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Sample records for antipyrine

  1. Antipyrine clearance during experimental and occupational exposure to toluene

    DEFF Research Database (Denmark)

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

    1983-01-01

    Exposure to toluene vapour enhances hepatic microsomal enzyme function in animals as assessed by the metabolism of the test drug antipyrine. Thirty six printing trade workers with long term occupational exposure to a mixture of organic solvents and 39 matched controls were randomly allocated...... clearance 12 printing trade workers with 17 years (median) of occupational exposure to toluene vapour at concentrations of about 100 ppm were investigated before and four weeks after cessation of exposure. No difference in antipyrine clearance was found either within the groups or between the groups at any...

  2. 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 ...

  3. 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

  4. Solvent extraction studies on the mixed ligand complexes of lanthanides with antipyrine and perchlorate

    International Nuclear Information System (INIS)

    Murthy, M.V.K.; Satyanarayana, D.

    1981-01-01

    Lanthanide ions are found to form colourless mixed-ligand complexes with antipyrine in presence of perchlorate at pH 4.0, and these are quantitatively extractable into nitrobenzene. The composition of the extracted species is shown to be metal:antipyrine:perchlorate = 1:6:3. The variation of the extraction constants with atomic number of the lanthanides is attributed to the 'tetrad effect'. (author)

  5. 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.

  6. Measurement of local cerebral blood flow with Indo (14C) antipyrine. [/sup 131/I, rats, cats

    Energy Technology Data Exchange (ETDEWEB)

    Sakurada, O.; Kennedy, C.; Jehle, J.; Brown, J.D.; Carbin, G.L.; Sokoloff, L.

    1978-01-01

    The autoradiographic diffusible tracer technique for the measurement of local cerebral blood flow was originally designed for use with the radioactive, inert gas /sup 131/I-labeled trifluoroiodomethane and is applicable only with tracers that exhibit unrestricted diffusion through the blood-brain barrier. Because of the technical problems associated with the use of gaseous tracers, a suitable nonvolatile tracer has been sought. (/sup 14/C)-antipyrine has been used previously and found to be unsuitable because of limitations in its diffusion through the blood-brain barrier. An analogue of (/sup 14/C)-antipyrine, iodo-(/sup 14/C)-antipyrine, exhibits higher partition coefficients than (/sup 14/C)-antipyrine between nonpolar solvents and water and might, therefore, be expected to diffuse more freely through the barrier. Its use as the tracer in the local blood flow technique leads to values considerably above those obtained with (/sup 14/C)-antipyrine in the rat and cat and essentially the same as those obtained with the gas trifluoro-(/sup 131/I)-iodomethane in the cat. Iodo-(/sup 14/C)-antipyrine appears, therefore, to be a satisfactory nonvolatile tracer for the measurement of local cerebral blood flow.

  7. 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....

  8. 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....

  9. 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

  10. 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

  11. 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)

  12. 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.

  13. Synthesis, spectral and thermal studies of some lanthanide(III) complexes of 4-[N-(benzalidene) amino] antipyrine thiosemicarbazone

    International Nuclear Information System (INIS)

    Singh, Lakshman; Tyagi, Neelam; Dhaka, Naresh P.; Sindhu, S.K.

    1999-01-01

    A new series of sixteen lanthanide(III) complexes of 4[N-(benzalidene) amino] antipyrine thiosemicarbazone (BAAPTS) with the general composition LnX 3 .n(BAAPTS) (X =Cl - , n = 2; X = NO -3 , n = 1; Ln = La, Pr, Nd, Sm, Gd, Tb, Dy and Ho) have been synthesized and characterized by chemical analysis, conductance, molar weight, magnetic moments measurements, infrared and electronic spectra. The ligand BAAPTS behaves as neutral tridentate (N, N, S) ligand. The probable coordination number is nine in these complexes. (author)

  14. 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.

  15. 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

  16. Antipyrine-Benzocaine Otic

    Science.gov (United States)

    ... to be both safe and effective prior to marketing. Please see the FDA website for more information on unapproved drugs (http://www.fda.gov/AboutFDA/Transparency/Basics/ucm213030.htm) and the approval process (http://www. ...

  17. Study of the electron paramagnetic resonance spectra of Zn(antipyrine){sub 2}(NO{sub 3}){sub 2}:VO{sup 2+}

    Energy Technology Data Exchange (ETDEWEB)

    Xie Linhua, E-mail: xielh1974@163.co [Institute of Solid State Physics, Sichuan Normal University, Chengdu 610066 (China); Zhao Guoping [Institute of Solid State Physics, Sichuan Normal University, Chengdu 610066 (China); State Key Laboratory of Electronic Thin Films and Integrated Devices, University of Electronic Science and Technology of China, Chengdu 610054 (China); Qiu Min [Institute of Solid State Physics, Sichuan Normal University, Chengdu 610066 (China)

    2010-08-15

    In this work, a full ligand-field energy matrix (10x10) diagonalization treatment for 3d{sup 1} ions in tetragonal symmetry is developed on the basis of the two-s.o.-coupling-parameter model. Spin Hamiltonian parameters (g factors g{sub ||}, g{sub perpendicular} and hyperfine structure constants A{sub ||}, A{sub perpendicular}) of the tetragonal V{sup 4+} center in Zn(antipyrine){sub 2}(NO{sub 3}){sub 2} are calculated from the complete energy matrix diagonalization method and the perturbation theory method. The calculated results from both methods are not only close to each other but also in good agreement with the experimental values. Furthermore, the compressed defect structure of V{sup 4+} center is discussed.

  18. Design, synthesis, anti-inflammatory activity and molecular docking of potential novel antipyrine and pyrazolone analogs as cyclooxygenase enzyme (COX) inhibitors.

    Science.gov (United States)

    El Sayed, Mardia T; El-Sharief, Marwa A M Sh; Zarie, Eman S; Morsy, Nesrin M; Elsheakh, Ahmed R; Voronkov, Andrey; Berishvili, Vladimir; Hassan, Ghada S

    2018-03-01

    As a part of a directed program for development of new active agents, novel heterocyclic derivatives with antipyrine and pyrazolone moieties -incorporated in- have been designed and synthesized. Starting with 4-arylidene-3-methyl-1-phenyl-5-pyrazolone derivative 2a,b novel Mannich bases derivatives have been synthesized and biologically evaluated for their anti-inflammatory activity. Furthermore, the activity of such compounds has been tested interestingly as COX-1 and COX-2 inhibitors. Structure elucidation of the synthesized compounds was attained by the use of elemental analysis, IR, 1 H NMR, 13 C NMR, and Mass spectrometry techniques. Compounds 3b, 3d and 4b represent the high % inhibition values for both COX-1 and COX-2. On the other hand, compound 8 showed little selectivity against COX-2 while compound 10 showed good selectivity against COX-1 only. Structure activity relationship has been discussed and the results were confirmed by molecular docking calculations. Copyright © 2018 Elsevier Ltd. All rights reserved.

  19. 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

  20. 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.

  1. Synthesis and characterization of some metal complexes derived from azo compound of 4,4‧-methylenedianiline and antipyrine: Evaluation of their biological activity on some land snail species

    Science.gov (United States)

    AbouEl-Enein, Saeyda A.; Emam, Sanaa M.; Polis, Magdy W.; Emara, Esam M.

    2015-11-01

    A novel series of metal complexes of the azo dye; bis-(1,5-dimethyl-4-[(E)-(3-methylphenyl)diazenyl]-2-phenyl-1,2-dihydro-3H-pyrazol-3-one) derived from 4,4‧-methylenedianiline and antipyrine was synthesized and characterized by different spectral, thermal and analytical methods. The tetradentate ligand reacts with the metal ions as a half unit. All complexes display an octahedral geometry, except Pd(II) complex (7) which has a square planar one. The thermal studies reveal that the complexes have higher thermal stability comparable with that of the free ligand. The activation thermodynamic parameters, such as activation energy (E*), enthalpy of activation (ΔH*), entropy of activation (ΔS*) and Gibbs free energy (ΔG*) have been calculated using DTG curves. The ESR spectra of the solid Cu(II) complexes showed an axial symmetry with 2B1g as a ground state and hyperfine structure. The biological activities of the ligand, as well as its metal complexes have been tested in vitro against two land snail species; Eobania vermiculata and Monacha obstructa. The results show that all the tested compounds have significant biological activities against the two tested land snail species with different sensitivity levels.

  2. 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

  3. Metabolic switching of drug pathways as a consequence of deuterium substitution

    International Nuclear Information System (INIS)

    Horning, M.G.; Haegele, K.D.; Sommer, K.R.; Nowlin, J.; Stafford, M.

    1975-01-01

    An investigation was made of the metabolism of deuterated analogs of caffeine (1-CD 3 -caffeine and 7-CD 3 -caffeine) and antipyrine (N-CD 3 -antipyrine and 3-CD 3 -antipyrine) because both caffeine and antipyrine are metabolized by multiple alternate pathways. Since it is well established that carbon-deuterium bonds are more stable than carbon-hydrogen bonds, it was postulated that oxidation of the CD 3 group would be depressed and that metabolism of the labeled compounds would be shifted to another pathway that did not involve cleavage of a carbon-deuterium bond. Metabolic switching of drug pathways was observed in vivo for both of the caffeine analogs and was observed both in vivo and in vitro for 3-CD 3 -antipyrine

  4. SHORT COMMUNICATION SYNTHESIS AND PRELIMINARY ...

    African Journals Online (AJOL)

    a

    amino]antipyrine semicarbazone. INTRODUCTION. Thiosemicarbazones and their metal complexes have been the subject of extensive investigations because of their potential pharmacological properties and a wide variation in their modes of.

  5. Changes in hepatic microsomal enzyme function in workers exposed to mixtures of chemicals.

    Science.gov (United States)

    Døssing, M

    1982-09-01

    Antipryine clearance was measured during occupational exposure and after an exposure-free interval of 3 wk in 26 spray painters, 44 workers in a herbicide-producing (phenoxyacids) plant, and 10 pesticide-exposed greenhouse gardeners. A control group of 39 workers were investigated simultaneously. A noninvasive simplified antipyrine clearance was used. Antipyrine clearance was greater in pesticide-exposed persons, but it was 15% less in workers exposed to spray paints compared to 3 wk after discontinuation of exposure. Clearance was unchanged in the control group examined at the same interval. Thus, the combined action of different spray paints, grinding dust, and cleaners may inhibit, and phenoxyacids, chlorophenols, and various pesticides may induce, the microsomal enzyme function. The workers had been exposed to the chemicals for years, but the change in antipyrine clearance apparently was reversible.

  6. .sup.18 F-4-Fluoroantipyrine

    Science.gov (United States)

    Shiue, Chyng-Yann; Wolf, Alfred P.

    1984-03-13

    The novel radioactive compound .sup.18 F-4-fluoroantipyrine having high specific activity which can be used in nuclear medicine in diagnostic applications, prepared by the direct fluorination of antipyrine in acetic acid with radioactive fluorine at room temperature and purifying said radioactive compound by means of gel chromatography with ethyl acetate as eluent is disclosed. The non-radioactive 4-fluoroantipyrine can also be prepared by the direct fluorination of antipyrine in acetic acid with molecular fluorine at room temperature and purified by means of gel chromotography with ethyl acetate eluent.

  7. Author Details

    African Journals Online (AJOL)

    Sunil, Atkuru Veera Venkata Naga Krishna. Vol 6, No 1 (2015) - Articles Use of electrophilic coupling reagents, 3-methyl-2-benzothiazolinone hydrazone hydrochloride and 4-amino antipyrine, for the spectrophotometric analysis of vardenafil in tablet dosage forms. Abstract PDF. ISSN: 1821-7613. AJOL African Journals ...

  8. Browse Title Index

    African Journals Online (AJOL)

    Items 51 - 57 of 57 ... ... of electrophilic coupling reagents, 3-methyl-2-benzothiazolinone hydrazone hydrochloride and 4-amino antipyrine, for the spectrophotometric analysis of vardenafil in tablet dosage forms, Abstract PDF. Atkuru Veera Venkata Naga Krishna Sunil, Chandra Bala Sekaran, Tamanampudi Varahala Reddy.

  9. LDH and G-6PDH activities in the ovaries of adult female Wistar rats ...

    African Journals Online (AJOL)

    STORAGESEVER

    2009-04-06

    Apr 6, 2009 ... determination of hydrolysed phenol with amino-antipyrine. J. Clin. Pathol. 7: 322. King J, Jagatheeson KA (1959). A method for the determination of tartrate-labile, prostatic acid phosphatase in serum. J. Clin. Path. 12: 85. Kletzien RF, Harris PK, Foellmi LA (1994). Glucose-6-phosphate dehydrogenase: a ...

  10. formation of toxic nitrosamine as a complication of prostatic ...

    African Journals Online (AJOL)

    Dr Olaleye

    oxytetracycline and amino antipyrine, to form various types of nitroso compounds. The possibility of the interaction, and its attendant toxicity to the liver as a complication in some established cases of urinary tract infection [UTI], was the main focus of the study. This toxicity and its specificity for the liver, as a consequence of ...

  11. CCl4 cirrhosis in rats

    DEFF Research Database (Denmark)

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

    1991-01-01

    measurements were reduced in a differentiated manner. Ranked according to the most pronounced changes they are: capacity of urea-N synthesis (CUNS), galactose elimination capacity (GEC) and antipyrine clearance (APC). Hepatic glutathione concentrations were only slightly decreased after the CCl4 treatment...

  12. 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...

  13. Skin perfusion pressure on the legs measured as the external pressure required for skin reddening after blanching

    DEFF Research Database (Denmark)

    Holstein, P; Nielsen, P.E.; Lund, P

    1980-01-01

    the skin blood flow cessation external pressure (FCEP) was recorded using intra-dermal [131I-]-antipyrine mixed with histamine in estimating the skin blood flow. The external pressure was measured with an airfilled plastic cushion connected to a mercury manometer. Over a wide range of pressures as obtained...

  14. 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

    -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...

  15. 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

    . Placental passage of benzoic acid, caffeine, and glyphosate in an ex vivo human perfusion system. J. Toxicol. Environ. Health, Part A 71, 984-991]. In this work, the transport of these same three compounds, plus the reference compound antipyrine, was investigated using BeWo (b30) cell monolayers. Transport......The placental passage of three compounds with different physicochemical properties was recently investigated in ex vivo human placental perfusion experiments (caffeine, benzoic acid, and glyphosate) [Mose, T., Kjaerstad, M.B., Mathiesen, L., Nielsen, J.B., Edelfors, S., Knudsen, L.E., 2008...... 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...

  16. 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.

  17. 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...

  18. 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...... weight in the age range studied. Glutathione showed an increase of 35% from 8 to 44 weeks of age expressed per g liver. Careful age matching of control animals is important for experimental rat studies....

  19. Riboswitch-Mediated Aptamer Binding for Imaging and Therapy (RABIT): A Novel Technique to Selectively Target an Intracelluar Ligand Specific for Ovarian Cancer

    Science.gov (United States)

    2015-12-01

    solution with PCR using a biotin labeled primer for the reverse strand. The dsDNA PCR products were then attached to streptavidin beads. The DNA strands...Biotinylated DNA containing the complementary docking sequence was attached to streptavidin coated magnetic beads. After incubation of the library and... DNA and RNA aptamers to antipyrine, the 2nd proposed aptamer, and have been working on isolating aptamers to iodoantipyrine. We have also

  20. 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.

  1. 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...

  2. L'absurde dans le théâtre français Dada et présurréaliste

    OpenAIRE

    Kunesova, Mariana

    2014-01-01

    The aim of this doctoral dissertation is to analyze the absurd as an aesthetic category in French Dada and pre-surrealist theatre between 1916 and 1923, dealing with three texts : La Première aventure céleste de Monsieur Antipyrine by Tristan Tzara (1916), S’il vous plaît, by André Breton et Philippe Soupault (written in 1919) and Les Mystères de l’amour by Roger Vitrac (written in 1923).The absurd as a theatre and drama category was examined especially at the half of the last century by the ...

  3. 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

  4. Utility of 4-formylantipyrine in heterocyclic synthesis

    Directory of Open Access Journals (Sweden)

    Abdou O. Abdelhamid

    2010-04-01

    Full Text Available Pyrrolo[3,4-c]pyrazole-4,6(1H,5H-dione, pyrano[2,3-c]pyrazole-5-carbonitrile, pyrano[2,3-d]4-imidazolines, pyrido[2,1-b]benzimidazole, pyrido[2,1-b][1,3]benzoxazole, pyrido[2,1-b][1,3]benzothiazole and pyrido[2,1-b]quinazoline were synthesised from antipyrine derivatives with appropriate reagents such as maleimides, malononitrile, ethyl cyanoacetate, benzimidazole-2-acetonitrile, benzothiazole-2-acetonitrile, benzoxazol-2-acetonitrile, benzoylacetonitrile and other reagents. The newly synthesised compounds were established by elemental analysis, spectral data, and alternative synthetic routes whenever possible.

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

    Energy Technology Data Exchange (ETDEWEB)

    Elo, H.A.; Ylitalo, P.; Kyoettilae, J.; Hervonen, H. (Department of Biomedical Sciences, University of Tampere, Tampere, Finland)

    1982-01-01

    The penetration of different intravenous tracer molecules such as /sup 14/C-labelled 2-methyl-4-chlorophenoxyacetic acid (/sup 14/C-MCPA), /sup 14/C-p-aminobenzoic acid (/sup 14/C-PABA), /sup 14/C-sucrose, /sup 14/C-antipyrine and iodinated (/sup 125/I) human albumin (/sup 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 /sup 14/C-MCPA and /sup 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 /sup 14/C-sucrose, /sup 14/C-antipyrine and /sup 125/I-HA were also increased in the brain and CSF of intoxicated animals, but the increases were less pronounced than those of /sup 14/C-MCPA or /sup 14/C-PABA. The results indicate that MCPA intoxication caused a selective damage of the blood-brain barrier in the brain areas studied.

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

    Energy Technology Data Exchange (ETDEWEB)

    Sakane, T.; Nakatsu, M.; Yamamoto, A.; Hashida, M.; Sezaki, H.; Yamashita, S.; Nadai, T. (Faculty of Pharmaceutical Sciences, Setsunan University, Osaka (Japan))

    1991-06-01

    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.

  7. 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

  8. Drug metabolism and genetic polymorphism in subjects with previous halothane hepatitis

    DEFF Research Database (Denmark)

    Ranek, L; Dalhoff, K; Poulsen, H E

    1993-01-01

    To test the hypothesis that halothane hepatitis is caused by a combination of altered drug metabolism and an immunoallergic disposition, the metabolism of antipyrine, metronidazole, sparteine, phenytoin, and racemic R- and S-mephenytoin was investigated in seven subjects with previous halothane h...... hepatitis do not appear to be different from controls with regard to drug metabolism and HLA tissue type. The possibility of a higher frequency of complement C3 phenotype F and FS needs further investigation....... hepatitis. The HLA tissue types and the complement C3 phenotypes were also determined. The metabolism of antipyrine and metronidazole was within normal range in all subjects, and they were all fast or extensive metabolizers of sparteine, mephenytoin, and phenytoin. HLA tissue types were unremarkable. Five...... of the seven subjects had complement C3 phenotypes F or FS. In the general population phenotype S is the most common, but the difference in complement C3 phenotypes is not statistically significant (p = 0.07). We conclude, although in a limited number of patients, that subjects with previous halothane...

  9. 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.

  10. Preliminary interlaboratory comparison of the ex vivo dual human placental perfusion system

    DEFF Research Database (Denmark)

    Myllynen, Päivi; Mathiesen, Line; Weimer, Marc

    2010-01-01

    )pyridine) and IQ (2-amino-3-methylimidazo(4,5-f)quinoline] has been/will be published separately. For this project, a comparative re-analysis was done, by curve fitting the data and calculating two endpoints: AUC(120), defined as the area under the curve between time 0 and time 120min and as t(0.5), defined...... as the time when the fetal to maternal concentration ratio is expected to be 0.5. The transport of the compounds from maternal to fetal circulation across the perfused placenta could be ranked in the order of antipyrine>IQ>PhIP in terms of both t(0.5) and AUC(120) by both partners. For benzo......(a)pyrene the curve fitting failed. These prevalidation results give confidence for harmonization of the placental perfusion system to be used as one of the test methods in a panel for reproductive toxicology to model placental transfer in humans....

  11. 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.

  12. Clinical trials assessing ototopical agents in the treatment of pain associated with acute otitis media in children.

    Science.gov (United States)

    Wood, Daniel N; Nakas, Nermina; Gregory, Christopher W

    2012-09-01

    Otalgia (ear pain) is one of the characteristic symptoms and best predictor of acute otitis media (AOM) in children. Although oral pain medications are the current mainstay for the treatment of AOM-associated otalgia, ototopical agents have been investigated as an alternative treatment strategy. To permit review and assessment of this treatment modality, a systematic literature search was conducted to identify all randomized, controlled trials of ototopical agents. Four trials were identified, including those examining ototopical benzocaine in combination with antipyrine, lidocaine, tetracaine, and herbal extracts. Although the current available evidence suggests ototopical agents may be safe and effective, we conclude that further studies with more rigorous methodology are needed to conclusively demonstrate their utility in this setting. Copyright © 2012 Elsevier Ireland Ltd. All rights reserved.

  13. 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......Hg no less than nine (82 per cent) suffered severe wound complications. Out of the 48 cases with an SPP above 30 mmHg severe wound complications occurred in only four cases (8 per cent). The difference in wound complication rate is highly significant (P less than 0.01). The postoperative SPP measured...... 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...

  14. 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......Hg no fewer than 9 (82 per cent) suffered wound complications. Out of the 48 cases with an SPP above 30 mmHg severe wound complications occurred in only 4 cases (8 per cent). The difference in wound complication rate is highly significant (P ... ischaemic wound complications in above-knee amputations as has previously been shown to be the case in below-knee amputations....

  15. 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......Hg, no less than six (75 per cent) failed to heal and required reamputation at the above-knee level. Of the 12 cases with an SPP between 20 and 30 mmHg four cases (33 per cent) failed to heal but of the 40 cases with an SPP above 30 mmHg, there were only four cases (10 per cent) which did not heal...... closely to the postoperative clinical course. We conclude that a low SPP can be used to predict ischaemic wound complications, leading to reamputation at a higher level....

  16. Increased cerebral blood flow during hypercapnia is not affected by lesion of the nucleus locus ceruleus

    International Nuclear Information System (INIS)

    Harik, S.I.; Prado, R.; Busto, R.; Ginsberg, M.D.

    1986-01-01

    To test the hypothesis that the putative noradrenergic innervation of intraparenchymal cerebral blood vessels from the nucleus locus ceruleus mediates the vasodilatory response to hypercapnia, regional cerebral blood flow was measured by iodo-[ 14 C]antipyrine autoradiography in awake and restrained rats with unilateral 6-hydroxydopamine lesion of the nucleus locus ceruleus and in unlesioned control rats. Hypercapnia, induced by the inhalation of 5% or 8% CO 2 in air for 8 minutes caused a 2 to 5-fold increase in regional cerebral blood flow. However, despite a marked reduction of about 90% in cortical norepinephrine levels ipsilateral to the lesion, blood flow to the frontal and parietal cortex, hippocampus, striatum and cerebellum increased to the same extent in ipsilateral and contralateral regions. Thus, lesion of the locus ceruleus and the resultant depletion of endogenous cortical and hippocampal norepinephrine, does not influence the cerebrovascular response to hypercapnia

  17. 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.

  18. Skin perfusion pressure measured by isotope washout in legs with arterial occlusive disease. Evaluation of different tracers, comparison to segmental systolic pressure, angiography and transcutaneous oxygen tension and variations during changes in systemic blood pressure

    DEFF Research Database (Denmark)

    Holstein, P; Trap-Jensen, J; Bagger, H

    1983-01-01

    ), 131I- -antipyrine (131I- -a.p.) was compared to Na(131I-) and 99Tcm-pertechnetate (99Tcm). The average SPP by 131I- -a.p. and by 131I- were approximately equal, 57.0 mmHg (range 18-93) compared to 56.3 mmHg (range 13-88) (P greater than 0.1). The average SPP by 99Tcm was just slightly higher, 60.3 mm...... that 99Tcm is as suitable as the 131I- -labelled tracers in estimating the SPP. The SPP is significantly correlated to skin blood flow, to systolic blood pressure, to tc pO2 and to angiographic findings. Correction of SPP for systemic blood pressure changes can be made in proportion with the measured...

  19. 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.

  20. Composition and properties of dirhodanohexaantipyrinelanthanide(3) rhodanides and hexacaprolactamlanthanide(3) halogenhalogenaates

    International Nuclear Information System (INIS)

    Eremin, Yu.G.; Bondarenko, G.I.

    1976-01-01

    Consideration was made of molecular electroconductivity, solubility, infra-red spectra, thermograms and thermograviograms of complexes [Ln(Clm) 6 ][I(I 2 )] 3 , [Ln(Clm) 6 ] [Br(Br 2 )] 3 and [Ln(NCS) 2 (Ant) 6 ]SCN, where Ln=Y, Sm, Yb, La; Clm is caprolactam; Ant is antipyrine. The molecular electroconductivity was termined at 25 deg C in ethanol solutions. The composition of inner spheres of complexes was determined. All complexes containing Clm dissociate in solution to produce four ions. Complexes containing bromobromaates have higher solubility than complexes with iodoiodaates. Complexes with iodoiodaates are somewhat more stable because they begin to decompose at about 200 deg . Corresponding complexes with bromobromaates decompose at about 150 deg

  1. Coordination versatility of N2O4 polydentate hydrazonic ligand in Zn(II, Cu(II, Ni(II, Co(II, Mn(II and Pd(II complexes and antimicrobial evaluation

    Directory of Open Access Journals (Sweden)

    Fathy A. El-Saied

    2017-12-01

    Full Text Available New polydentate hydrazone ligand, was synthesized by the condensation of 1,5-dimethyl-3-oxo-2-phenylpyrazole-4-carbaldehyde with adipodihydrazide. The structure of the synthesized ligand, N′1,N′6-bis((1,5-dimethyl-3-oxo-2-phenyl-2,3-dihydro-1H-pyrazol-4-yl methylene adipohydrazide was elucidated by various analytical and spectroscopic techniques. The reactions of the ligand with zinc(II, copper(II, nickel(II, cobalt(II, manganese(II and palladium(II salts afforded homobinuclear metal complexes. Characterization and structure elucidation of the prepared complexes were achieved using different analytical and spectroscopic techniques. The analyses data indicated that this ligand behaved as N2O4 dibasic hexadentate ligand bonded covalency to the metal ions through the enolic carbonyl oxygen of hydrazide moiety and coordinated via carbonyl oxygen of antipyrine moiety and azomethine nitrogen atoms forming distorted octahedral geometry around the metal ions. The ESR spectra of copper(II complexes (3 and (4 showed an axial symmetry with g||>g⊥>ge, indicating distorted octahedral structure and presence of the unpaired electron in d(x2−y2 orbital. The microbicide studies of the ligand and its metal complexes (2, (3, (4, (5, (8, (11 and (13 showed that, all these complexes exhibit moderate to mild inhibitory effects on B. subtilis, E. coli while complexes (2, (3, (4 and (13 exhibit moderate to mild inhibitory effects on A. niger. Keywords: Hexadentate, Hydrazone, Antipyrine, ESR, Adipohydrazide, Microbicide

  2. The effect of probenecid and MK-571 on the feto-maternal transfer of saquinavir in dually perfused human term placenta.

    Science.gov (United States)

    Rahi, Mea Melissa; Heikkinen, Tuija Maarit; Hakala, Kristo Eerik; Laine, Kari Petri

    2009-07-12

    Human placenta, particularly the blood-placenta barrier, with various transporters has crucial role to protect the fetus and, on the other hand, to facilitate movement of compounds towards the fetal circulation. This study aimed to characterize the role of basal transporters of the syncytiotrophoblast, which appear to be yet less studied, in the fetal-to-maternal transfer of saquinavir by use of dually perfused human placentas. A dual perfusion of human placenta was performed to study effect of MK-571 and probenecid, inhibitors of the MRP1 and OATP transporters, expressed in the basal trophoblast membrane, on the transfer of saquinavir. The fetal-to-maternal placental transfer of saquinavir in the control group as measured by TPT(AUC)% (absolute fraction of the dose crossing placenta) was 14.0%, which is 73% less than the transfer of the freely diffusible antipyrine. The two inhibitors, MK-571 and probenecid caused a non-significant (P = 0.34 for ANOVA) reduction of 43% and 24%, respectively, in the mean amount of saquinavir transferred from the fetal to the maternal side. MK-571 also somewhat (by 31%) reduced the TPT(AUC)% of antipyrine, but this finding did not reach statistical significance (P = 0.25). Neither of the employed inhibitors had an effect on the placental transfer index of saquinavir transfer (P = 0.77). The present results indicated lack of significant effect by MK-571 and probenecid on the fetal-to-maternal transfer of saquinavir and suggest that MRP1 and, possibly, OATP2B1 do not play a significant role in the fetal-to-maternal transfer of saquinavir.

  3. 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.

  4. 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.

  5. 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.

  6. 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.

  7. Characterization of transplacental transfer of paroxetine in perfused human placenta: development of a pharmacokinetic model to evaluate tapered dosing.

    Science.gov (United States)

    Nagai, Marie; Ohtani, Hisakazu; Satoh, Hiroki; Matsuoka, Sayo; Hori, Satoko; Fujii, Tomoyuki; Taketani, Yuji; Sawada, Yasufumi

    2013-12-01

    The aim of this study was to determine whether a tapered dosage regimen of paroxetine in pregnant women might be useful to avoid withdrawal syndromes in neonates after delivery. We characterized the transplacental transfer of paroxetine in perfused human placenta, fitting a pharmacokinetic model to the results and applying the model and parameters to evaluate a tapered dosage regimen. Paroxetine was perfused from the maternal or fetal side of an isolated human placental preparation with various perfusion protocols, and paroxetine concentrations in the effluent and placental tissue were determined. The transplacental pharmacokinetic parameters of paroxetine were estimated by simultaneous fitting of a five-compartment transplacental pharmacokinetic model to the set of paroxetine concentration profiles. The developed model and parameters were used to simulate the maternal and fetal concentrations of paroxetine, and the results were compared with reported data. Paroxetine showed a larger distribution volume in placental tissue and a smaller transplacental transfer as compared with antipyrine, a passive diffusion marker. A five-compartment model could well describe the transplacental transfer of paroxetine and could well simulate the maternal and umbilical venous concentrations of paroxetine at delivery. Transplacental transfer kinetic parameters of paroxetine were estimated by fitting a pharmacokinetic model to perfusion study data. The model and parameters appeared to be suitable for simulation of paroxetine kinetics in fetus. The model was also applicable to design a dosage regimen to avoid an abrupt decrease of paroxetine concentration in fetal plasma.

  8. 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.

  9. 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.

  10. 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.

  11. 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

  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. 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.

  14. 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.

  15. 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.

  16. Bidirectional sodium fluxes across the placenta of conscious sheep.

    Science.gov (United States)

    Weedon, A P; Stacey, T E; Ward, R H; Boyd, R D

    1978-12-01

    Conscious pregnant sheep in the last 3 wk of gestation were studied 1--3 days after surgery. Fetal plasma sodium concentration was significantly lower than maternal. A mean electrical potential difference (PD) of 34 +/- 4 (SE) mV (n = 24) was recorded between maternal and fetal intravascular catheters, the mother being positive with reference to fetus. Unidirectional fetomaternal (Jf leads to m) and maternofetal (Jm leads to f) sodium fluxes were determined by application of Fick's principle to uterine and umbilical circulations following injection of 22NaCl or 24NaCl to fetus or mother, respectively. Blood flows were measured by an antipyrine technique. Jm leads to f = 0.142 +/- 0.029 mmol/min (n = 10); Jf leads to m =0.137 +/- 0.015 mmol/min (n = 21). Jm leads to f increased as a linear function of calculated fetal weight. In seven sheep both Jm leads to f and Jf leads to m were measured in a single experiment. The measured ratio Jm leads to f/Jf leads to m was significantly different from the ratio predicted using Ussing's flux ratio equation. There is probably a transplacental sodium pump active in the direction fetus to mother.

  17. 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.

  18. Interspecies allometric meta-analysis of the comparative pharmacokinetics of 85 drugs across veterinary and laboratory animal species.

    Science.gov (United States)

    Huang, Q; Gehring, R; Tell, L A; Li, M; Riviere, J E

    2015-06-01

    Allometric scaling is widely used for the determination of first dosage regimen and the interpolation or extrapolation of pharmacokinetic parameters across many animal species during drug development. In this article, 85 drugs used in veterinary medicine obtained from the Food Animal Residue Avoidance Databank database were selected for allometric scaling analysis. Outlier species were identified by statistical methods. The results showed that 77% and 88% of drugs displayed significant correlations between total systemic clearance (CL) and volume of distribution at steady status (Vss) vs. body weight (P allometric exponent b for CL and Vss displays approximate normal distribution, with means (0.87 and 0.99) and standard deviations (0.143 and 0.157) for CL and Vss, respectively. Twelve drugs were identified to have at least one outlier species for CL and ten drugs for Vss. The human CL and Vss were predicted for selected drugs by the obtained allometric equations. The predicted CL and Vss were within a threefold error compared to observed values, except the predicted CL values for antipyrine, warfarin and diazepam. The results can be used to estimate cross-species pharmacokinetic profiles for predicting drug dosages in veterinary species, and to identify those species for which interpolation or extrapolation of pharmacokinetics properties may be problematic. © 2014 John Wiley & Sons Ltd.

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

    Energy Technology Data Exchange (ETDEWEB)

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

    1982-01-01

    The tracer kinetics of 4-Fluoro(/sup 18/F)-, 4-Bromo(/sup 82/Br)- and 4-Iodo(/sup 125/I)-antipyrine and /sup 15/O-water were compared in a cat or baboon animal model. First-pass cerebral extraction and clearance with alterations in PaCO/sub 2/ were measured for whole brain. The Renkin/Crone model was used to evaluate brain capillary permeability-surface area product for 4-/sup 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-/sup 18/FAP. 4-Bromoantipyrine labeled with /sup 78/Br (t = 6.5 m) is suggested as a tracer for determination of rCBF with PET.

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

    Energy Technology Data Exchange (ETDEWEB)

    Schroeck, H.K.; Kuschinsky, W. (Univ. of Bonn (Germany, F.R.))

    1989-10-01

    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.

  1. Glucose metabolism in pregnant sheep when placental growth is restricted

    International Nuclear Information System (INIS)

    Owens, J.A.; Falconer, J.; Robinson, J.S.

    1989-01-01

    The effect of restricting placental growth on glucose metabolism in pregnant sheep in late gestation was determined by primed constant infusions of D-[U- 14 C]- and D-[2- 3 H]glucose and antipyrine into fetuses of six control sheep and six sheep from which endometrial caruncles had been removed before pregnancy (caruncle sheep). In the latter, placental and fetal weights were reduced, as was the concentration of glucose in fetal arterial blood. Fetal glucose turnover in caruncle sheep was only 52-59% of that in controls, largely because of lower umbilical loss of glucose back to the placenta (38-39% of control) and lower fetal glucose utilization (61-74% of control). However, fetal glucose utilization on a weight-specific basis was similar in control and caruncle sheep. Significant endogenous glucose production occurred in control and caruncle fetal sheep. Maternal glucose production and partition of glucose between the gravid uterus and other maternal tissues were similar in control and caruncle sheep. In conclusion, when placental and fetal growth are restricted, fetal glucose utilization is maintained by reduced loss of glucose back to the placenta and mother and by maintaining endogenous glucose production

  2. « Destruction de la langue » dans la première œuvre Dada : des impertinences lexicales à la théâtralité

    Directory of Open Access Journals (Sweden)

    Kunešová Mariana

    2015-12-01

    Full Text Available The paper deals with the issue of signification in Dada creation which is well known for its goal of « abolition of logic », and its literary consequence: structures not respecting the speech acts to the point that they seem to destroy the very possibility of presence of acceptable significations. The author of the paper, suggesting to name these rebel structures « motivation attacks », starts her research from the famous interpretation of Dada activity by Jacques Rivière : « It is impossible for a man to say something that has no meaning » (La Nouvelle Revue Française, 1920, and puts out these main questions: What can be the concrete impact of motivation attacks? To which acceptable significations can they lead? Can these have a different form than the one of general connotations of chaos or aggression? The corpus of the research is La Première aventure céleste de Monsieur Antipyrine by Tristan Tzara – the legendary first literary Dada opus, being nevertheless little known itself. The choice of the text is due also to its specific genre: written in a theatrical form, this « collage » is likely to have no other characteristics of scenicity and thus to be theatrically nonoperational. However, the signification, precisely, is a potential means capable of ensuring the attention of the public during the performance. Thus, an analysis of signification should also contribute to clarifying the question of the theatrical potential of La Première aventure.

  3. 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

  4. 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.

  5. 11C-Iodoantipyrine for the measurement of regional cerebral blood flow by positron emission tomography. Validation studies

    Energy Technology Data Exchange (ETDEWEB)

    Ginsberg, M.D.; Lockwood, A.H.; Busto, R.; Finn, R.D.; Campbell, J.A.; Boothe, T.E.

    Positron emission tomography (PET) makes it possible to employ an in vivo autoradiographic paradigm to measure regional cerebral blood flow (rCBF) in man. In this study, we synthesized the positron-emitting radiopharmaceutical 11C-iodoantipyrine (11C-IAP) and validated its suitability as a CBF tracer. 11C ( T and one-half 20.4 min) was produced by the (p,alpha) nuclear reaction on 14N. 11C-methyl iodide was used to methylate 3-methyl-1-phenyl-2-pyrazolin-5-one to form 11C-antipyrine, which was iodinated. Radiochemical purity of the 11C-IAP product was 93-98% except as described below. rCBF was measured with 11C-IAP in nitrous oxide-anesthetized Wistar rats by the method of indicator fractionation, and values were compared with rCBF values measured with simultaneously administered commercially produced 14C-IAP. rCBF was studied over a range of arterial Pco2 values (31-58 mm Hg, mean 43.0 +/- 3.5). Mean rCBF data for the 2 tracers agreed to within 4.8% for cerebral hemispheral samples, 3.8% for cerebellum, and 5.3% for brainstem. Mean values (+/- SEM) for rCBF using 11C-IAP were 1.67 +/- 0.20 ml gm-1 min-1 for cerebral hemispheres; 1.32 +/- 0.17 for cerebellum; and 1.50 +/- 0.21 for brainstem. When chromatographic analysis revealed tracer impurity, rCBF, as measured with 11C-IAP, fell consistently below values obtained with 14C-IAP. The data indicate that 11C-IAP, when properly synthesized and submitted to batch-by-batch quality control, may be suitable for measuring rCBF in man by emission tomography.

  6. Regional cerebral blood flow during hypoxia-ischemia in immature rats

    Energy Technology Data Exchange (ETDEWEB)

    Vannucci, R.C.; Lyons, D.T.; Vasta, F.

    1988-02-01

    Immature rats subjected to a combination of unilateral common carotid artery ligation and hypoxia sustain brain damage confined largely to the ipsilateral cerebral hemisphere. To ascertain the extent and distribution of ischemic alterations in the brains of these small animals, we modified the Sakurada technique to measure regional cerebral blood flow using carbon-14 autoradiography. Seven-day-old rats underwent right common carotid artery ligation following which they were rendered hypoxic with 8% O2 at 37 degrees C. Before and during hypoxia, the rat pups received an injection of iodo(/sup 14/C)antipyrine for determination of regional cerebral blood flow. Blood flows to individual structures of the ipsilateral cerebral hemisphere were not influenced by arterial occlusion alone; flows to the contralateral hemisphere and to the brainstem and cerebellum actually increased by 25-50%. Hypoxia-ischemia was associated with decreases in regional cerebral blood flow of the ipsilateral hemisphere such that by 2 hours, flows to subcortical white matter, neocortex, striatum, and thalamus were 15, 17, 34, and 41% of control, respectively. The hierarchy of the blood flow reductions correlated closely with the distribution and extent of ischemic neuronal necrosis. However, unlike the pathologic pattern of this model, the degree of ischemia appeared homogeneous within each brain region. Blood flows to contralateral cerebral hemispheric structures were relatively unchanged from prehypoxic values, whereas flows to the brainstem and cerebellum nearly doubled and tripled, respectively. Thus, ischemia is the predominant factor that determines the topography of tissue injury to major regions of immature rat brain, whereas metabolic factors may influence the heterogeneous pattern of damage seen within individual structures.

  7. 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.

  8. High-resolution MS and MS(n) investigation of ozone oxidation products from phenazone-type pharmaceuticals and metabolites.

    Science.gov (United States)

    Favier, Maxime; Dewil, Raf; Van Eyck, Kwinten; Van Schepdael, Ann; Cabooter, Deirdre

    2015-10-01

    Phenazone-type pharmaceuticals, such as aminopyrine, metamizole, phenazone and propyphenazone, are widely used analgesics that have been detected in wastewater treatment plant effluents in μg L(-1) concentrations. Acetamido antipyrine (AAA) and formyl aminoantipyrine (FAA) - the main metabolites of aminopyrine and metamizole - have also been detected in sub μg L(-1) concentrations in environmental water bodies and in resources used to produce drinking water, suggesting their highly persistent character. In this study phenazone, propyphenazone, AAA and FAA were treated with ozone under laboratory conditions and 17 degradation products were identified by an elucidation approach based on high-resolution mass spectrometry (LTQ Orbitrap). Typical oxidation of carbon-carbon double bonds by ozone was observed among other mechanisms of ring opening. It was demonstrated that reactivity of these compounds with ozone is high (rate constants kO3 ranging from 6.5×10(4) to 2.4×10(6) M(-1) s(-1)). The toxicity of the degradation products from ozonation was estimated by quantitative structure-activity relationships (QSAR). It was shown that, when the carbon-carbon double bond is partially oxidized to an epoxy, the toxicity towards fish and daphnids is higher than that of the parent compound. By further oxidizing the molecules, a common degradation product - 1-acetyl-1-methyl-2-phenylhydrazide (AMPH) - was also found to be more toxic than its parent compounds, which is of concern since this compound has previously been reported in environmental waters. Copyright © 2015 Elsevier Ltd. All rights reserved.

  9. Validated HPLC method for determination of caffeine level in human plasma using synthetic plasma: application to bioavailability studies.

    Science.gov (United States)

    Alvi, Syed N; Hammami, Muhammad M

    2011-04-01

    Several high-performance liquid chromatography (HPLC) methods have been described for the determination of caffeine in human plasma. However, none have been cross validated using synthetic plasma. The present study describes a simple and reliable HPLC method for the determination of the caffeine level in human plasma. Synthetic plasma was used to construct calibration curves and quality control samples to avoid interference by caffeine commonly present in donor's human plasma. After deproteination of plasma samples with perchloric acid, caffeine and antipyrine (internal standard, IS) were separated on a Waters Atlantis C18 column using a mobile phase of 15 mM potassium phosphate (pH 3.5) and acetonitrile (83:17, v/v), and monitored by photodiode array detector, with the wavelength set at 274 nm. The relationship between caffeine concentrations and peak area ratio (caffeine-IS) was linear over the range of 0.05-20 μg/mL. Inter-run coefficient of variation was ≤ 5.4% and ≤ 6.0% and bias was ≤ 3% and ≤ 7% using human and synthetic plasma, respectively. Mean extraction recovery from human plasma of caffeine and the IS was 91% and 86%, respectively. Caffeine in human plasma was stable for at least 24 h at room temperature or 12 weeks at -20 °C, and after three freeze-thaw cycles. The method was successfully applied to monitor caffeine levels in healthy volunteers with correction of caffeine levels using the mean ratio of the slopes of the calibration's curves constructed using human and synthetic plasma.

  10. Monitoring of 1300 organic micro-pollutants in surface waters from Tianjin, North China.

    Science.gov (United States)

    Kong, Lingxiao; Kadokami, Kiwao; Wang, Shaopo; Duong, Hanh Thi; Chau, Hong Thi Cam

    2015-03-01

    In spite of the quantities and species of chemicals dramatically increased with rapid economic growth in China in the last decade, the focus of environmental research was mainly on limited number of priority pollutants. Therefore, to elucidate environmental pollution by organic micro-pollutants, this work was conducted as the first systematic survey on the occurrence of 1300 substances in 20 surface water samples of Tianjin, North China, selected as a representative area of China. The results showed the presence of 227 chemicals. The most relevant compounds in terms of frequency of detection and median concentration were bis(2-ethylhexyl) phthalate (100%; 0.26μgL(-1)), siduron (100%; 0.20μgL(-1)), lidocaine (100%; 96ngL(-1)), antipyrine (100%; 76ngL(-1)), caffeine (95%; 0.28μgL(-1)), cotinine (95%; 0.20μgL(-1)), phenanthrene (95%; 0.17μgL(-1)), metformin (90%; 0.61μgL(-1)), diethyl phthalate (90%; 0.19μgL(-1)), quinoxaline-2-carboxylic acid (90%; 0.14μgL(-1)), 2-(methylthio)-benzothiazole (85%; 0.11μgL(-1)) and anthraquinone (85%; 54ngL(-1)). Cluster analysis discriminated three highly polluted sites from others based on data similarity. Principle component analysis identified four factors, corresponding to industrial wastewater, domestic discharge, tire production and atmospheric deposition, accounting for 78% of the total variance in the water monitoring data set. This work provides a wide reconnaissance on broad spectrum of organic micro-contaminants in surface waters in China, which indicates that the aquatic environment in China has been polluted by a large number of chemicals. Copyright © 2014 Elsevier Ltd. All rights reserved.

  11. 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.)

  12. Multi-walled carbon nanotubes with selected properties for dynamic filtration of pharmaceuticals and personal care products.

    Science.gov (United States)

    Wang, Yifei; Ma, Jing; Zhu, Jiaxin; Ye, Ning; Zhang, Xiaolei; Huang, Haiou

    2016-04-01

    In this study, multi-walled carbon nanotubes (MWCNT) with selected properties, including pristine MWCNT, hydroxylated MWCNT (H-MWCNT), thin-walled MWCNT with large inner diameter (L-MWCNT), aminated MWCNT, and high-purity MWCNT were investigated for dynamic removal of eight pharmaceuticals and personal care products (PPCP). The removal ratios of different PPCP by the pristine MWCNT followed a decreasing order of triclosan (0.93) > prometryn (0.71) > 4-acetylamino-antipyrine (0.67) > carbendazim (0.65) > caffeine (0.42) > ibuprofen (0.34) > acetaminophen (0.29) at 100 min of filtration. Similar or even higher PPCP removals were obtained for all PPCP as the influent concentration decreased, suggesting potential consistent PPCP removals at environmental PPCP concentrations. The removal ratio of acetaminophen was increased to 0.74 by using H-MWCNT. SRFA (Suwannee River fulvic acid) suppressed PPCP adsorption to MWCNT, to greater extents with increasing SRFA concentrations. The L-MWCNT, despite a large inner diameter of 52 ± 3 nm, did not provide better resistance to the competitive adsorption of SRFA than MWCNT with a small inner diameter of 10 ± 2 nm. Future research will be conducted to minimize the effect of SRFA and facilitate application of MWCNT to the treatment of PPCP-contaminated water. Copyright © 2016 Elsevier Ltd. All rights reserved.

  13. A fundamental study of the impact of pressure on the adsorption mechanism in reversed-phase liquid chromatography.

    Science.gov (United States)

    Åsberg, Dennis; Samuelsson, Jörgen; Fornstedt, Torgny

    2016-07-29

    A fundamental investigation of the pressure effect on individual adsorption sites was undertaken based on adsorption energy distribution and adsorption isotherm measurements. For this purpose, we measured adsorption equilibrium data at pressures ranging from 100 to 1000bar at constant flow and over a wide concentration range for three low-molecular-weight solutes, antipyrine, sodium 2-naphthalenesulfonate, and benzyltriethylammonium chloride, on an Eternity C18 stationary phase. The adsorption energy distribution was bimodal for all solutes, remaining clearly so at all pressures. The bi-Langmuir model best described the adsorption in these systems and two types of adsorption sites were identified, one with a low and another with a high energy of interaction. Evidence exists that the low-energy interactions occur at the interface between the mobile and stationary phases and that the high-energy interactions occur nearer the silica surface, deeper in the C18 layer. The contribution of each type of adsorption site to the retention factor was calculated and the change in solute molar volume from the mobile to stationary phase during the adsorption process was estimated for each type of site. The change in solute molar volume was 2-4 times larger at the high-energy site, likely because of the greater loss of solute solvation layer when penetrating deeper into the C18 layer. The association equilibrium constant increased with increasing pressure while the saturation capacity of the low-energy site remained almost unchanged. The observed increase in saturation capacity for the high-energy site did not affect the column loading capacity, which was almost identical at 50- and 950-bar pressure drops over the column. Copyright © 2016 Elsevier B.V. All rights reserved.

  14. 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

  15. Quantitation of small intestinal permeability during normal human drug absorption

    Science.gov (United States)

    2013-01-01

    Background Understanding the quantitative relationship between a drug’s physical chemical properties and its rate of intestinal absorption (QSAR) is critical for selecting candidate drugs. Because of limited experimental human small intestinal permeability data, approximate surrogates such as the fraction absorbed or Caco-2 permeability are used, both of which have limitations. Methods Given the blood concentration following an oral and intravenous dose, the time course of intestinal absorption in humans was determined by deconvolution and related to the intestinal permeability by the use of a new 3 parameter model function (“Averaged Model” (AM)). The theoretical validity of this AM model was evaluated by comparing it to the standard diffusion-convection model (DC). This analysis was applied to 90 drugs using previously published data. Only drugs that were administered in oral solution form to fasting subjects were considered so that the rate of gastric emptying was approximately known. All the calculations are carried out using the freely available routine PKQuest Java (http://www.pkquest.com) which has an easy to use, simple interface. Results Theoretically, the AM permeability provides an accurate estimate of the intestinal DC permeability for solutes whose absorption ranges from 1% to 99%. The experimental human AM permeabilities determined by deconvolution are similar to those determined by direct human jejunal perfusion. The small intestinal pH varies with position and the results are interpreted in terms of the pH dependent octanol partition. The permeability versus partition relations are presented separately for the uncharged, basic, acidic and charged solutes. The small uncharged solutes caffeine, acetaminophen and antipyrine have very high permeabilities (about 20 x 10-4 cm/sec) corresponding to an unstirred layer of only 45 μm. The weak acid aspirin also has a large AM permeability despite its low octanol partition at pH 7.4, suggesting

  16. 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

  17. Analysis of the photo catalytic degradation of the 4-chloro phenol and endosulfan by gas chromatography; Analisis de la degradacion fotocatalitica del 4-clorofenol y endosulfan por cromatografia de gases

    Energy Technology Data Exchange (ETDEWEB)

    Pichardo S, E. [ININ, 52750 La Marquesa, Estado de Mexico (Mexico)

    2007-07-01

    maximum degradation percentage of 87.87, 62.49, 52.56 and 35.75 to these concentrations and of the same way by ultraviolet-visible, was obtained: 91.6, 61.5, 50.64 and 37.71 degradation percentage respectively, showing that the results correspond in both techniques. As soon as refers to the endosulfan didn't register results of ultraviolet-visible spectroscopy since it was not possible to determine it by the amine 4-antipyrine method. On the other hand, by means of gas chromatography they didn't register results of the quantitative analysis of the endosulfan because they were not observed results during the analysis. An explanation was that the endosulfan was adsorbed in TiO{sub 2} surface, to be able to corroborate this, the samples were analyzed by the Total Organic Carbon technique (COT). At the end of the work it is made an analysis and discussion of the results of the 4-chloro phenol, where the two used control techniques are compared. (Author)