS/MS method in Ringer HEPES buffer was developed and validated according to current regulatory guidelines, with respect to selectivity, precision, and reliability. Various biological and analytical challenges were met during method validation, highlighting the importance of careful method development. The positive controls antipyrine, caffeine, diazepam, and propranolol showed mean endothelial permeability coefficients (P e) in the range of 17-70 × 10(-6) cm/s, indicating moderate to high BBB permeability when compared to the barrier integrity marker sodium fluorescein (mean P e 3-5 × 10(-6) cm/s). The negative controls atenolol, cimetidine, and vinblastine showed mean P e values < 10 × 10(-6) cm/s, suggesting low permeability. In silico calculations were in agreement with in vitro data. With the exception of quinidine (P-glycoprotein inhibitor and substrate), BBB permeability of all control compounds was correctly predicted by this new, easy, and fast to set up human in vitro BBB model. Addition of retinoic acid and puromycin did not increase transendothelial electrical resistance (TEER) values of the BBB model.

  18. Comparison of Mass Transfer Models for Determination of the Intestinal Permeability

    Directory of Open Access Journals (Sweden)

    P Zakeri-Milani

    2008-09-01

    Full Text Available Background and the purpose of the study: In determination of the permeability of the intestinal wall by external perfusion techniques, several models have been proposed. In the present study three models were used for experimental results that differ in their convection and diffusion assumptions. Material and Methods: Permeability coefficients for 13 compounds (metoprolol, propranolol, naproxen, ketoprofen, furosemide, hydrochlorothiazide, cimetidine, ranitidine, atenolol, piroxicam, antipyrine, ibuprofen and carbamazepine with known human intestinal permeability values were determined in anaesthetized rats by different mass transfer models and plotted versus the observed human intestinal permeabilities. Results: The calculated dimensionless wall permeability values were in the range of 0.37 - 4.85, 0.38-6.54 and 0.41-16.59 for complete radial mixing, mixing tank and laminar flow models respectively. The results indicated that all of the models work relatively well for our data despite fundamentally different assumptions. The wall permeabilities were in the order laminar flow > mixing tank > complete radial mixing. Conclusion: Although laminar flow model provides the most direct measure of the intrinsic wall permeability, it has limitations for highly permeable drugs such as ibuprofen. The normal physiological hydrodynamics is more complex and more investigation is required to find out the real hydrodynamics.

  19. Modified scintigrafic technique for amputation level selection in diabetics

    Energy Technology Data Exchange (ETDEWEB)

    Dwars, B.J.; Rauwerda, J.A.; Broek, T.A.A. van den; Rij, G.L. van; Hollander, W. den; Heidendal, G.A.K.

    1989-01-01

    A modified /sup 123/I-antipyrine cutaneous washout technique for the selection of amputation levels is described. The modifications imply a reduction of time needed for the examination by simultaneous recordings on different levels, and a better patient acceptance by reducing inconvenience. Furthermore, both skin perfusion pressure (SPP) and skin blood flow (SBF) are determined from each clearance curve. In a prospective study among 26 diabetic patients presenting with ulcers or gangrene of the foot, both SPP and SBF were determined preoperatively on the selected level of surgery and on adjacent amputation sites. These 26 patients underwent 12 minor foot amputations and 17 major lower limb amputations. Two of these amputations failed to heal. SBF values appeared indicative for the degree of peripheral vascular disease, as low SBF values were found with low SPP values. SPP determinations revealed good predictive values: All surgical procedures healed when SPP>20 mmHg, but 2 out of 3 failed when SPP<2 mmHg. If SPP values would have been decisive, the amputation would have been converted to a lower level in 6 out of 17 cases. This modified scintigrafic technique provides accurate objective information for amputation level selection.

  20. Microbial degradation of pharmaceuticals in estuarine and coastal seawater

    International Nuclear Information System (INIS)

    Benotti, Mark J.; Brownawell, Bruce J.

    2009-01-01

    Microbial degradation rates were measured for 19 pharmaceuticals in estuarine and coastal surface water samples. Antipyrine, carbamazepine, cotinine, sulfamethoxazole, and trimethoprim were the most refractory (half-lives, t 1/2 = 35 to >100 days), making them excellent candidates for wastewater tracers. Nicotine, acetaminophen, and fluoxetine were labile across all treatments (t 1/2 = 0.68-11 days). Caffeine, diltiazem, and nifedipine were also and relatively labile in all but one of the treatments (t 1/2 = 3.5-13 days). Microbial degradation of caffeine was further confirmed by production 14 CO 2 . The fastest decay of non-refractory compounds was always observed in more sewage-affected Jamaica Bay waters. Degradation rates for the majority of these pharmaceuticals are much slower than reported rates for small biomolecules, such as glucose and amino acids. Batch sorption experiments indicate that removal of these soluble pharmaceuticals from the water column to sediments is a relatively insignificant removal process in these receiving waters. - Microbial degradation rates were measured for 19 structurally variable pharmaceuticals in wastewater-impacted estuarine and coastal seawater

  1. Rapid Enzymatic Method for Pectin Methyl Esters Determination

    Directory of Open Access Journals (Sweden)

    Lucyna Łękawska-Andrinopoulou

    2013-01-01

    Full Text Available Pectin is a natural polysaccharide used in food and pharma industries. Pectin degree of methylation is an important parameter having significant influence on pectin applications. A rapid, fully automated, kinetic flow method for determination of pectin methyl esters has been developed. The method is based on a lab-made analyzer using the reverse flow-injection/stopped flow principle. Methanol is released from pectin by pectin methylesterase in the first mixing coil. Enzyme working solution is injected further downstream and it is mixed with pectin/pectin methylesterase stream in the second mixing coil. Methanol is oxidized by alcohol oxidase releasing formaldehyde and hydrogen peroxide. This reaction is coupled to horse radish peroxidase catalyzed reaction, which gives the colored product 4-N-(p-benzoquinoneimine-antipyrine. Reaction rate is proportional to methanol concentration and it is followed using Ocean Optics USB 2000+ spectrophotometer. The analyzer is fully regulated by a lab written LabVIEW program. The detection limit was 1.47 mM with an analysis rate of 7 samples h−1. A paired t-test with results from manual method showed that the automated method results are equivalent to the manual method at the 95% confidence interval. The developed method is rapid and sustainable and it is the first application of flow analysis in pectin analysis.

  2. High-throughput optimization by statistical designs: example with rat liver slices cryopreservation.

    Science.gov (United States)

    Martin, H; Bournique, B; Blanchi, B; Lerche-Langrand, C

    2003-08-01

    The purpose of this study was to optimize cryopreservation conditions of rat liver slices in a high-throughput format, with focus on reproducibility. A statistical design of 32 experiments was performed and intracellular lactate dehydrogenase (LDHi) activity and antipyrine (AP) metabolism were evaluated as biomarkers. At freezing, modified University of Wisconsin solution was better than Williams'E medium, and pure dimethyl sulfoxide was better than a cryoprotectant mixture. The best cryoprotectant concentrations were 10% for LDHi and 20% for AP metabolism. Fetal calf serum could be used at 50 or 80%, and incubation of slices with the cryoprotectant could last 10 or 20 min. At thawing, 42 degrees C was better than 22 degrees C. After thawing, 1h was better than 3h of preculture. Cryopreservation increased the interslice variability of the biomarkers. After cryopreservation, LDHi and AP metabolism levels were up to 84 and 80% of fresh values. However, these high levels were not reproducibly achieved. Two factors involved in the day-to-day variability of LDHi were identified: the incubation time with the cryoprotectant and the preculture time. In conclusion, the statistical design was very efficient to quickly determine optimized conditions by simultaneously measuring the role of numerous factors. The cryopreservation procedure developed appears suitable for qualitative metabolic profiling studies.

  3. Analysis of skin permeation-enhancing mechanism of iontophoresis using hydrodynamic pore theory.

    Science.gov (United States)

    Manabe, E; Numajiri, S; Sugibayashi, K; Morimoto, Y

    2000-05-15

    The effects of constant DC iontophoresis (0-1.5 mA/0.966 cm(2)) on the permeation of three hydrophilic compounds, antipyrine (ANP, M.W. 188.23), sucrose (SR, M.W. 342.30) and 1-kestose (KT, M.W. 506.73), through excised hairless rat skin were evaluated using hydrodynamic pore theory. The electro-osmotic flow caused by iontophoresis was measured using deuterium oxide (D(2)O). The penetration-enhancing mechanism of iontophoresis was found to increase solvent flow through electro-osmosis and pore enlargement and/or new pore production in the skin barrier, together with enhancement of electrochemical potential difference across the skin. These effects were closely related to the strength of the current applied. The electro-osmotic flow of D(2)O (J(D(2)O)) greatly enhanced the skin permeation clearance of all hydrophilic penetrants (CL(drug)). Pore production was classified into reversible and irreversible processes, which resulted from lower (0-0.5 mA/0.966 cm(2)) and higher (0.5-1. 5 mA/0.966 cm(2)) currents, respectively. Thus, the enhancing effects of iontophoresis on skin permeation of nonionic hydrophilic compounds can be explained by increase in pore size and higher solvent flow.

  4. Different molecular conformations co-exist in each of three 2-aryl-N-(1,5-dimethyl-3-oxo-2-phenyl-2,3-dihydro-1H-pyrazol-4-yl)acetamides: hydrogen bonding in zero, one and two dimensions.

    Science.gov (United States)

    Narayana, Badiadka; Yathirajan, Hemmige S; Rathore, Ravindranath S; Glidewell, Christopher

    2016-09-01

    4-Antipyrine [4-amino-1,5-dimethyl-2-phenyl-1H-pyrazol-3(2H)-one] and its derivatives exhibit a range of biological activities, including analgesic, antibacterial and anti-inflammatory, and new examples are always of potential interest and value. 2-(4-Chlorophenyl)-N-(1,5-dimethyl-3-oxo-2-phenyl-2,3-dihydro-1H-pyrazol-4-yl)acetamide, C19H18ClN3O2, (I), crystallizes with Z' = 2 in the space group P\\overline{1}, whereas its positional isomer 2-(2-chlorophenyl)-N-(1,5-dimethyl-3-oxo-2-phenyl-2,3-dihydro-1H-pyrazol-4-yl)acetamide, (II), crystallizes with Z' = 1 in the space group C2/c; the molecules of (II) are disordered over two sets of atomic sites having occupancies of 0.6020 (18) and 0.3980 (18). The two independent molecules of (I) adopt different molecular conformations, as do the two disorder components in (II), where the 2-chlorophenyl substituents adopt different orientations. The molecules of (I) are linked by a combination of N-H...O and C-H...O hydrogen bonds to form centrosymmetric four-molecule aggregates, while those of (II) are linked by the same types of hydrogen bonds forming sheets. The related compound N-(1,5-dimethyl-3-oxo-2-phenyl-2,3-dihydro-1H-pyrazol-4-yl)-2-(3-methoxyphenyl)acetamide, C20H21N3O3, (III), is isomorphous with (I) but not strictly isostructural; again the two independent molecules adopt different molecular conformations, and the molecules are linked by N-H...O and C-H...O hydrogen bonds to form ribbons. Comparisons are made with some related structures, indicating that a hydrogen-bonded R2(2)(10) ring is the common structural motif.

  5. The role of sympathetic reflex control of cerebral blood flow and microcirculation during normoxia and hypoxia

    International Nuclear Information System (INIS)

    Kissen, I.

    1989-01-01

    The purpose of this study was to investigate the hypothesis that there is sympathetic reflex regulation of the cerebral blood flow (CBF) and the utilization of microvessels during normoxia and hypoxia. Regional CBF was determined in conscious Long Evans rats with 4-iodo[N-methyl- 14 C]antipyrine. The percentage of the microvessels perfused as determined by comparing perfused microvessels (FITC-dextran), with the total microvasculature (alkaline phosphatase stain). To test this hypothesis, arcs of the proposed reflex were eliminated. The first experiment examined the effect of bilateral superior cervical ganglionectomy on CBF and microcirulation during normoxia and hypoxia. CBF increased during hypoxia from 67 ± 2 to 115 ± 3 ml/min/100 g in control, and from 77 ± 2 to 155 ± 6 ml/min/100 g in ganglionectomized animals. In control, hypoxic flow to caudal areas was higher than to rostral areas and that difference was prevented by ganglionectomy. Utilization of arterioles during hypoxia increased from 51 ± 2% to 63 ± 2% in control, and from 52 ± 1% to 77 ± 2% in ganglionectomized group. The percent perfused capillaries during normoxia was 49 ± 2% in control, and 52 ± 1% in ganglionectomized group, and during hypoxia it was 73 ± 2% in both groups. In the second study, cerebral vascular responses to hypoxia were determined after administration of alpha-adrenoceptor antagonists N-methyl chlorpromazine (does not cross the blood-brain barrier), and phenoxybenzamine (crosses the blood-brain barrier). Neither phenoxybenzamine nor N-methyl chlorpromazine affected CBF and microcirculation during normoxia. During hypoxia, they similarly reversed the rostral to caudal gradient of flow, increased utilization of arterioles in rostral brain areas, and did not affect capillaries

  6. Effect of operating conditions in soil aquifer treatment on the removals of pharmaceuticals and personal care products

    Energy Technology Data Exchange (ETDEWEB)

    He, Kai, E-mail: hekai@urban.env.kyoto-u.ac.jp; Echigo, Shinya; Itoh, Sadahiko

    2016-09-15

    Soil aquifer treatment (SAT) is an alternative advanced treatment for wastewater reclamation, and it has the potential to control micropollutants including pharmaceuticals and personal care products (PPCPs). However, the relationship of operating conditions in SAT and removals of micropollutants was not clear. In this study, the effects of operating conditions on the removals of PPCPs were evaluated by using lab-scale columns and plant pilot-scale reactors under different operating conditions. Firstly, weathered granite soil (WGS), standard sand (SAND) and Toyoura standard sand (TS) have different soil characteristics such as total organic carbon (TOC) and cation exchange capacity (CEC). In the columns with these packing materials, the removals of carboxylic analgesics and antilipidemics were effective regardless packing materials. The removals of antibiotics were more effective in WGS than in TS and SAND, indicating high TOC and CEC enhance the sorption in SAT. Secondly, with the extension of hydraulic retention time (HRT), the removals of sulfamethoxazole, acetaminophen, crotamiton, and antipyrine were improved in WGS columns, and adaptable biodegradation for moderately removable PPCPs was formed. Thirdly, the removal efficiencies of sulfamethoxazole and crotamiton were higher in the WGS column under vadose condition than in the WGS column under saturated condition, because of aerobic condition in WGS column under vadose condition. Though long HRT and vadose condition had positive influence on the removals of several PPCPs such as sulfamethoxazole, WGS column with an HRT of 7 days under saturated condition removed most PPCPs. - Highlights: • Soil organic matter and cation exchange capacity enhanced the removals of antibiotics in SAT. • A hydraulic retention time (HRT) of 7 days was sufficient for the removals of most PPCPs. • The removals of most selected PPCPs were similar under vadose and saturated conditions. • Vadose condition contributed to the

  7. Hepatic drug clearance following traumatic injury.

    Science.gov (United States)

    Slaughter, R L; Hassett, J M

    1985-11-01

    Trauma is a complex disease state associated with physiologic changes that have the potential to alter hepatic drug clearance mechanisms. These responses include alterations in hepatic blood flow, reduction in hepatic microsomal activity, reduction in hepatic excretion processes, and changes in protein binding. Hepatic blood flow is influenced by sympathomimetic activity. Both animal and human studies demonstrate an initial reduction and subsequent increase in hepatic blood flow, which coincides with an observed increase and subsequent return to normal in serum catecholamine concentrations. Unfortunately, there are no human studies that address the importance these findings may have to the clearance processes of high intrinsic clearance compounds. Animal studies of trauma indicate that hepatic microsomal activity is depressed during the post-traumatic period. Reduction in the hepatic clearance of antipyrine, a model low intrinsic compound, has also been demonstrated in animal models of trauma. In addition to these effects, hepatic excretion of substances such as indocyanine green and bilirubin have been demonstrated to be impaired in both traumatized animals and humans. Finally, substantial increases in the serum concentration of the binding protein alpha 1-acid glycoprotein occur in trauma patients. This has been reported to be associated with subsequent decreases in the free fraction of lidocaine and quinidine. In addition to changing serum drug concentration/response relationships, the pharmacokinetic behavior of drugs bound to alpha 1-acid glycoprotein should also change. Preliminary observations in our laboratory in a dog model of surgically-induced trauma have shown a reduction in the total clearance of lidocaine and reduction in free lidocaine concentration.(ABSTRACT TRUNCATED AT 250 WORDS)

  8. Influence of frequently used industrial solvents and monomers of plastics on xenobiotic metabolism

    Energy Technology Data Exchange (ETDEWEB)

    Gut, I. (Institut Hygieny a Epidemiologie, Prague (Czechoslovakia))

    1983-11-01

    In male Wistar rats, inhalation of benzene, toluene, or styrene induced a dose-dependent increase of the in vitro hepatic microsomal metabolism of benzene, but toluene metabolism and microsomal cytochrome P-450 level were little affected. In phenobarbital pretreated rats the solvents induced increased biotransformation of benzene metabolism toluene, but relatively less than in controls, and benzene and toluene inhalation actually caused an apparent destruction of cytochrome P-450. In vivo rates of metabolism of toluene and styrene were in good agreement with the in vitro hepatic microsomal biotransformation of benzene or toluene, but benzene metabolism not due to inhibition of benzene metabolism in vivo caused by benzene metabolites. In simultaneously administered two solvents, toluene, styrene or xylene markedly inhibited metabolism of benzene-/sup 14/C, but toluene-/sup 14/C metabolsim was little affected by coadministered benzene, styrene or xylene. Various industrial solvents inhibited metabolism of acrylonitrile along the oxidative pathway leading to thiocyanate, but actually increased the rate of the conjugative pathway beginning with cyanoethylation of glutathion and the final products. Various derivatives of benzene had low inhibiting effect on antipyrine metabolism and clinical significance of such effect is of little significance. Inhibition of benzene metabolism by toluene followed in significantly decreased myelotoxicity of benzene, but the modification of acrylonitrile metabolism and pharmacokinetics by organic solvents given at low doses markedly increased lethal effects of acrylonitrile. The prediction of in vivo rates of metabolism based on the in vitro rates of hepatic microsomal metabolism is therefore possible, provided the inhibiting potency of the xenobiotic and/or its metabolites, self-induction of their metabolism, as well as differences in their pharmacokinetics are considered.

  9. Evaluation of a Silicone Membrane as an Alternative to Human Skin for Determining Skin Permeation Parameters of Chemical Compounds.

    Science.gov (United States)

    Uchida, Takashi; Yakumaru, Masafumi; Nishioka, Keisuke; Higashi, Yoshihiro; Sano, Tomohiko; Todo, Hiroaki; Sugibayashi, Kenji

    2016-01-01

    We evaluated the effectiveness of a silicone membrane as an alternative to human skin using the skin permeation parameters of chemical compounds. An in vitro permeation study using 15 model compounds was conducted, and permeation parameters comprising permeability coefficient (P), diffusion parameter (DL(-2)), and partition parameter (KL) were calculated from each permeation profile. Significant correlations were obtained in log P, log DL(-2), and log KL values between the silicone membrane and human skin. DL(-2) values of model compounds, except flurbiprofen, in the silicone membrane were independent of the lipophilicity of the model compounds and were 100-fold higher than those in human skin. For antipyrine and caffeine, which are hydrophilic, KL values in the silicone membrane were 100-fold lower than those in human skin, and P values, calculated as the product of a DL(-2) and KL, were similar. For lipophilic compounds, such as n-butyl paraben and flurbiprofen, KL values for silicone were similar to or 10-fold higher than those in human skin, and P values for silicone were 100-fold higher than those in human skin. Furthermore, for amphiphilic compounds with log Ko/w values from 0.5 to 3.5, KL values in the silicone membrane were 10-fold lower than those in human skin, and P values for silicone were 10-fold higher than those in human skin. The silicone membrane was useful as a human skin alternative in an in vitro skin permeation study. However, depending on the lipophilicity of the model compounds, some parameters may be over- or underestimated.

  10. Principles of the tracer method in assessing regional blood flow

    International Nuclear Information System (INIS)

    Potchen, E.J.; Siegel, B.; Meidinger, R.

    1972-01-01

    The standard brain scan is abnormal when there is relative increase in blood volume or when there is an abnormal permeability to substances which normally cannot enter the brain tissue. The usual mechanism of abnormal permeability is based upon neovascularity in tissues which do not maintain the tight junctions one sees in the normal brain endothelium. These tight junctions prohibit the leakage of materials from the intra- to extravascular space, and when they are not available many materials can readily transit into the abnormal tissue substance and can therefore be discerned on a standard brain scan. In many instances, however, there is no gross breakdown in this blood-brain barrier, but more subtle derangement may be detected by determining changes in regional brain blood volume or the relative volume of distribution of various labeled materials. We have studied whether or not we can discern differences in brain spaces of two isotopes in experimental situations where the brain scan would be normal. For these models, we have used water-induced brain edema and triethyl-tin-induced brain edema in the experimental animal. In water intoxication, there is no difference in the microvascular anatomy or change in the 99 /sup m/Tc pertechnetate space, but it is apparent from our studies that the brain swells at the expense of brain blood volume and by measuring brain blood volume against brain mass, i.e., transit of 131 I antipyrine versus 51 Cr labeled red cells, one can detect brain edema in a situation where the brain scan would be normal. It is these approaches with cameras and computers using dual energies that may afford a more simplified estimation of altered regional brain function than is now available with the internal carotid injection technique. (U.S.)

  11. Permeability of human placenta and fetal membranes to thyrotropin-stimulating hormone in vitro.

    Science.gov (United States)

    Bajoria, R; Fisk, N M

    1998-05-01

    We determined the placental transfer of TSH in an in vitro model of dually perfused isolated lobule in 28 human term placentas by adding varying concentrations (5-60 microIU mL(-1)) of TSH as a single bolus dose to the closed maternal circulation. Transmembrane transfer of TSH was also studied by adding 45 microIU mL(-1) to the maternal or fetal compartment of a dual chamber of fetal membranes in culture. Passage of freely diffusible markers creatinine and antipyrine were also studied in this model. TSH concentration was measured by third generation chemiluminescence assay with a sensitivity of 10 mIU mL(-1). In the perfusion experiments, at physiologic concentrations the slow decline of TSH in the maternal circulation was associated with a small linear increase in fetal levels to 0.11 +/- 0.04% of initial dose at 2 h. The placental transfer rate was 0.08 microIU min(-1). Increasing maternal concentrations of TSH were associated with proportional increases in transfer rate (y = 0.002x; R2 = 0.99) and placental uptake (y = 0.01x; R2 = 0.97). The placental permeability of TSH was 2.4 x 10(-4) mL min(-1) g(-1) and was proportional to its coefficients of diffusion in water and molecular size. The transmembrane transfer and permeability of TSH was comparable to those of the placenta. We conclude that TSH crosses the human term placenta and fetal membranes sparingly.

  12. Environmental sustainability of the solar photo-Fenton process for wastewater treatment and pharmaceuticals mineralization at semi-industrial scale.

    Science.gov (United States)

    Foteinis, Spyros; Monteagudo, Jose Maria; Durán, Antonio; Chatzisymeon, Efthalia

    2018-01-15

    The environmental sustainability of a semi-industrial solar photo-Fenton reactor, treating real effluents emanating from a pharmaceutical laboratory, is assessed herein. The life cycle assessment/analysis (LCA) methodology was employed and real life cycle inventory (LCI) data was collected from a ferrioxalate-assisted homogeneous solar photo-Fenton wastewater treatment plant (WWTP), at Ciudad Real, Spain. Electricity was provided by photovoltaic (PV) panels in tandem with a battery bank, making the plant autonomous from the local grid. The effective treatment of 1m 3 of secondary-treated pharmaceutical wastewater, containing antipyrine, was used as a functional unit. The main environmental hotspot was identified to be the chemical reagents used to enhance treatment efficiency, mainly hydrogen peroxide (H 2 O 2 ) and to a smaller degree oxalic acid. On the other hand, land use, PV panels, battery units, compound parabolic collectors (CPC), tanks, pipes and pumps, as materials, had a low contribution, ranging from as little as 0.06% up to about 2% on the total CO 2eq emissions. Overall, the solar photo-Fenton process was found to be a sustainable technology for treating wastewater containing micropollutants at semi-industrial level, since the total environmental footprint was found to be 2.71kgCO 2 m -3 or 272mPtm -3 , using IPCC 2013 and ReCiPe impact assessment methods, respectively. A sensitivity analysis revealed that if the excess of solar power is fed back into the grid then the total environmental footprint is reduced. Depending on the amount of solar power fed back into the grid the process could have a near zero total environmental footprint. Copyright © 2017 Elsevier B.V. All rights reserved.

  13. The effect of respiratory disorders on clinical pharmacokinetic variables.

    Science.gov (United States)

    Taburet, A M; Tollier, C; Richard, C

    1990-12-01

    Respiratory disorders induce several pathophysiological changes involving gas exchange and acid-base balance, regional haemodynamics, and alterations of the alveolocapillary membrane. The consequences for the absorption, distribution and elimination of drugs are evaluated. Drug absorption after inhalation is not significantly impaired in patients. With drugs administered by this route, an average of 10% of the dose reaches the lungs. It is not completely clear whether changes in pulmonary endothelium in respiratory failure enhance lung absorption. The effects of changes in blood pH on plasma protein binding and volume of distribution are discussed, but relevant data are not available to explain the distribution changes observed in acutely ill patients. Lung diffusion of some antimicrobial agents is enhanced in patients with pulmonary infections. Decreased cardiac output and hepatic blood flow in patients under mechanical ventilation cause an increase in the plasma concentration of drugs with a high hepatic extraction ratio, such as lidocaine (lignocaine). On a theoretical basis, hypoxia should lead to decreased biotransformation of drugs with a low hepatic extraction ratio, but in vivo data with phenazone (antipyrine) or theophylline are conflicting. The effects of disease on the lung clearance of drugs are discussed but clinically relevant data are lacking. The pharmacokinetics of drugs in patients with asthma or chronic obstructive pulmonary disease are reviewed. Stable asthma and chronic obstructive pulmonary disease do not appear to affect the disposition of theophylline or beta 2-agonists such as salbutamol (albuterol) or terbutaline. Important variations in theophylline pharmacokinetics have been reported in critically ill patients, the causes of which are more likely to be linked to the poor condition of the patients than to a direct effect of hypoxia or hypercapnia. Little is known regarding the pharmacokinetics of cromoglycate, ipratropium, corticoids or

  14. Subcutaneous blood flow in psoriasis

    International Nuclear Information System (INIS)

    Klemp, P.

    1985-01-01

    The simultaneously recorded disappearance rates of 133 xe from subcutaneous adipose tissue in the crus were studied in 10 patients with psoriasis vulgaris using atraumatic labeling of the tissue in lesional skin (LS) areas and symmetrical, nonlesional skin (NLS) areas. Control experiments were performed bilaterally in 10 younger, healthy subjects. The subcutaneous washout rate constant was significantly higher in LS, 0.79 +/- 0.05 min-1 x 10(2) compared to the washout rate constant of NLS, 0.56 +/- 0.07 min-1. 10(2), or the washout rate constant in the normal subjects, 0.46 +/- 0.17 min-1 x 10(2). The mean washout rate constant in NLS was 25% higher than the mean washout rate constant in the normal subjects. The difference was, however, not statistically significant. Differences in the washout rate constants might be due to abnormal subcutaneous tissue-to-blood partition (lambda) in the LS--and therefore not reflecting the real differences in the subcutaneous blood flow (SBF). The lambda for 133 Xe was therefore measured--using a double isotope washout method ( 133 Xe and [ 131 I]antipyrine)--in symmetrical sites of the lateral crus in LS and NLS of 10 patients with psoriasis vulgaris and in 10 legs of normal subjects. In LS the lambda was 4.52 +/- 1.67 ml/g, which was not statistically different from that of NLS, 5.25 +/- 2.19 ml/g, nor from that of normal subcutaneous tissue, 4.98 +/- 1.04 ml/g. Calculations of the SBF using the obtained lambda values gave a significantly higher SBF in LS, 3.57 +/- 0.23 ml/100 g/min, compared to SBF in the NLS, 2.94 +/- 0.37 ml/100 g/min. There was no statistically significant difference between SBF in NLS and SBF in the normal subjects. The increased SBF in LS of psoriatics might be a secondary phenomenon to an increased heat loss in the lesional skin

  15. Late radiation damage in bone, bone marrow and brain vasculature, with particular emphasis upon fractionation models

    International Nuclear Information System (INIS)

    Pitkaenen, Maunu.

    1986-04-01

    X-ray induced changes in rat and human bone and bone marrow vasculature and in rat brain vasculature were measured as a function of time after irradiation and absorbed dose. The absorbed dose in the organ varied from 5 to 25 Gy for single dose irradiations and from 19 to 58 Gy for fractionated irradiations.The number of fractions varied from 3 to 10 for the rats and from 12 to 25 for the human. Blood flow changes were measured using an ''1''2''5I antipyrine or ''8''6RbCl extraction technique. The red blood cell (RBC) volume was examined by ''5''1Cr labelled red cells. Different fractionation models have been compared. Radiation induced reduction of bone and bone marrow blood flow were both time and dose dependent. Reduced blood flow 3 months after irradiation would seem to be an important factor in the subsequent atrophy of bones. With a single dose of 10 Gy the bone marrow blood flow returned to the control level by 7 months after irradiation. In the irradiated bone the RBC volume was about same as that in the control side but in bone marrow the reduction was from 32 to 59%. The dose levels predicted by the nominal standard dose (NSD) formula produced about the same damage to the rat femur seven months after irradiation when the extraction of ''8''6Rb chloride and the dry weight were concerned as the end points. However, the results suggest that the NSB formula underestimates the late radiation damage in bone marrow when a small number of large fractions are used. In the irradiated brains of the rats the blood flow was on average 20.4% higher compared to that in the control group. There was no significant difference in brain blood flow between different fractionation schemes. The value of 0.42 for the exponent of N corresponds to the average value for central nervous system tolerance in the literature. The model used may be sufficiently accurate for clinical work provided the treatment schemes used do not depart too radically from standard practice