WorldWideScience

Sample records for antipyrine

  1. Antipyrine-Benzocaine Otic

    Science.gov (United States)

    ... benzocaine benzocaine and antipyrine benzocaine, antipyrine, and zinc acetate benzocaine, chloroxylenol, and hydrocortisone chloroxylenol and pramoxine chloroxylenol, pramoxine, and hydrocortisone BACKGROUND: ...

  2. Family study of antipyrine clearance.

    OpenAIRE

    Blain, P G; Mucklow, J C; Wood, P; Roberts, D F; Rawlins, M D

    1982-01-01

    Antipyrine clearance was measured in 208 healthy volunteers from 78 families. After the values had been corrected for weight and sex, antipyrine clearance was observed to be significantly correlated between siblings (r = 0.590) and between spouses (r = 0.320), but not between parents and their offspring. After the clearance values had been corrected for tobacco and oral contraceptive use, there was still no significant correlation between parents and offspring. These results are incompatible ...

  3. Inhibition of antipyrine metabolism by interferon.

    OpenAIRE

    Williams, S.J.; Farrell, G C

    1986-01-01

    Antipyrine clearance was measured before and 1 day after administration of a single intramuscular dose of recombinant human leukocyte alpha A interferon. In the nine patients studied, antipyrine clearance was reduced after interferon from 0.49 (0.21-1.13) ml kg-1 min-1 (median (range)) to 0.41 (0.20-1.07) ml kg-1 min-1, P less than 0.01. In individual patients, the decrement in antipyrine clearance was variable, ranging from 5-47% (median, 16%). This study provides the first direct evidence t...

  4. Reduction of antipyrine clearance in psoriasis.

    OpenAIRE

    Marsden, J R; Williams, F M; Keys, B; Rawlins, M D; Shuster, S

    1984-01-01

    Antipyrine clearance was determined in 41 psoriatics and age-sex matched controls, using sequential measurements of salivary concentration. Antipyrine clearance and elimination rate constant were less in psoriatics (P less than 0.05) and apparent volumes of distribution were similar. These differences were greater between female psoriatics and controls (P less than 0.025; P less than 0.05) and the differences between male psoriatics and controls were not significant. Correlation of simultaneo...

  5. Effect of rifampicin on metoprolol and antipyrine kinetics.

    OpenAIRE

    Bennett, P N; John, V. A.; Whitmarsh, V B

    1982-01-01

    1 Effects of rifampicin on the pharmacokinetics of single oral doses of metoprolol and antipyrine are reported. 2 Rifampicin, administered daily for 15 days, reduced the area under the plasma concentration-time curve (AUC) of metoprolol but the rate constant for elimination (beta) of metoprolol from plasma did not alter significantly. 3 Administration of rifampicin for 13 days reduced AUC and increased beta of antipyrine. Thirteen days after discontinuing rifampicin. AUC and beta of antipyrin...

  6. Antipyrine clearance during occupational exposure to styrene.

    OpenAIRE

    Døssing, M

    1983-01-01

    Animal experiments have indicated that styrene, which is a widely used organic solvent, may induce the microsomal enzyme function of the liver. Thirteen workers with long-term exposure to styrene in a polyester plant were investigated. They worked at air concentrations about the maximal allowed time-weighted average concentration of styrene in most Western countries (50 ppm). The clearance of antipyrine was determined from saliva concentrations before and after three weeks free of exposure an...

  7. 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 into...

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

    International Nuclear Information System (INIS)

    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

  9. Impact of dioxins on antipyrine metabolism in firefighters.

    Science.gov (United States)

    Chernyak, Yury I; Merinova, Alla P; Shelepchikov, Andrey A; Kolesnikov, Sergey I; Grassman, Jean A

    2016-05-27

    Antipyrine (AP) metabolism was used to assess factors associated with the activity of hepatic oxidative enzymes in firefighters. Emphasis was placed on 3-hydroxymethylantipyrine (3HMAP), the metabolite with the greatest dependence on dioxin-inducible cytochrome P4501A2 (CYP1A2) activity. AP urinary metabolites were measured by HPLC in 38 male subjects from Eastern Siberia. Subjects were divided into three groups having similar ages and BMIs: current firefighters (n=11); former firefighters (n=17) and non-firefighters (n=10). Multiple regression models were constructed using the three major AP metabolites as a dependent variable to assess the influence of age, smoking as urinary cotinine concentration, dioxin exposure (as either WHO-TEQ or body burden), group, and CYP1A2*F (-163C>A) genotypes. Models for the proportion of dose excreted as the metabolite 3HMAP produced the best fit (adjusted R(2)=0.46, pfirefighters, only those based on 3HMAP were statistically significant (adjusted R(2) of 0.80 (p<0.002)) due to contributions from urinary cotinine (β=0.56, p<0.01) and dioxin expressed as body burden (β=0.55, p=0.014). These results indicate that the antipyrine test can be used as metabolic probe of biological response to recent dioxin exposure provided the impact of smoking is carefully controlled. PMID:27067104

  10. Effect of antipyrine coadministration on the kinetics of acetaminophen and lidocaine.

    Science.gov (United States)

    Blyden, G T; Greenblatt, D J; LeDuc, B W; Scavone, J M

    1988-01-01

    Pharmacokinetic interactions between antipyrine and acetaminophen were evaluated in 7 healthy volunteers. On 3 occasions subjects received: 1, antipyrine 1.0 g intravenously (i.v.); 2, acetaminophen 650 mg i.v.; 3, antipyrine 1.0 g and acetaminophen 650 mg i.v. simultaneously. Between Trials 1 and 3, antipyrine elimination t1/2 (17.2 vs 17.4 h), clearance (0.44 vs 0.43 ml.min-1.kg-1) and 24-h recovery of antipyrine and metabolites (313 vs 293 mg) did not differ significantly. Between Trials 2 and 3, acetaminophen VZ was reduced (1.14 vs 1.00 l.kg-1), t1/2 prolonged (2.7 vs 3.3 h), clearance reduced (4.8 vs 3.6 ml.min-1.kg-1), and fractional urinary recovery of acetaminophen glucuronide reduced. Eight additional subjects received 50 mg of lidocaine hydrochloride i.v. in the control state, and on a second occasion immediately after antipyrine 1.0 g given i.v. The two trials did not differ significantly in lidocaine VZ (2.6 vs 2.7 l.kg-1), t1/2 (2.0 vs 2.4 h) or clearance (15.0 vs 13.5 ml.min-1.kg-1). Although acetaminophen does not alter antipyrine kinetics, acute administration of antipyrine appears to impair acetaminophen clearance, possibly via inhibition of glucuronide formation. However, antipyrine has no significant effect on the kinetics of a single i.v. dose of lidocaine. PMID:3197750

  11. 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.

  12. Synergism in the extraction of lanthanides, copper and thorium in presence of HTTA and antipyrine

    International Nuclear Information System (INIS)

    Synergism in the extraction of lanthanum, europium, lutetium, copper and thorium has been studied using a mixture of HTTA and 2,3-dimethyl, 1-phenyl pyrazol-5-one (antipyrine). Synergism was observed in all the cases copper. The nature of extracted species has been determined on the basis of log-log plots and the equilibrium constants for the adducts have been evaluated. Antipyrine has been found to be a good donor comparable in strength to other alkylphosphorus donors. (author)

  13. Differential effect of cigarette smoking on antipyrine oxidation versus acetaminophen conjugation.

    Science.gov (United States)

    Scavone, J M; Greenblatt, D J; LeDuc, B W; Blyden, G T; Luna, B G; Harmatz, J S

    1990-01-01

    The effect of cigarette smoking on drug oxidation and conjugation was studied using antipyrine and acetaminophen as marker compounds. For the antipyrine study, healthy cigarette smokers (n = 30) and nonsmoking controls (n = 53) received a single 1.0-gram intravenous dose of antipyrine. For the acetaminophen study, 14 smokers and 15 nonsmokers received a 650-mg intravenous dose of acetaminophen. The clearance of antipyrine was significantly increased (0.93 vs. 0.60 ml/min/kg, p less than 0.0001) and elimination half-life was correspondingly reduced (8.9 vs. 13.0 h, p less than 0.0001) in smokers compared to nonsmoking controls. Total recovery of antipyrine and metabolites excreted in urine did not differ between groups, but there was a significantly increased fractional clearance of antipyrine via formation of 4-hydroxyantipyrine and 3-hydroxymethyl metabolites in smokers. Fractional clearance via formation of norantipyrine did not differ significantly between groups. Comparison of acetaminophen kinetics between smokers and nonsmokers indicated no significant differences in elimination half-life, clearance or volume of distribution. Thus, cigarette smoking is more likely to induce drug oxidation rather than drug conjugation. However, not all oxidative pathways are equally influenced; induction effects of smoking are highly substrate selective and pathway specific. PMID:2345775

  14. 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; Sletting, Susanne; Prip, A; Mølholm Hansen, J

    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....

  15. Antipyrine-gamma cyclodextrin inclusion complex: Molecular modeling, preparation, characterization and cytotoxicity studies

    Science.gov (United States)

    Gannimani, Ramesh; Perumal, Amanda; Ramesh, Muthusamy; Pillay, Karen; Soliman, Mahmoud E.; Govender, Patrick

    2015-06-01

    Molecular docking, semi-empirical and molecular dynamics studies were conducted for α, β and γ-cyclodextrin-associated inclusion complexes of antipyrine. The results of molecular modeling were systematically analyzed to determine the stability of inclusion complexes. In preliminary computational screening, β and γ-cyclodextrin inclusion complexes of antipyrine were found to be more stable as compared to α-cyclodextrin based on docking score and binding free energies. Further, inclusion complex of antipyrine with γ-cyclodextrin was prepared by freeze drying method. Formation of the inclusion complex was investigated by solid state characterization techniques such as thermogravimetric analysis, differential scanning calorimetry, X-ray diffraction, Fourier transform infrared spectroscopy and scanning electron microscopy. The changes observed in decomposition temperature, diffractogram, vibrational frequencies and morphological appearance confirmed the formation of inclusion complex. In addition, results from 1H NMR and 2D NOESY studies supported the inclusion phenomenon. The results obtained from computational studies were found to be in consistent with experimental data to ascertain the encapsulation of antipyrine into γ-cyclodextrin. The inclusion complex was found to be non-toxic toward MDCK-1 cell lines. Thus, this approach may be helpful in the formulation of drug molecules using cyclodextrins.

  16. 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....

  17. Synthesis and Spectral Investigations of Some Platinum Metals Ions Coordination Compounds of 4[N-(Furan-2'-carboxalidene)Amino]Antipyrine Thiosemicarbazone and 4[N-(3',4',5'-Trimethoxybenzalidene)Amino]Antipyrine Thiosemicarbazone

    OpenAIRE

    Ram K. Agarwal; PRASAD, Surendra

    2005-01-01

    The present work describes the synthesis and spectral properties of some platinum metals chlorides coordination compounds of 4[N-(-(furan-2'-carboxalidene)amino]antipyrine thiosemicarbazone (FFAAPTS) and 4[N-(3',4',5'-trimethoxybenzalidene)amino]antipyrine thiosemicarbazone (TMBAAPTS). All the compounds have the general composition MCl2(L) (M = Pd2+ or Pt2+ ; L = FFAAPTS or TMBAAPTS) or MCl3(L) (M = Ru3+ , Rh3+ or Ir3+ ; L = FFAAPTS or TMBAAPTS). All the complexes...

  18. Synthesis and characterization of some oxocation(IV) coordination compounds of Schiff bases derived from 4-amino antipyrine

    Energy Technology Data Exchange (ETDEWEB)

    Agarwal, R.K.; Chakraborti, I. [Dept. of Chemistry, Lajpat Rai College, Sahibabad (India)

    1994-12-31

    The reaction of oxozirconium(IV) chloride with 4[N-2`-nitrobenzalidene) amino] antipyrine (2`-NO{sub 2}BAAP), 4[N-(3`-nitrobenzalidene) amino] antipyrine (3`-NO{sub 2}BAAP), 4[N-(benzalidene) amino] antipyrine thiosemicarbazone (BAAPT), 4[N-dimethyl aminobenzalidene) amino] antipyrine thiosemicarbazone (DABAAPT), 4[N-(4-methoxybenzalidene) amino] antipyrine thiosemicarbazone (MBAAPT) and 4[N-(4-hydroxy-3-methoxybenzalidene) amino] antipyrine thiosemicarbazone (HMBAAPT) and with oxovanadium(IV) salts with BAAPT and DABAAPT resulted in the formation of ZrOCl{sub 2}.2L.H{sub 2}O (L = 2`-NO{sub 2}BAAP, 3`-NO{sub 2}BAP, BAAPT, DABAAPT, MBAAPT or HMBAAPT and VOX{sub 2}.L.nH{sub 2}O (X = Cl,Br,I,NO{sub 3} or NCS, n=0, X=ClO{sub 4}, n=1; L=BAAPT or DABAAPT) respectively. The structure of the complexes were assigned on the basis of elemental analyses, conductivity, molecular weight, magnetic moment, infrared and electronic spectral data. IR spectral data suggest the bidentate nature (N,O) of 2`-NO{sub 2}BAAP and 3`-NO{sub 2}BAAP, while the thiosemicarbazones behave as tridentate. (N,N,S) ligands. The probable coordination number of zirconium is either six eight and vanadium is five. Thermal properties of the compounds have been investigated through thermogravimetric analysis. (author). 43 refs, 6 tabs.

  19. Synthesis and characterization of some oxocation(IV) coordination compounds of Schiff bases derived from 4-amino antipyrine

    International Nuclear Information System (INIS)

    The reaction of oxozirconium(IV) chloride with 4[N-2'-nitrobenzalidene) amino] antipyrine (2'-NO2BAAP), 4[N-(3'-nitrobenzalidene) amino] antipyrine (3'-NO2BAAP), 4[N-(benzalidene) amino] antipyrine thiosemicarbazone (BAAPT), 4[N-dimethyl aminobenzalidene) amino] antipyrine thiosemicarbazone (DABAAPT), 4[N-(4-methoxybenzalidene) amino] antipyrine thiosemicarbazone (MBAAPT) and 4[N-(4-hydroxy-3-methoxybenzalidene) amino] antipyrine thiosemicarbazone (HMBAAPT) and with oxovanadium(IV) salts with BAAPT and DABAAPT resulted in the formation of ZrOCl2.2L.H2O (L = 2'-NO2BAAP, 3'-NO2BAP, BAAPT, DABAAPT, MBAAPT or HMBAAPT and VOX2.L.nH2O (X = Cl,Br,I,NO3 or NCS, n=0, X=ClO4, n=1; L=BAAPT or DABAAPT) respectively. The structure of the complexes were assigned on the basis of elemental analyses, conductivity, molecular weight, magnetic moment, infrared and electronic spectral data. IR spectral data suggest the bidentate nature (N,O) of 2'-NO2BAAP and 3'-NO2BAAP, while the thiosemicarbazones behave as tridentate. (N,N,S) ligands. The probable coordination number of zirconium is either six eight and vanadium is five. Thermal properties of the compounds have been investigated through thermogravimetric analysis. (author). 43 refs, 6 tabs

  20. Discussion of results of investigation into cocrystallization of antipyrine derivatives of some lanthanide iodides from solutions

    International Nuclear Information System (INIS)

    Regularities of component distribution between solid and liqid phases in ternary systems (Ce(AP)6)I3-(Ln(AP6)I3-S (AP-antipyrine; Ln-Nd, Dy; S-water, DMPA) are clarified. It is shown, that cocrystallization of the complexes is considerably affected by the degree of solvent structure ordering (entropy factor), as well as by solubility of incividual compounds

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

    International Nuclear Information System (INIS)

    Thorium (IV) and dioxouranium (VI) complexes of Schiff base 4-[N-(furfural) amino] antipyrine (FFAP) derived from furfural and 4-aminoantipyrine having general composition ThX4.nL (X = Cl-, Br-, NCS-or NO3-, n = 2; x = I- or ClO4-n = 3, L = FFAP) and UO2X2.nL (X Br-, I-, NCS-,NO3- or CH3COO-, n = 2; X = ClO4-n = 3, L = FFAP) have been synthesized and characterized by molecular weight, conductivity, IR spectral and thermoanalytical studies. (author)

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

    DEFF Research Database (Denmark)

    Jelnes, R; Astrup, A

    1985-01-01

    131Iodo-antipyrine (131I-AP) is commonly used for blood flow measurements in adipose tissue. These estimations have been based on the assumption of the tissue-to-blood partition coefficient being 1 ml g-1. No exact determination of the tissue-to-blood partition coefficient for 131I-AP in adipose...

  3. Degradation of antipyrine by UV, UV/H2O2 and UV/PS

    International Nuclear Information System (INIS)

    Highlights: • The antipyrine decomposition exhibited a pseudo-first-order kinetics pattern well. • The kobs with irradiance or oxidant dosage presented a linear relationship well. • The kobs exhibit an exponential trend as a function of [AP]0 for three systems. • UV/H2O2 behaved best at pH 2.5–10, while UV/PS behaved best at pH 10.0–11.5. • Cost for chemicals was firstly taken into account in calculation of the EE/O values. -- Abstract: Degradation of antipyrine (AP) in water by three UV-based photolysis processes (i.e., direct UV, UV/H2O2, UV/persulfate (UV/PS)) was studied. For all the oxidation processes, the AP decomposition exhibited a pseudo-first-order kinetics pattern. Generally, UV/H2O2 and UV/PS significantly improved the degradation rate relevant to UV treatment alone. The pseudo-first-order degradation rate constants (kobs) were, to different degrees, affected by initial AP concentration, oxidant dose, pH, UV irradiation intensity, and co-existing chemicals such as humic acid, chloride, bicarbonate, carbonate and nitrate. The three oxidation processes followed the order in terms of treatment costs: UV/PS > UV > UV/H2O2 if the energy and chemical costs are considered. Finally, the AP degradation pathways in the UV/H2O2 and UV/PS processes are proposed. Results demonstrated that UV/H2O2 and UV/PS are potential alternatives to control water pollution caused by emerging contaminants such as AP

  4. Synthesis of antipyrine/pyridazinone hybrids and investigation of their in vivo analgesic and anti-inflammatory activities

    OpenAIRE

    BAYTAŞ, Sultan; İNCELER, Nazan; MAVANEH, Khatereh Fattahpour

    2012-01-01

    Eleven antipyrine/pyridazinone hybrids were synthesized and evaluated for their in vivo analgesic and anti-inflammatory activities by p-benzoquinone-induced writhing test and carrageenan-induced paw edema model, respectively. The test results indicated that compounds 6a, 6c, and 6d were equally or more potent analgesic and anti-inflammatory agents than aspirin and indomethacin, respectively. Side effects of the compounds were examined on gastric mucosa. Most of the compounds were fou...

  5. Electrical conductivity and dielectric relaxation of 2-(antipyrin-4-ylhydrazono)-2-(4-nitrophenyl)acetonitrile

    International Nuclear Information System (INIS)

    The electrical and dielectric properties of the synthesized 2-(antipyrin-4-ylhydrazono)-2-(4-nitrophenyl)acetonitrile (AHNA) have been studied. The direct and alternating current (DC and AC) conductivities and complex dielectric constant were investigated in temperature range 303–403 K. The AC conductivity and dielectric properties of AHNA were investigated over frequency range 100 Hz–5 MHz. From DC and AC measurements, electrical conduction is found to be a thermally activated process. The frequency-dependent AC conductivity obeys Jonscher's universal power law in which the frequency exponent decreases with increasing temperature. The correlated barrier hopping (CBH) is the predominant model for describing the charge carrier transport in which the electrical parameters are evaluated. The activation energy is found to decrease with increasing frequency. The behaviors of dielectric and dielectric loss are discussed in terms of a polarization mechanism. The dielectric loss shows frequency power law from which the maximum barrier height is determined as 0.19 eV in terms of the Guintini model

  6. Electrical conductivity and dielectric relaxation of 2-(antipyrin-4-ylhydrazono)-2-(4-nitrophenyl)acetonitrile

    Energy Technology Data Exchange (ETDEWEB)

    El-Menyawy, E.M., E-mail: emad_elmenyawy@yahoo.com [Solid State Electronics Laboratory, Solid State Physics Department, Physics Division, National Research Center, Dokki, Cairo 12311 (Egypt); Zedan, I.T. [Basic Science Department, High Institute of Engineering and Technology, El-Arish, North Sinai (Egypt); Nawar, H.H. [Department of Chemistry, Faculty of Education, Al Jabal Al Gharbi University (Libya)

    2014-03-15

    The electrical and dielectric properties of the synthesized 2-(antipyrin-4-ylhydrazono)-2-(4-nitrophenyl)acetonitrile (AHNA) have been studied. The direct and alternating current (DC and AC) conductivities and complex dielectric constant were investigated in temperature range 303–403 K. The AC conductivity and dielectric properties of AHNA were investigated over frequency range 100 Hz–5 MHz. From DC and AC measurements, electrical conduction is found to be a thermally activated process. The frequency-dependent AC conductivity obeys Jonscher's universal power law in which the frequency exponent decreases with increasing temperature. The correlated barrier hopping (CBH) is the predominant model for describing the charge carrier transport in which the electrical parameters are evaluated. The activation energy is found to decrease with increasing frequency. The behaviors of dielectric and dielectric loss are discussed in terms of a polarization mechanism. The dielectric loss shows frequency power law from which the maximum barrier height is determined as 0.19 eV in terms of the Guintini model.

  7. 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.

  8. Organic-solvent-free extraction systems with phase separation based on antipyrine, sulfo salicylic acid, sodium sulphate and water for extraction of metal ions macro amounts

    International Nuclear Information System (INIS)

    It is determined that the aqueous system delamination occurred in the case of pouring of 2 mol/l solutions of antipyrin and sulfo salicylic acid in the molar ratio of 2 : 1. Volume of lower organic phase equal to 3.25 ml depends on the concentration of original components, appending salting-out agent and the medium acidity. The ratio of components antipyrin : sulfo salicylic acid : H2O into organic phase was determined. The optimal conditions for the macro amounts extraction of Fe (III), Ga (III), In (III), and Tl (III) were established. The extraction mechanism and the composition of extracted complexes were suggested. (author)

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

    International Nuclear Information System (INIS)

    A new series of sixteen lanthanide(III) complexes of 4[N-(benzalidene) amino] antipyrine thiosemicarbazone (BAAPTS) with the general composition LnX3.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)

  10. Influencing factors and degradation products of antipyrine chlorination in water with free chlorine

    Institute of Scientific and Technical Information of China (English)

    Meiquan Cai; Liqiu Zhang; Fei Qi; Li Feng

    2013-01-01

    Owing to its low cost,free chlorine is one of the most common disinfectants for wastewater and drinking water treatment.However,the formation of disinfection byproducts has been found to occur after free chlorine disinfection in recent decades.Antipyrine (ANT),an anti-inflammatory analgesic,has been frequently detected in the aquatic environment.In this work.the removal efficiency of ANT by free chlorine oxidation in ultrapure water was investigated with batch experiments.The influencing factors on the removal of ANT were explored at initial concentrations of ANT from 0.04 to 0.64 mg/L,free chlorine dosage from 0.30 to 1.31 mg/L,and pH from 1.5 to 9.0.The main degradation products were identified by solid phase extraction-gas chromatography-mass spectrometry.The results showed that ANT reacted rapidly with free chlorine in ultrapure water systems and up to 90.6% removal efficiency of ANT was achieved after 25 sec (initial free chlorine 1 mg/L,ANT 0.5 mg/L,pH 7.0).Higher oxidant dosage,lower ANT initial concentration and low pH favor the ANT removal.The main degradation product in ANT chlorination was a monochlorine substitution product (4-chloro-l,2-dihydro1,5-dimethyl-2-phenyl-3H-pyrazol-3-one),which can be further chlorinated by free chlorine.In addition,the total organic carbon result indicated that ANT is difficult to be mineralized using chlorine.

  11. Age-related pharmacokinetic changes of acetaminophen, antipyrine, diazepam, diphenhydramine, and ofloxacin in male cynomolgus monkeys and beagle dogs.

    Science.gov (United States)

    Koyanagi, Takashi; Yamaura, Yoshiyuki; Yano, Koji; Kim, Soonih; Yamazaki, Hiroshi

    2014-10-01

    1. The pharmacokinetics of acetaminophen (marker of gastric emptying), antipyrine (marker of hepatic metabolic activity and total body water), diazepam (lipophilic and highly distributed), diphenhydramine (hepatic blood flow-limited and alpha-1 acid glycoprotein bound) and ofloxacin (renally eliminated) were evaluated in cynomolgus monkeys (3-18 years old) and beagle dogs (2-11 years old) as models in elderly persons. 2. Gastric pH fluctuated with aging in monkeys and dogs. The concentration of alpha-1 acid glycoprotein appeared to be increased by aging. There were no age-related differences in the absorption rates of the drugs under the conditions used in the study. Total body fat increased and water decreased in monkeys, but these parameters did not change in dogs. 3. Hepatic blood flow decreased in both species, but a significant decrease of hepatic clearance was only seen in monkeys. Renal clearance decreased significantly with age in monkeys and showed a tendency to decrease in dogs. 4. Age-related alterations of physiological parameters in monkeys are in agreement with clinical observations in humans, except for the lack of a change in the plasma albumin concentration. Therefore, this study suggests that monkey might be a suitable animal model for prediction of age-related changes in pharmacokinetics in humans. PMID:24650193

  12. Synthesis and structural investigations of some five-coordinated oxovanadium(IV) complexes of 4[N-(benzylidene)amino] antipyrine semicarbazone

    International Nuclear Information System (INIS)

    The synthesis and spectral characteristics of a new series of five coordinated oxovanadium(IV) complexes of 4[N-(benzylidene) antipyrine semicarbazone (BAAPS) with general composition VOX2.BAAPS (X=Cl, Br, I, No3 or NCS) and VO(ClO4)2. BAAPS.H2O are reported together with molecular conductivity, molecular weights, magnetic susceptibility, infrared and electronic spectra. In all the complexes, the BAAPS behaves as neutral tridentate (N,N,O) ligand. (author). 12 refs., 3 tabs

  13. 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)

    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

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

    International Nuclear Information System (INIS)

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

  15. Antipyrine-Benzocaine Otic

    Science.gov (United States)

    ... not currently approved by the FDA for safety, effectiveness, and quality. Federal law generally requires that prescription drugs in the U.S. be shown to be both safe and effective prior to marketing. Please see the FDA website for more information on unapproved drugs (http://www. ...

  16. Optical properties and device characteristics of 2-(antipyrin-4-ylhydrazono)-2-(4-nitrophenyl)acetonitrile thin films for photodiode applications

    Science.gov (United States)

    El-Menyawy, E. M.; Zedan, I. T.

    2015-02-01

    2-(Antipyrin-4-ylhydrazono)-2-(4-nitrophenyl)acetonitrile (AHNA) films were deposited via thermal evaporation technique. The optical properties of AHNA films and electrical characteristics of Au/AHNA/n-Si/Au heterojunction diode have been reported. The optical properties of AHNA films were investigated using the spectrophotometric measurements of optical transmittance and reflectance over spectral range 190-2500 nm. The films have indirect allowed optical band gap of 3.6 eV. The refractive index of the films was calculated and the dispersion parameters of the films were determined on the light of the single oscillator model. The electrical properties of Au/AHNA/n-Si/Au heterojunction diode were studied in terms of current-voltage characteristics. The device showed rectification behaviour with a rectification ratio of 100 at ±1 V. The conduction mechanisms and diode parameters such as ideality factor, barrier height and series resistance of the device were determined. The device under illumination showed photovoltaic properties. The short circuit current and open circuit voltage were found to be function of illumination intensity. The device satisfies the conditions to be used as photodiode.

  17. Enhancement effect of p-menthane-3,8-diol on in vitro permeation of antipyrine and indomethacin through Yucatan micropig skin.

    Science.gov (United States)

    Fujii, Makiko; Takeda, Yasuhiro; Yoshida, Minako; Matsumoto, Mitsuo; Watanabe, Yoshiteru

    2004-07-01

    The enhancing effect of p-Menthane-3,8-diol (MDO) on skin permeation of antipyrine (ANP) and indomethacin (IM) through Yucatan micropig skin in vitro was compared with 1-menthol. p-Menthane-3,8-diol is a metabolite of 1-menthol and has little odor. It is easy to combine the vehicle because of lower lipophilicity than 1-menthol. All formulations contained 40% (v/v) ethanol. The permeation of ANP increased with MDO about three times that without enhancer by increasing ANP concentration in the skin. However, the MDO effect was about a quarter that of 1-menthol. The permeation of IM with MDO was about 15 times that with no enhancer and it was almost the same as that with 1-menthol. The lag time of permeation was not significantly changed by MDO, which was not so in the case of 1-menthol. Skin concentration of IM increased about 11 times and six times with MDO and 1-menthol, respectively. MDO and 1-menthol partitioned to the skin relatively high concentrations, 5.9 and 2.5 mg/ cm3, respectively. The solubility of IM in the skin was improved by MDO, and consequently, the permeation of IM was enhanced. PMID:15285341

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

    International Nuclear Information System (INIS)

    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−1·day−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

  19. Single crystal XRD, vibrational spectra, quantum chemical and thermal studies on a new semi-organic crystal: 4-Aminium antipyrine chloride

    Science.gov (United States)

    Chitradevi, A.; Suresh Kumar, S.; Athimoolam, S.; Asath Bahadur, S.; Sridhar, B.

    2015-11-01

    The new semi-organic crystal of 4-aminium antipyrine chloride was grown as a single crystal by slow evaporation solution growth method. The crystal and molecular structure of the grown crystal was determined by single crystal diffraction techniques. The single crystal XRD studies reveal that the phenyl ring and pyrazolone ring of the cation has been inclined at an angle of 52.3 (1)°. The molecular aggregations were stabilized through intricate three dimensional hydrogen bonding network formed by the classical N-H⋯O and N-H⋯Cl hydrogen bonds. The cationic dimer R22(10) motif formed through N-H⋯O intermolecular hydrogen bonds was observed around the inversion center of the unit cell. The amino group from the cation and the chlorine anion was linked through N-H⋯Cl intermolecular hydrogen bond leading to a R24 (8) ring motif. These two ring motifs were extended along the a-axis of the unit cell and forms a hydrophilic layer at z = 0 and 1, which is sandwiched between the hydrophobic layer at z = 1/2. Geometry optimization of the molecules was done by Density Functional Theory (DFT) using the B3LYP function and Hartree-Fock (HF) level with 6-311++G(d,p) basis set. The optimized molecular geometry and computed vibrational spectra were compared with experimental results which show a significant agreement. The natural bond orbital (NBO) analysis was carried out to interpret hyperconjucative interaction and intramolecular charge transfer (ICT). The chemical hardness, electro-negativity and chemical potential of the molecule were carried out by HOMO-LUMO plot. The lower band gap value of the frontier orbitals shows the possible bioactivity of the molecule.

  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. Determination of Antipyrine and Caffeine Contents of Antipyriineand Caffeine Citrate Tablets by HPLC%HPLC法测定米格来宁片中安替比林与咖啡因的含量

    Institute of Scientific and Technical Information of China (English)

    刘震凌; 王佳楠

    2016-01-01

    目的:用HPLC法同时测定米格来宁片中安替比林与咖啡因的含量。方法采用 Waters C18色谱柱;以乙腈-水(20:80)为流动相;检测波长为273 nm。结果安替比林进样量在0.01412~0.70620μg、咖啡因进样量在0.00279~0.13960μg,均与峰面积呈良好的线性关系,安替比林、咖啡因的平均回收率与RSD分别为99.7%、0.6%,100.0%、0.5%(n=9)。结论该方法简便、准确,专属性强,重现性好,可用于该制剂的质量控制。%Objective We measured antipyrine and caffeine content in the Antipyriineand Caffeine Citrate Tablets by HPLC.Methods We used Waters C18 column, and used acetonitrile-water(20:80)as the mobile phase,and the detection wavelength was 273 nm.ResultsThe injection volume of antipyrine was 0.014 12 to 0.706 20 μg, and the injection volume of caffeine was 0.002 79 to 0.139 60 μg. They were associated with the peak area showed a good linear relationship. The antipyrine’s and caffeine’s average recovery and RSD respectively 99.7%,0.6%,100.0%,0.5%(n=9). ConclusionThe method is simple,accurate,specific,reproducible,and can be used for quality control of the preparation.

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

    International Nuclear Information System (INIS)

    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

  3. Structure and bonding of some newly synthesized complexes of lanthanide(III) complexes of 4[N-(p-dimetaylaminobenzalidene) amino] antipyrine thiosemicarbazone

    International Nuclear Information System (INIS)

    A series of complexes of the type LnX3.2(DABAAPTS), where Ln = La, Pr, Nd, Sm, Gd, Tb, Dy and Ho, X = ClO4-, or NCS-, DABAAPTS=4[N- (p-dimethylaminobenzalidene) amino] anti pyrine thiosemicarbazone have been synthesized and characterized on the basis of elemental analysis, molecular weight measurements, molar conductance, room temperature magnetic moment, infrared and electronic spectral data. The ligand DABAAPTS behaves as neutral tridentate (N2S) ligand. (author)

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

    International Nuclear Information System (INIS)

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

  5. Transplacental diffusion and blood flow of gravid bovine uterus

    International Nuclear Information System (INIS)

    Electromagnetic blood flow transducers and uterine arterial, uterine venous, umbilical venous, fetal femoral arterial, and fetal femoral venous catheters were implanted in 11 cows on day 161 +/- 4 of gestation. Antipyrine (0.66 M) plus NaCl (0.16 M) dissolved in deuterium oxide (D2O), or H2O, was infused at a constant rate into the fetal femoral vein catheter. Concentrations of antipyrine and D2O in uterine arterial and venous blood and antipyrine in fetal arterial and umbilical venous blood, as well as middle uterine arterial blood flow (electromagnetic transducer), were determined. Antipyrine and D2O gave similar estimates (steady-state diffusion method) of gravid uterine blood flow. In addition, the slope of the regression of D2O on antipyrine estimates was not different from one. Electromagnetic transducers gave estimates of uterine blood flow that were 32-42% of those obtained with steady-state diffusion but were correlated with estimates obtained by use of both antipyrine and D2O. The transplacental clearance rate of antipyrine was similar (per kg placenta) to that observed in ewes. It was suggested that the maternal and fetal microvasculatures of the bovine placenta could have a concurrent arrangement with vascular shunts or maldistribution of flows, as has been suggested for the ewe

  6. Effect of inhibitors of prostaglandin synthesis on hepatic drug clearance.

    OpenAIRE

    Feely, J; Wood, A. J.

    1983-01-01

    The effect of inhibition of prostaglandin synthesis on the systemic clearance of indocyanine green and antipyrine was studied in seven subjects. Antipyrine clearance was not altered by indomethacin suggesting that oxidative metabolism was not affected. Both aspirin and indomethacin decreased the clearance of indocyanine green presumably by reducing liver blood flow. These results suggest that an effect of inhibitors of prostaglandin synthesis on hepatic drug clearance is likely to be confined...

  7. Thermal decomposition kinetics of samarium (III) isothiocyanate complexes with Schiff base ligands

    International Nuclear Information System (INIS)

    Parameters related to thermal decomposition kinetics, viz., E*, A and ΔS* are computed on the basis of thermal decomposition data of the complexes of samarium (III) isothiocynate with Schiff base ligands, viz., 4-[N-(cinnamalidene) amino] antipyrine (CAAP) and 4-[N(furfural)amino] antipyrine (FFAAP), using three different methods and it was inferred that the values of E* are sufficiently high and positive while values of ΔS* are negative. (author)

  8. Studies on the extraction of vanadium (IV) in the presence of some anions and neutral oxygen donors

    International Nuclear Information System (INIS)

    Extraction of vanadium (IV) in the presence of perchlorate, nitrate, halides, and thiocyanate and neutral oxygen donors like n-butanol, TBP and antipyrine into various solvents is studied. Composition of the extracting species and the stability constants are determined. The effectiveness of the three neutral oxygen donors studied in the extraction of vanadium (IV)-anion system is found to follow the order : antipyrine>TBP>n-bunanol. (author)

  9. The Effects of Acute Infection of Fasciola hepatica on the Metabolism and Pharmacokinetics of Antipyrine in Water Buffaloes%水牛急性实验感染肝片吸虫对安替比林代谢动力学的影响

    Institute of Scientific and Technical Information of China (English)

    江善祥; 毛鑫智; Bayon J E; Gonalez-Gallego J

    2003-01-01

    5头健康雄性去势水牛(2~3岁、体重300~500 kg),经粪便和Dot-ELISA检测确认无肝片吸虫感染.每头水牛一次经口感染1600个肝片吸虫囊蚴,研究急性感染(一次大剂量)肝片吸虫对水牛安替比林代谢动力学影响.用HPLC法测定血浆安替比林(AP)及其代谢物的浓度,分析其动力学参数.每周定时采血测定血清酶水平变化.结果表明:水牛急性感染肝片吸虫后急性期安替比林静脉给药后的动力学参数没有显著变化,在慢性期,血浆消除半衰期T1/2β延长41.42%,总消除率CL下降60.10%,表观分布容积Vdss减小43.61%,平均保留时间MRT上升41.16%,血浆浓度-时间曲线下面积AUC增大150.61%.AP给药后48 h内各代谢物的形成比率及尿清除率与对照期相比在急性期无显著差异,而慢性期极显著降低,AP试验结果与血浆酶水平变化相一致.

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

    Science.gov (United States)

    Mose, T; Mathiesen, L; Karttunen, V; Nielsen, J K S; Sieppi, E; Kummu, M; Mørck, T A; Myöhänen, K; Partanen, H; Vähäkangas, K; Knudsen, L E; Myllynen, P

    2012-05-01

    In the E.U. integrated project NewGeneris, we studied placental transport of thirteen immunotoxic and genotoxic agents in three ex vivo placental perfusion laboratories. In the present publication, all placental perfusion data have been re-analyzed and normalized to make them directly comparable and rankable. Antipyrine transfer data differed significantly between the studies and laboratories, and therefore normalization of data was necessary. An antipyrine normalization factor was introduced making the variance significantly smaller within and between the studies using the same compound but performed in different laboratories. Non-normalized (regular) and normalized data showed a good correlation. The compounds were ranked according to their transplacental transfer rate using either antipyrine normalized AUC120 or transfer index (TI120(%)). Normalization generated a division of compounds in slow, medium and high transfer rate groups. The transfer rate differed slightly depending on the parameter used. However, compounds with passage similar to antipyrine which goes through the placenta by passive diffusion, and good recovery in media (no accumulation in the tissue or adherence to equipment) were highly ranked no matter which parameter was used. Antipyrine normalization resulted in the following ranking order of compounds according to AUC(120NORM) values: NDMA ≥ EtOH ≥ BPA ≥ IQ ≥AA ≥ GA ≥ PCB180 ≥ PhIP ≥ AFB1 > DON ≥ BP ≥ PCB52 ≥ TCDD. As the variance in all parameters within a study decreased after antipyrine normalization, we conclude that this normalization approach at least partially corrects the bias caused by the small methodological differences between studies. PMID:22374511

  11. Synthesis, Spectroscopic and Physicochemical Characterization and Biological Activity of Co(II) and Ni(II) Coordination Compounds with 4-Aminoantipyrine Thiosemicarbazone

    OpenAIRE

    Ram K. Agarwal; Surendra Prasad

    2004-01-01

    We describe the synthesis and characterization of cobalt(II) and nickel(II) coordination compounds of 4[N-(furan-2’-aldimine)amino]antipyrine thiosemicarbazone (FFAAPTS) and 4[N-(4'-nitrobenzalidene) amino]antipyrine thiosemicarbazone (4'-NO2BAAPTS). All the isolated compounds have the general composition MX2(L)(H2O) (M = Co2+ or Ni2+; X = Cl, Br, NO3, NCS or CH3COO; L = FFAAPTS or 4'-NO2BAAPTS) and M(ClO4)2(L)2 (M = Co2+ or Ni2+; L = FFAAPTS or 4'-NO2BAAPTS). Infrared spectral studies i...

  12. Synthesis, Spectral and Thermal Properties of Some Penta-Coordinated Complexes of Oxovanadium(IV) Derived from Thiosemicarbazones of 4-Aminoantipyrine

    OpenAIRE

    Ram K. Agarwal; PRASAD, Surendra; GAHLOT, Neetu

    2004-01-01

    The paper reports the synthesis of crystalline oxovanadium(IV), VO2+, complexes of thiosemicarbazones, i.e. 4[N-(4'-nitrobenzalidene)amino]antipyrine thiosemicarbazone (4'-NO2BAAPTS) and 4[N-(furan-2'-aldimine)amino]antipyrine thiosemicarbazone (FFAAPTS) with general composition VOX2L (X = Cl, Br, I, NO3 or NCS) and VO(ClO4)2(L)H2O (L = 4'-NO2BAAPTS or FFAAPTS). All the complexes were characterized by elemental analyses, molar mass, molar conductance, magnetic susc...

  13. Antipyrene clearance in Indian villagers.

    OpenAIRE

    Desai, N K; Sheth, U K; Mucklow, J C; Fraser, H S; Bulpitt, C J; Jones, S.W.; Dollery, C. T.

    1980-01-01

    1 Antipyrine clearance has been measured using saliva samples in 50 Maharashtrans from a village to the north of Bombay. 2 All subjects were very lean and were also anaemic probably as a result of hookworm infestation. 3 Antipyrine clearance was 36% faster than in White Londoners studied previously and more than twice as fast as in Asian immigrants living in London. 4 Clearance was 25% faster in men than in women but volume of distribution was also greater in men and mean half-lives did not d...

  14. Rate-controlled rectal drug delivery in man with a hydrogel preparation

    NARCIS (Netherlands)

    Leede, de L.G.J.; Boer, de A.G.; Pörtzgen, E.; Feijen, J.; Breimer, D.D.

    1986-01-01

    Cylindrical hydrogels of hydroxyethyl methacrylate (HEMA) and ethylene glycol dimethacrylate (EGDMA) as crosslinking agent were prepared by radical polymerization at 70°C. After washing they were soaked in an aqueous drug solution of antipyrine or theophylline. The in vitro drug release experiments

  15. 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 mmHg no...

  16. 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; Knudsen, Lisbeth E

    2009-01-01

    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....... 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...... 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...

  17. Skin Disposition of Drugs after Topical Application in Hairless Rats

    OpenAIRE

    柳本, 剛; 林, 輝朗; 長谷川, 哲也; 関, 俊暢; 從二, 和彦; 杉林, 堅次; 森本, 雍憲

    1999-01-01

    Drug fraction transported from a topical formulation on skin to subsutaneous tissues or muscles is dependent on the physicochemical properties of the entrapped drug. Cutaneous disposition of model drugs, antipyrine(ANP), lidocaine (LC) and piroxicam (PXC) as well as flurbiprofen (FP) was thus evaluated in hairless rats in which an agar gel disc was subcutaneously inserted into abdominal region as a drug receptor and a drug donor cell was placed above it. Time courses of plasma level and agar ...

  18. Some ozone advanced oxidation processes to improve the biological removal of selected pharmaceutical contaminants from urban wastewater

    OpenAIRE

    Espejo, Azahara; Aguinaco, Almudena; Amat Payá, Ana María; Fernando J. Beltrán

    2014-01-01

    Removal of nine pharmaceutical compounds¿acetaminophen (AAF), antipyrine (ANT), caffeine (CAF), carbamazepine (CRB), diclofenac (DCF), hydrochlorothiazide (HCT), ketorolac (KET), metoprolol (MET) and sulfamethoxazole (SMX)¿spiked in a primary sedimentation effluent of a municipal wastewater has been studied with sequential aerobic biological and ozone advanced oxidation systems. Combinations of ozone, UVA black light and Fe(III) or Fe3O4 constituted the chemical systems. During the ...

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

    DEFF Research Database (Denmark)

    Mose, T; Mathiesen, L; Karttunen, V;

    2012-01-01

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

  20. The Ex Vivo Human Placental Transfer of the Anti-HIV Nucleoside Inhibitor Abacavir and the Protease Inhibitor Amprenavir

    OpenAIRE

    Bawdon, R E

    1998-01-01

    Objective: The transfer of abacavir, a new nucleoside inhibitor, and amprenavir, a new protease inhibitor, used for the treatment of human immunodeficiency virus, has been studied in the ex vivo human placental model.Methods: The ex vivo human placental model used C14 antipyrine to determine the transport fraction and clearance index of these compounds at both the peak and trough serum concentrations. The clearance index accumulation and tissue concentrations were determined for each drug by ...

  1. The ex vivo human placental transfer of the anti-HIV nucleoside inhibitor abacavir and the protease inhibitor amprenavir.

    OpenAIRE

    Bawdon, R E

    1998-01-01

    OBJECTIVE: The transfer of abacavir, a new nucleoside inhibitor, and amprenavir, a new protease inhibitor, used for the treatment of human immunodeficiency virus, has been studied in the ex vivo human placental model. METHODS: The ex vivo human placental model used C14 antipyrine to determine the transport fraction and clearance index of these compounds at both the peak and trough serum concentrations. The clearance index accumulation and tissue concentrations were determined for each drug by...

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

    DEFF Research Database (Denmark)

    Holstein, P

    1980-01-01

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

  3. Adsorption of certain surface-active organic substances on lead, and their effect on hydrogen evolution kinetics in sulfuric acid

    Energy Technology Data Exchange (ETDEWEB)

    Sherstobitova, I.N.; Iskhakov, R.N.

    1988-02-01

    The adsorption of tetrabutylammonium sulfate, n-butyl, n-amyl, isoamyl, n-hexyl alcohol, butyric acid, butylamine, antipyrine and diantipyrylmethane was measured by differential-capacitance at a frequency of 10 kHz at smooth lead electrodes under cathodic polarization. Isotherms were determined by logarithms. Parameters in the Frumkin equation for adsorption of certain organic substances on lead were also determined and tabulated.

  4. 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.

  5. The impact of cocaine and heroin on the placental transfer of methadone

    Directory of Open Access Journals (Sweden)

    Wenzinger Silvana

    2009-06-01

    Full Text Available Abstract Background Methadone is the therapeutic agent of choice for the treatment of opiate addiction in pregnancy. The co-consumption (heroin, cocaine which may influence the effects of methadone is frequent. Therefore, the impact of cocaine and heroin on the placental transfer of methadone and the placental tissue was investigated under in vitro conditions. Methods Placentae (n = 24 were ex-vivo perfused with medium (m (control, n = 6, m plus methadone (n = 6, m plus methadone and cocaine (n = 6 or m plus methadone and heroin (n = 6. Placental functionality parameters like antipyrine permeability, glucose consumption, lactate production, hormone production (hCG and leptin, microparticles release and the expression of P-glycoprotein were analysed. Results Methadone accumulated in placental tissue. Methadone alone decreased the transfer of antipyrine from 0.60 +/- 0.07 to 0.50 +/- 0.06 (fetal/maternal ratio, mean +/- SD, P Conclusion The combination of cocaine or heroin with methadone increase antipyrine permeability. Changes of MPs resemble findings seen in oxidative stress of syncytiotrophoblast.

  6. Application of Osmotic Pumps for Sustained Release of 1-Aminobenzotriazole and Inhibition of Cytochrome P450 Enzymes in Mice: Model Comparison with the Hepatic P450 Reductase Null Mouse.

    Science.gov (United States)

    Stringer, Rowan A; Ferreira, Suzie; Rose, Jonathan; Ronseaux, Sebastien

    2016-08-01

    The effectiveness of controlled release 1-aminobenzotriazole (ABT) administration to inhibit cytochrome P450 (P450) enzymes has been evaluated in mice. To maximize the duration of P450 inhibition in vivo, ABT was administered via an osmotic pump. The degree of P450 inhibition was compared with that achieved with a single bolus dose of ABT. Two-hour prior subcutaneous treatment of mice with ABT (50 mg/kg) inhibited antipyrine clearance by 88%. A less pronounced inhibitory effect (29% reduction in clearance) was observed when ABT was administered 24-hours before antipyrine administration, indicating partial restoration of P450 activity during this longer pretreatment time. The duration of ABT in mice was very short (mean residence time = 1.7 hours) after subcutaneous bolus administration. When the inhibitor was delivered by an osmotic pump, maximum blood concentrations of the inhibitor were observed 24 hours after device implantation and were maintained at steady state for 6 days. Inhibition of P450 activity, as measured by antipyrine clearance, was confirmed at 24 hours and 120 hours after pump implantation, highlighting the utility of this method as a longer-term model for P450 inhibition in mice. The magnitude of P450 inhibition in ABT-treated mice was compared with that in hepatic P450 reductase null mice and both models were comparable. In vivo ABT administration by an osmotic pump offers an effective approach for longer-term P450 inhibition in mice and avoids the necessity for multiple dosing of the inhibitor. PMID:27271368

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

    OpenAIRE

    Brayden, David James; Bzik, V. A.; Lewis, A L; Illum, L.

    2012-01-01

    Purpose CriticalSorb™ is a novel absorption enhancer based on Solutol® HS15, one that has been found to enhance the nasal transport. It is in clinical trials for nasal delivery of human growth hormone. The hypothesis was that permeating enhancement effects of the Solutol®HS15 component would translate to the intestine. Methods Rat colonic mucosae were mounted in Ussing chambers and Papp values of [14C]-mannitol, [14C]-antipyrine, FITC-dextran 4000 (FD-4), and TEER values were calcul...

  8. Quality assessment of a placental perfusion protocol

    DEFF Research Database (Denmark)

    Mathiesen, Line; Mose, Tina; Mørck, Thit Juul;

    2010-01-01

    placental perfusion model in Copenhagen including control substances. The positive control substance antipyrine shows no difference in transport regardless of perfusion media used or of terms of delivery (n=59, p<0.05). Negative control studies with FITC marked dextran correspond with leakage criteria (<3...... ml h(-1) from the fetal reservoir) when adding 2 (n=7) and 20mg (n=9) FITC-dextran/100 ml fetal perfusion media. Success rate of the Copenhagen placental perfusions is provided in this study, including considerations and quality control parameters. Three checkpoints suggested to determine success...

  9. The state and kinetic stability of scandium (3) complex with octaphenyltetraazaporphin in proton-donor media

    International Nuclear Information System (INIS)

    The state of scandium (3) complex with octaphenyltetraazaporphin and acetate (Ac) extraligand in proton-donor media: HOAc-benzene, HOAc-antipyrine-sulfur acid and HOAc-sulfur acid has been studied by the spectrophotometric method. It is shown that in the media with acidity in terms of Hammet H0 = +6.26 - +1.84 ionic associate is formed subject to dissociation at H0 ≥ +1.84. Kinetic stability of the scandium complex in sulfur acid solutions has been studied. Kinetic parameters of solvoprotolytic dissociation of complex have been ascertained, its mechanism being suggested

  10. Synthesis, Spectroscopic and Physicochemical Characterization and Biological Activity of Co(II and Ni(II Coordination Compounds with 4-Aminoantipyrine Thiosemicarbazone

    Directory of Open Access Journals (Sweden)

    Ram K. Agarwal

    2004-01-01

    Full Text Available We describe the synthesis and characterization of cobalt(II and nickel(II coordination compounds of 4[N-(furan-2’-aldimineamino]antipyrine thiosemicarbazone (FFAAPTS and 4[N-(4'-nitrobenzalidene amino]antipyrine thiosemicarbazone (4'-NO2BAAPTS. All the isolated compounds have the general composition MX2(L(H2O (M = Co2+ or Ni2+; X = Cl, Br, NO3, NCS or CH3COO; L = FFAAPTS or 4'-NO2BAAPTS and M(ClO42(L2 (M = Co2+ or Ni2+; L = FFAAPTS or 4'-NO2BAAPTS. Infrared spectral studies indicate that both the thiosemicarbazones coordinate in their neutral form and they act as {N,N,S} tridentate chelating ligands. Room temperature magnetic measurements and electronic spectral studies suggest the distorted octahedral geometries of the prepared complexes. Thermogravimetric studies are also reported and the possible structures of the complexes are proposed. Antibacterial and antifungal properties of these metal-coordination compounds have also been studied.

  11. Late functional changes in the vasculature of the rat brain after local X-irradiation

    International Nuclear Information System (INIS)

    The brains of young adult rats were irradiated with doses of 500 to 4000 rad. At intervals of 3 to 15 months after irradiation regional changes in the functional vasculature were investigated using the iodoantipyrine extraction technique. Modifications in vascular function were restricted to animals locally irradiated with doses of 2000 and 3000 rad. The first change was observed three months after irradiation and was characterized by a reduction in antipyrine extraction in the mid-brain and brain stem of animals irradiated with 2000 rad. At six and nine months after exposure to both 2000 and 3000 rad significant increases in antipyrine extraction were found in the four brain regions examined, although the effect was greatest in the mid-brain. These results are compared and contrasted with functional changes reported in other normal tissues; the link between these functional changes in the brain vasculature and the appearance of gross vascular lesions after a latent period of one year is discussed. It is suggested that the increase in iodoantipyrine extraction represents a regulatory reaction by the vasculature of the brain to tissue hypoxia and that focal vascular lesions in the brain occur as a consequence of the failure of this reaction to hypoxia. (author)

  12. Proteolytic enzyme conjugated to SC-glucan as an enzymatic transdermal drug penetration enhancer.

    Science.gov (United States)

    Sim, Y C; Nam, Y S; Shin, Y H; Shin, E; Kim, S; Chang, I S; Rhee, J S

    2003-04-01

    The objective of this study was to investigate the effect of papain, a proteolytic enzyme, on the percutaneous absorption of drugs. To guarantee the enzyme stability during the skin penetration, papain was modified by the conjugation to SC-glucan. The enhancing activity of drug penetration was evaluated using antipyrine and indomethacin as hydrophilic and hydrophobic model drugs, respectively. The SC-glucan-papain conjugate was found to be very effective for facilitating the percutaneous absorption of antipyrine. Microscopic observations showed that the thickness of stratum corneum and viable epidermis was increased by the treatment of the SC-glucan-papain conjugate. Moreover, it induced phase separation, lacuna formation, and lamellar disruption within the stratum corneum interstices. These structural changes by the SC-glucan-papain conjugate are likely to be induced from hydrolysis of extensive crosslinking of corneocyte envelopes and intracellular proteins. However, the SC-glucan-papain conjugate showed no skin irritation according to the Draize test, which may be due to the difficulty of the SC-glucan-papain conjugate in penetrating into the skin. PMID:12749407

  13. Maternal-fetal transfer of indocyanine green across the perfused human placenta.

    Science.gov (United States)

    Rubinchik-Stern, Miriam; Shmuel, Miriam; Bar, Jacob; Eyal, Sara; Kovo, Michal

    2016-07-01

    Indocyanine green (ICG) is an FDA-approved near-infrared imaging probe, given also to pregnant women. We aimed to characterize ICG's transplacental transfer using the ex-vivo perfusion model. Placentas were obtained from caesarean deliveries. Cotyledons were cannulated and dually perfused. ICG, 9.6μg/mL and antipyrine (50μg/mL) were added to the maternal circulation in the absence (n=4) or the presence of the organic anion transporting polypeptide (OATPs) inhibitor rifampin (10μg/mL; n=5) or the P-glycoprotein inhibitor valspodar (2μg/mL; n=3). ICG's maternal-to-fetal transfer was evaluated over 180min. The cumulative percent of ICG in the fetal reservoir was minor. When ICG transfer was normalized to that of antipyrine, it was lower in the presence of rifampin (a 41% decrease; p<0.05). Valspodar did not appear to modify the kinetics of ICG. ICG's transplacental transfer is minimal and is probably OATP-mediated. The placenta is an effective protective barrier to ICG's distribution into the fetus. PMID:27132189

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

    International Nuclear Information System (INIS)

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

  15. Inductive effects of rifapentine on mice hepatic mixed function oxidase system.

    Science.gov (United States)

    Liu, D Y; Wang, Y S

    1990-03-01

    Rifapentine (R773, DL473) is a long-acting antituberculous drug used in China. In our experiments we have found some manifestations of induction of hepatic mixed function oxidase system in mice following pretreatment with rifapentine or phenobarbital. Both rifapentine and phenobarbital significantly increased the rate of antipyrine and pentobarbital metabolism in vivo. They also increased liver weight, the content of liver microsomal protein and cytochrome P-450, the activity of NADPH-cytochrome C reductase and NADPH oxidase. SDS-polyacylamide gel electrophoresis showed that the relative proportions of some polypeptide bands in mice microsomal fraction were significantly changed following rifapentine or phenobarbital pretreatment. The results indicate that rifapentine, like phenobarbital, is a potent inducer of hepatic mixed function oxidase system in mice and that it should be used carefully in clinical therapy, when combined with other drugs. PMID:2319833

  16. Could quantitative liver function tests gain wide acceptance among hepatologists?

    Institute of Scientific and Technical Information of China (English)

    Giovanni Tarantino

    2009-01-01

    It has been emphasized that the assessment of residual liver function is of paramount importance to determine the following: severity of acute or chronic liver diseases independent of etiology; long-term prognosis; step-bystep disease progression; surgical risk; and efficacy of antiviral treatment. The most frequently used tools are the galactose elimination capacity to asses hepatocyte cytosol activity, plasma clearance of indocyanine green to assess excretory function, and antipyrine clearance to estimate microsomal activity. However, a widely accepted liver test (not necessarily a laboratory one) to assess quantitative functional hepatic reserve still needs to be established, although there have been various proposals. Furthermore, who are the operators that should order these tests? Advances in analytic methods are expected to allow quantitative liver function tests to be used in clinical practice.

  17. 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....

  18. 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.

  19. 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.

  20. Intramolecular proton transfer through the adjoining π-conjugated system in Shiff base: Application for colorimetric sensing of fluoride anion

    Energy Technology Data Exchange (ETDEWEB)

    Yu, Xudong, E-mail: 081022009@fudan.edu.cn [College of Chemistry and Material Sciences, Hebei Normal University, Yuhua Road 113, Shijiazhuang 050024 (China); College of Science and Hebei Research Center of Pharmaceutical and Chemical Engineering, Hebei University of Science and Technology, Yuhua Road 70, Shijiazhuang 050080 (China); Zhang, Ping [College of Chemistry and Material Sciences, Hebei Normal University, Yuhua Road 113, Shijiazhuang 050024 (China); Li, Yajuan; Zhen, Xiaoli; Geng, Lijun; Wang, Yanqiu [College of Science and Hebei Research Center of Pharmaceutical and Chemical Engineering, Hebei University of Science and Technology, Yuhua Road 70, Shijiazhuang 050080 (China); Ma, Zichuan, E-mail: ma7405@hebtu.edu.cn [College of Chemistry and Material Sciences, Hebei Normal University, Yuhua Road 113, Shijiazhuang 050024 (China)

    2014-07-01

    In this paper, a new kind of phenol-based chemsensor L2 comprised of a Schiff base and azo groups was rationally designed and synthesized. It could selectively recognize fluoride anion among tested anions such as F{sup −}, AcO{sup −}, H{sub 2}PO{sub 4}{sup −}, Cl{sup −}, Br{sup −}, and I{sup −} with obvious color changes from yellow to fuchsia. The intramolecular PT (proton transfer) in L1 and L2 was responsible for the sensing ability, which was certified by the {sup 1}H NMR and Uv–vis experiments. - Highlights: • The phenol derivative L2 could selectively sense F{sup −} among test anions. • Intramolecular proton transfer happened when L2 was bonded with F{sup −}. • It is the first antipyrine-based anion receptor.

  1. Efficient and Convenient Route for the Synthesis of Some New Antipyrinyl Monoazo Dyes: Application to Polyester Fibers and Biological Evaluation

    Directory of Open Access Journals (Sweden)

    Ahmed A. Fadda

    2013-01-01

    Full Text Available Nine variously substituted azo dye derivatives 2–10 of antipyrine were prepared. The effects of the nature and orientation of the substituents on the color and dyeing properties of these dyes for polyester fibers were evaluated. The newly synthesized compounds were characterized on the basis of elemental analyses and spectral data. On the other hand, the investigated dyes were applied to polyester fabrics and showed good light, washing, heat, and acid perspiration fastness. The remarkable degree of brightness after washings is indicative of the good penetration and the excellent affinity of these dyes for the fabric. The results in general revealed the efficiency of the prepared compounds as new monoazo disperse dyes. The newly synthesized compounds were screened for their antioxidant and cytotoxic activity against Vitamin C and 5-fluorouracil, respectively. The data showed clearly that most of the compounds exhibited good antioxidant and cytotoxic activities.

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

    International Nuclear Information System (INIS)

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

  3. Investigation into the hypersensitive transitions of Ln(III)-(1-phenyl-3-methyl-4-benzoyl pyrazolone-5) anthranilic acid and (1-phenyl-3-methyl-4-benzoyl-pyrazolone-5) aminoantipyrine complexes-II

    International Nuclear Information System (INIS)

    (1-phenyl-3-methy1-4-benzoyl pyrazolone-5) anthranilic acid (PMBAA) and (1-phenyl-3-methyl-4-benzoyl-pyrazolone-5) amino-antipyrine (PMBAAP) form complexes with lanthanides of the type [Ln(PMBAA)2NO3] and (Ln(PMBAAP)3] where Ln = La, Pr, Nd, Sm, Eu, Gd, Tb, Dy and Y. These compounds have been characterized from physico-chemical studies. The electronic spectra of the Nd(III) complexes have been studied in detail to investigate the phenomenon of hypersensitivity with respect to the coordination environment and solvent medium. In these compounds solvents do play a significant role to cause variation in hypersensitivity. In general Nd(III) PMBAA complexes showed greater hypersensitivity than the Nd(III) PMBAAP complexes. IR and NMR have also been interpreted. (author). 13 refs., 4 tabs

  4. Acute hypoxia and cytochrome P450-mediated hepatic drug metabolism in humans

    DEFF Research Database (Denmark)

    Jürgens, Gesche; Christensen, Hanne Rolighed; Brøsen, Kim; Sonne, Jesper; Loft, Steffen; Olsen, Niels Vidiendal

    2002-01-01

    measured before departure, at 24 and 96 hours after arrival to high-altitude location, and at 1 month after return to sea level. CYP enzyme activities were measured by means of the metabolic ratios of sparteine (CYP2D6), endogenous cortisol metabolism (CYP3A4), and caffeine (CYP1A2), as well as by the S......% confidence interval, 1.0 to 4.2; P =.047, Friedman test). These changes indicate a small decrease in the activity of CYP2D6 and CYP3A4. There were no significant changes regarding the metabolic ratio of caffeine, the S/R ratio of mephenytoin, or antipyrine clearance. CONCLUSION: The small changes observed...

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

    Directory of Open Access Journals (Sweden)

    Sérgio Luiz Dalmora

    2008-01-01

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

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

    International Nuclear Information System (INIS)

    The tracer kinetics of 4-Fluoro(18F)-, 4-Bromo(82Br)- and 4-Iodo(125I)-antipyrine and 15O-water were compared in a cat or baboon animal model. First-pass cerebral extraction and clearance with alterations in PaCO2 were measured for whole brain. The Renkin/Crone model was used to evaluate brain capillary permeability-surface area product for 4-18FAP 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 4-18FAP. 4-Bromoantipyrine labeled with 78Br (t = 6.5 m) is suggested as a tracer for determination of rCBF with PET

  7. 1,5-Dimethyl-2-phenyl-1H-pyrazol-3(2H-one–4,4′-(propane-2,2-diylbis[1,5-dimethyl-2-phenyl-1H-pyrazol-3(2H-one] (1/1

    Directory of Open Access Journals (Sweden)

    Krzysztof Lyczko

    2013-01-01

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

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

    International Nuclear Information System (INIS)

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

  9. 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. PMID:26084545

  10. Fetoplacental deamination and decarboxylation of leucine

    International Nuclear Information System (INIS)

    Fetal and placental metabolism of leucine (Leu) and ketoisocaproic acid (KIC) were studied in seven fetal lambs at 132 +/- 1.3-days gestation. Fetal infusions of [1-13C]Leu, [1-14C]Leu, and antipyrine were carried out for 4 h. Uterine and umbilical blood flows were measured using the antipyrine steady-state diffusion technique. Leu and KIC concentrations, [14C]Leu-specific activities, 14CO2, [13C]Leu, and [13C]KIC enrichment (mole percent enrichment) were measured in the maternal artery, uterine vein, and umbilical artery and vein to calculate net fluxes of tracee and tracer molecules between fetus and placenta and between the uteroplacenta and the maternal circulation. There were net Leu and KIC fluxes into the fetus from the placenta with the KIC flux equal to approximately 19% of the combined Leu plus KIC flux. In addition, there was a net KIC flux into the uterine circulation. The fraction of infused tracer Leu escaping the placenta into the mother was small (approximately 6%). By contrast, there was a rapid exchange of tracer Leu carbon between placenta and fetus resulting in a significant flux of labeled KIC from placenta to fetus. Approximately 20% of the infused tracer carbon was converted to CO2 within the fetus. This rate of conversion was greater than 80% of the total fetoplacental conversion rate and significantly higher than the flux of KIC tracer carbon from placenta to fetus. Fetal KIC decarboxylation rate, calculated from the fetal KIC enrichment data, was 2.83 +/- 0.40 mumol.min-1.kg fetus-1 and approximately 60% of the combined net Leu and KIC flux into the fetus from the placenta

  11. Synthesis and Spectroscopic Property of Acridinium-9-sulfonamides%新型吖啶-9-磺酰胺衍生物的合成及光谱学性质

    Institute of Scientific and Technical Information of China (English)

    穆小静; 肖尚友; 王建超; 吴彦蕾; 夏之宁

    2009-01-01

    By introducing an electro-withdrawing antipyrine group, N-(p-toluenesulfonyl)-N-(4-antipyrine)-10-methylacridinium-9-carboxamide triflate was prepared. The UV, FL and CL properties of the target compound and of its precursor were investigated by comparing with those of the model compound N-(p-toluenesulfonyl)-N-phenyl-10-methylacridinium-9-carboxamide triflate and the corresponding precursor respectively. The results show that acridine sulfonamide with a heterocyclic antipyrine group exhibits blue shift of both UV absorption and of maximum excitation wavelength(λex) and emission wavelength(λem) in FL spectra, comparing with the corresponding model compound. The λex of the final target and its precursor are 268 and 274 nm, respectively; and the λem are 321 and 327 nm, respectively, while λex of the model compound and its unmethylated precursor are 365 and 359 nm, respectively; and the λem are 504 and 440 nm, respectively. Moreover, the chemiluminescence of the final target compound triggered by H2O2 could finish within 1.1 s; and the quantum yield is similar to that of the model compound, being 5.6 times high as that of luminol.%在吖啶磺酰胺分子中引入杂环安替比林吸电性基团,合成了N-对甲基苯磺酰基-N-(4-安替比林)-10-甲基吖啶-9-磺酰胺三氟甲基磺酸鎓盐.最终产物与未甲基化的前体分别与模型化合物N-对甲基苯磺酰基-N-苯基-10-甲基吖啶-9-酰胺三氟甲基磺酸鎓盐及其前体的紫外-可见吸收光谱(UV)、荧光光谱(FL)进行比较.结果表明,引入杂环安替比林使吖啶磺酰胺的UV和FL谱发生了变化,尤其是FL谱的最大激发与发射峰的位置比相应的模型化合物大幅蓝移.最终产物及其前体的最大λex分别为268和274 nm; λem分别为321和327 nm.而模型化合物及前体最大λex分别为365和359 nm; λem分别为504和440 nm.H2O2引发的目标产物的化学发光(CL)在1.1 s完成;化学发光量子产率与模型化合物相

  12. Autoradiographic determination of regional cerebral blood flow and metabolism in conscious rats after fluid resuscitation from haemorrhage with a haemoglobin-based oxygen carrier.

    Science.gov (United States)

    Waschke, K F; Albrecht, D M; van Ackern, K; Kuschinsky, W

    1994-10-01

    The effects of resuscitation fluids on the brain have been investigated in previous studies by global measurements of cerebral blood flow and metabolism. In this study we have examined the effects of a novel haemoglobin-based oxygen carrier on local cerebral blood flow (LCBF) and local cerebral glucose utilization (LCGU) after resuscitation from a volume-controlled haemorrhage of 30 min (3.0 ml/100 g body weight) with ultrapurified, polymerized, bovine haemoglobin (UPBHB). LCBF and LCGU were measured in 34 brain structures of conscious rats 2 h after resuscitation using quantitative iodo(14C)antipyrine and 2-(14C)-deoxy-D-glucose methods. The data were compared with a control group without haemorrhage and fluid resuscitation. In the haemorrhage group, LCBF increased after resuscitation by 12-56% in the different brain structures (mean 36%). LCGU changed less (0 to +18%, mean +9%). In the control group there was a close relationship between LCGU and LCBF (r = 0.95). After fluid resuscitation the relationship was preserved (r = 0.95), although it was reset at a higher ratio of LCBF to LCGU (P < 0.05). We conclude that fluid resuscitation of a 30 min volume-controlled haemorrhage using the haemoglobin-based oxygen carrier, UPBHB, induced a moderate degree of heterogeneity in the resulting changes of LCGU and LCBF. Local disturbances of cerebral blood flow or metabolism were not observed. PMID:7999496

  13. Extraction-spectrophotometric study of ternary ion-association complexes of vanadium (4) with pyrogallol and tetrazolium salts

    International Nuclear Information System (INIS)

    The systems V(4)-pyrogallol-neotetrazolium chloride and V(4)-pyrogallo-iodonitrotetrazolium chloride are studied using spectrophotometric methods. The composition of the complexes is established. Obtained results reveal that the ternary ion-association complexes are easily extracted by butanol. The optimum conditions for extraction of vanadium into n-butanol are found. Distribution constants, recovery factors, association constants and molar absorptivities ε are calculated. Molar absorptivity of the ternary complex with 2-(4-iodophenyl)-3-(4-nitrophenyl)-tetrazolium chloride (ε=8.74·103 l/mol·cm) is higher as compared to that of the complex with 2,2';5,5'-tetraphenyl-3,3'-(p-biphenyl)-ditetrazolium chloride (ε=7.30·103 l/mol·cm) and to molar absorptivities of the ternary complexes with antipyrine (ε=4.2·103 l/mol·cm) and diphenylguanidine (ε=8.0·103 l/mol·cm)

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

    International Nuclear Information System (INIS)

    The effect of restricting placental growth on glucose metabolism in pregnant sheep in late gestation was determined by primed constant infusions of D-[U-14C]- and D-[2-3H]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

  15. 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.

  16. Macrolide antibacterials. Drug interactions of clinical significance.

    Science.gov (United States)

    von Rosensteil, N A; Adam, D

    1995-08-01

    Macrolide antibiotics can interact adversely with commonly used drugs, usually by altering metabolism due to complex formation and inhibition of cytochrome P-450 IIIA4 (CYP3A4) in the liver and enterocytes. In addition, pharmacokinetic drug interactions with macrolides can result from their antibiotic effect on microorganisms of the enteric flora, and through enhanced gastric emptying due to a motilin-like effect. Macrolides may be classified into 3 different groups according to their affinity for CYP3A4, and thus their propensity to cause pharmacokinetic drug interactions. Troleandomycin, erythromycin and its prodrugs decrease drug metabolism and may produce drug interactions (group 1). Others, including clarithromycin, flurithromycin, midecamycin, midecamycin acetate (miocamycin; ponsinomycin), josamycin and roxithromycin (group 2) rarely cause interactions. Azithromycin, dirithromycin, rikamycin and spiramycin (group 3) do not inactivate CYP3A4 and do not engender these adverse effects. Drug interactions with carbamazepine, cyclosporin, terfenadine, astemizole and theophylline represent the most frequently encountered interactions with macrolide antibiotics. If the combination of a macrolide and one of these compounds cannot be avoided, serum concentrations of concurrently administered drugs should be monitored and patients observed for signs of toxicity. Rare interactions and those of dubious clinical importance are those with alfentanil and sufentanil, antacids and cimetidine, oral anticoagulants, bromocriptine, clozapine, oral contraceptive steroids, digoxin, disopyramide, ergot alkaloids, felodipine, glibenclamide (glyburide), levodopa/carbidopa, lovastatin, methylprednisolone, phenazone (antipyrine), phenytoin, rifabutin and rifampicin (rifampin), triazolam and midazolam, valproic acid (sodium valproate) and zidovudine. PMID:7576262

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

    International Nuclear Information System (INIS)

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

  18. Pulmonary uptake of morphine (M)

    International Nuclear Information System (INIS)

    Previously the authors reported less than 5% of M was taken up during the first pass through the human lung. The low uptake of this basic lipophilic amine was further investigated in a single pass isolated perfused rat lung (IPL) in comparison to uptake of radiolabelled H2O, antipyrine (A), aminopyrine (AM), nicotine (N) and phenylethylamine (P). The IPL was perfused for 5 min with each drug (5nmol/ml) and effluent collected in 10 sec fractions. Pulmonary extraction was calculated using indocyanine green dye as a non-extractable reference indicator. Accumulation of all compounds in the IPL reached an apparent equilibrium within 4 min. At equilibrium lung/perfusate conc. ratios for H2O, A, AM, N, P and M were 1.04, 0.84, 0.85, 1.44, 2.57 and 1.13 respectively. The time course of M uptake differed from the other compounds since initial extraction of M was low (23%) compared to 75%, 53%, 35%, 82% and 86% for H2O, A, AM, N and P respectively. Also, the half time to equilibrium for M was longer (50 sec) compared to 18, 21, 26, 19 and 22 sec for H2O, A, AM, N and P respectively. The low initial pulmonary extraction of M compared to these compounds followed by greater M extraction during the remainder of drug infusion suggests uptake mechanisms for M different than the flow limited uptake for water and other basic amine drugs

  19. 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; Gyntelberg, F; Poulsen, H L

    1980-01-01

    The skin perfusion on the calf was measured photo-electrically and by isotope washout technique using external counter pressure by a blood pressure cuff. By the photocell the skin blanching threshold external pressure (BTEP) was recorded on histamine flared red skin. By isotope washout technique...... 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......Hg (range 18-187) compared to 80.8 mmHg (range 18-158) (P > 0.1). A normal material was obtained from twenty-four subjects measured on the thigh, calf and ankle; the average gradients between the auscultatory brachial mean blood pressure and the BTEP were: thigh 10.7 mmHg (SD 12.7); calf 4.0 mmHg (SD 12...

  20. Studies of transformer repair workers exposed to PCBs. II. Results of clinical laboratory investigations

    Energy Technology Data Exchange (ETDEWEB)

    Emmett, E.A.; Maroni, M.; Jefferys, J.; Schmith, J.; Levin, B.K.; Alvares, A.

    1988-01-01

    Thirty-eight transformer repairmen currently exposed to polychlorinated biphenyls (PCBs), 17 former transformer repairmen, and 56 comparison workers not known to be exposed to PCBs were studied. Measurements were made of serum liver function tests, gamma-glutamyl transpeptidase (GGT), lipid profile, thyroid function tests, and other serum biochemistry; hemoglobin; white cell count; 24-hour excretion of delta-aminolevulinic acid, porphyrins, 17-hydroxycorticosteriods and 17-ketosteroids; sperm count; spirometry; and antipyrine half-life to evaluate microsomal mixed function oxidase induction. The total exposed group differed significantly from the comparison group in albumin, LDH, T4, T4-RT3 index, and actual/predicted FEV1. Significant differences among all three exposure groups were seen for albumin, T4, T4-RT3 index, and 17-hydroxycorticosteroid excretion. Differences in FEV1 were attributable to smoking. Significant correlations between serum PCBs and serum lipids were removed by adjustment for confounding variables. After adjustment for confounding variables, there was a statistically significant positive correlation between serum PCBs and GGT and a negative correlation between adipose PCBs and 17-hydroxycorticosteroid excretion. These may reflect subtle metabolic effects of PCBs.

  1. Extraction of scandium by benzoylantipyrine from chloride-perchlorate solutions

    International Nuclear Information System (INIS)

    Distribution of scandium complexes in case of extraction by benzoyl-4-antipyrine (BANT) in chloroform from aqueous chloride-perchlorate solutions, depending on extraction, perchlorate-ion and salting out agents concentration, was studied. It has been ascertained that scandium distribution factor is nearly 50 at NaClO4 and BANT concentrations equal to 2 and 0.1 mol/l respectively. Introduction of salting out agents (NaCl, CaCl2) and HCl at a constant content of NaClO4 (0.5 mol/l) increases noticeably scandium extraction. For 0.1 mol/l BANT solution in chloroform the extraction capacity in terms of scandium makes up 1.26 g/l. The optimal conditions for the element extraction have been found, the composition of the complex extracted has been ascertained (Sc:BANT:ClO4- = 1:3:3) and extraction mechanism has been suggested. Influence of interfering elements on scandium distribution factor was studied

  2. [Oral exposure testing in non-aspirin-induced analgesic intolerance].

    Science.gov (United States)

    Wiedow, O; Brasch, J; Christophers, E

    1996-12-01

    Although intolerance reaction to analgesics are not uncommon, there is still a lack of standardized procedures to diagnose the problem. We retrospectively analyzed results of scratch tests as well as oral challenges with analgesics in order to evaluate risk and diagnostic relevance of these procedures. In 1987-1992 a total of 650 patients with supposed intolerance to drugs were tested by oral challenge. Among them were 98 patients with a positive history of intolerance to non-aspirin analgesics. In 56 patients the intolerance could be verified by oral challenge. In order of decreasing frequency, the most likely agents were propyphenazone, diclofenac, metamizole, ibuprofen, carbamazepine, indomethacin, phenazone (antipyrine), and paracetamol (acteaminophen). Oral provocation showed clear dose-response relationships. For propyphenazone, the half-effective provocation dose was the same for all symptoms (cutaneous, nasal, bronchial, anaphylactoid). Scratch testing was not of diagnostic significance. Standardized test protocols starting with low dose oral challenges are suitable and helpful in minimizing the risk of severe side effects. PMID:9081936

  3. Photonuclear method of production Cu-67

    International Nuclear Information System (INIS)

    The efficiently separation of 67Cu is achieved by using diantipyrylpropylmethane (DAPPM). Experimental separation of 67Cu from sulphuric solution (1 mol./L) of zinc (2 mol./L) with addition potassium iodide (0.1 mol./L) is realized with help DAPPM (0.02 mol./L), which dissolve in chloroform. The 84.4% 67Cu was extracted from water phase of ZnSO4 into organic phase (solution DAPPM in chloroform). The 67Cu remainder in organic phase is 4.6%. Effective extraction of protonated forms of reagent and ionic associate of metal+halide was realized by means of antipyrin forms in acid halide solution. The decrease of acidity of a water phase is necessary for effective re-extraction. Re-extraction was realised by means of consecutive washing of organic phase (DAPPM in chloroform) by means of distilled water. Some amount of ZnSO4 in process of extraction gets in organic phase that causes a low level re-extraction in first two tests. These tests re-extraction have low values pH. Re-extraction 67Cu from solution DAPPM in chloroform is carried out consistently four times by distilled water. The activity of 67Cu in third and fourth re-extraction tests was 72.7%.

  4. 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.

  5. Toxicokinetics of the food-toxin IQ in human placental perfusion is not affected by ABCG2 or xenobiotic metabolism

    DEFF Research Database (Denmark)

    Immonen, E; Kummu, M; Petsalo, A;

    2010-01-01

    M, n = 6) or Ko143 (specific inhibitor of ABCG2, 2 muM, n = 4) to study the role of ABCG2 inhibition in transfer while in Denmark perfusions were performed with (14)C-IQ alone. Critical parameters (leak from fetal to maternal circulation, pH values, blood gases, glucose consumption, the production of h......CG hormone and transport of antipyrine) were analyzed during the perfusions. (14)C-IQ on maternal and fetal sides was determined by liquid scintillation counting. In Finland IQ and its metabolites in final perfusates were determined also by LC/TOF-MS. ABCG2 expression and EROD activity (CYP1A1/2) were...... analyzed from perfused tissues. (14)C-IQ was easily transferred through the placenta from maternal to fetal side in both laboratories. Neither significant EROD activity nor IQ metabolites were found in placentas from non-smoking mothers. Inhibition of ABCG2 by GF120918 (FM-ratio of IQ 0.95) or Ko143 (FM...

  6. Functional Role of P-Glycoprotein and Binding Protein Effect on the Placental Transfer of Lopinavir/Ritonavir in the Ex Vivo Human Perfusion Model

    Directory of Open Access Journals (Sweden)

    Pierre-Francois Ceccaldi

    2009-01-01

    Methods. Cotyledons were perfused with lopinavir, ritonavir, and the internal control antipyrin, at various albumin concentrations (10, 30, 40 g/L. After the control phase of each experiment, the P-glycoprotein inhibitor ciclosporin A was added at middle perfusion (45 minutes. Fetal Transfer Rate (FTR and Clearance Index (CLI were compared between the 2 phases. Results. In the control phase, the clearance index of lopinavir decreased from 0.401 ± 0.058 to 0.007 ± 0.027, as albumin concentrations increased from 10 g/L to higher concentrations (30, 40 g/L. When adding ciclosporin A at physiological albumin concentrations, the clearance index of lopinavir increased significantly 10.3 fold (95% of CI difference [−0.156, −0.002], P=.046 and became positive for ritonavir. Conclusions. Even at high albumin concentrations, inhibition of placental P-glycoprotein increased placental transfer of lopinavir, suggesting that this efflux pump actively reduces placental transfer of the drug. This mechanism may play a role in fetal exposure to maternal antiretroviral therapy.

  7. 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 mmHg, 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. The...... difference in failure rate is highly significant (P less than 0.01). Four out of 30 diabetic patients required reamputation as against 10 out of 30 non-diabetics (0.05 less than P less than 0.10). The average SPP was higher in the diabetic group: 57 mmHg (range 18-93 mmHg) compared with 34 mmHg (range 8...

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

    International Nuclear Information System (INIS)

    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 132I--or 125I--antipyrine mixed with histamine. Out of the 11 cases with an SPP below 30 mmHg 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<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 previously been shown to be the case in below-knee amputations. (author)

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

    International Nuclear Information System (INIS)

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

  10. 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. PMID:26845455

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

    Science.gov (United States)

    He, Kai; 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 7days under saturated condition removed most PPCPs. PMID:27213846

  12. Effect of borneol on the transdermal permeation of drugs with differing lipophilicity and molecular organization of stratum corneum lipids.

    Science.gov (United States)

    Yi, Qi-Feng; Yan, Jin; Tang, Si-Yuan; Huang, Hui; Kang, Li-Yang

    2016-07-01

    The aim of the present paper was to investigate the promoting activity of borneol on the transdermal permeation of drugs with differing lipophilicity, and probe its alterations in molecular organization of stratum corneum (SC) lipids. The toxicity of borneol was evaluated in epidermal keratinocyte HaCaT and dermal fibroblast CCC-HSF-1 cell cultures and compared to known enhancers, and its irritant profile was also assessed by transepidermal water loss (TEWL) evaluation. The promoting effect of borneol on the transdermal permeation of five model drugs, namely 5-fluorouracil, antipyrine, aspirin, salicylic acid and ibuprofen, which were selected based on their lipophilicity denoted by logp value, were performed using in vitro skin permeation studies. Attenuated total reflection-Fourier transform infrared spectroscopy (ATR-FTIR) was employed to monitor the borneol-induced alteration in molecular organization of SC lipids. The enhancer borneol displayed lower cytotoxicity or irritation in comparison to the well-established and standard enhancer Azone. Borneol could effectively promote the transdermal permeation of five model drugs, and its enhancement ratios were found to be parabolic curve with the logp values of drugs, which exhibited the optimum permeation activity for relatively hydrophilic drugs (an estimated logp value of -0.5 ∼0.5). The molecular mechanism studies suggested that borneol could perturb the structure of SC lipid alkyl chains, and extract part of SC lipids, resulting in the alteration in the skin permeability barrier. PMID:26635061

  13. Phenylpyrazolone derivatives inhibit gastric emptying in rats by a capsaicin-sensitive afferent pathway

    Directory of Open Access Journals (Sweden)

    A.M. Vinagre

    2009-11-01

    Full Text Available Dipyrone (Dp, 4-aminoantipyrine (AA and antipyrine (At administered iv and Dp administered icv delay gastric emptying (GE in rats. The participation of capsaicin (Cps-sensitive afferent fibers in this phenomenon was evaluated. Male Wistar rats were pretreated sc with Cps (50 mg/kg or vehicle between the first and second day of life and both groups were submitted to the eye-wiping test. GE was determined in these animals at the age of 8/9 weeks (weight: 200-300 g. Ten minutes before the study, the animals of both groups were treated iv with Dp, AA or At (240 μmol/kg, or saline; or treated icv with Dp (4 μmol/animal or saline. GE was determined 10 min after treatment by measuring % gastric retention (GR of saline labeled with phenol red 10 min after orogastric administration. Percent GR (mean ± SEM, N = 8 in animals pretreated with Cps and treated with Dp, AA or At (35.8 ± 3.2, 35.4 ± 2.2, and 35.6 ± 2%, respectively did not differ from the GR of saline-treated animals pretreated with vehicle (36.8 ± 2.8% and was significantly lower than in animals pretreated with vehicle and treated with the drugs (52.1 ± 2.8, 66.2 ± 4, and 55.8 ± 3%, respectively. The effect of icv administration of Dp (N = 6 was not modified by pretreatment with Cps (63.3 ± 5.7% compared to Dp-treated animals pretreated with vehicle (62.3 ± 2.4%. The results suggest the participation of capsaicin-sensitive afferent fibers in the delayed GE induced by iv administration of Dp, AA and At, but not of icv Dp.

  14. Influence of diet and nutritional status on drug metabolism.

    Science.gov (United States)

    Walter-Sack, I; Klotz, U

    1996-07-01

    Genetic and environmental factors contribute to a wide inter- and intraindividual variability in drug metabolism. Among the environmental factors that may influence drug metabolism, the diet and nutritional status of the individuals are important determinants. As altered drug-metabolising enzyme activities can influence the intensity and duration of drug action, such factors should be considered in pharmacotherapy. For this reason the effects of dietary energy, protein deficiency, nutritional ingredients, special diet forms and nutrition regimens and malnutritional states must be differentiated. In various pharmacokinetic studies different model drugs metabolised either by oxidative phase I pathways [e.g. phenazone (antipyrine), aminopyrine, phenacetin, theophylline, propranolol, nifedipine] or phase II conjugation reactions [e.g. paracetamol (acetaminophen), oxazepam] were used and from the calculated pharmacokinetic data some information on the involved and affected drug-metabolising enzymes [e.g. cytochrome P450 (CYP) subspecies, glucuronosyltransferases] can be generated. It is well known that smoking, charcoal broiled food or cruciferous vegetables induce the metabolism of many xenobiotics, whereas grapefruit juice increases the oral bioavailability of the high clearance drugs nifedipine, nitrendipine or felodipine by inhibiting their presystemic (intestinal) elimination. Energy deficiency, and especially a low intake of protein, will cause a decrease of about 20 to 40% in phenazone and theophylline clearance and elimination of those drugs can be accelerated by a protein-rich diet. In the same way, protein deficiency induced by either vegetarian food or undernourishment will have the opposite pharmacokinetic consequences. On the basis of some more examples from the literature it is emphasised that the variable influence of the above factors should be taken into account in study participant selection and study design when the pharmacokinetics of a drug must be

  15. Labelling of some amino acids with radioiodine

    International Nuclear Information System (INIS)

    Some radioiodine labelled compounds which have application in nuclear medicine have been prepared. Two common techniques were employed. A comparative study on the radioiodination of the amino acids, L - tyrosine, L - a - methyl tyrosine and L-tyrosine methyl ester has been carried out by the electrophilic radioiodination technique. The blood flow reagent, antipyrine, also has been prepared by this technique using chloramine - T, iodogen and H2 O2 as oxidizing agents to generate electrophilic iodine. Radio chromatograms revealed side product impurities at long reaction times and high oxidizing agent concentrations. Comparison between the different oxidizing agents was done. Optimization of the radioiodination conditions, such as Ph of the medium, reaction time, oxidizing agent and substrate concentrations and carrier KI concentration was performed resulting in high radiochemical yields of 97% L - 3 -(131) iodotyrosine, 95% L -3-(131) iodo-a-methyl tyrosine, 88% L-3-(131) iodotyrosine methyl ester and 96% 4-(131) iodoantipyrine within short reaction times at room temperature when chloramine - T was used as oxidizing agent. Purification by high pressure liquid chromatography resulted in high radiochemically pure products suitable for medical application. Radioiodinated 3- iodotyrosine and 4- iodophenyl alanine have been prepared by the isotopic exchange technique using cuprous chloride as catalyst for the exchange reaction. The effect of solvents and the different parameters affecting the labelling yield were investigated to optimize the conditions for labelling of these compounds. Kinetic study indicated a second order reaction with an activation energy of 9.6 and 12.20 Kcal/mole for 3- iodotyrosine and 4-iodophenyl alanine respectively. Reducing agents were added to the Cu CI catalyzed reactions to improve the yield and decrease side products formation. Applying the results obtained to the radioiodination of the phenyl fatty acid 15(p-iodophenyl) pentadecanoic acid

  16. Pulmonary uptake of morphine (M)

    Energy Technology Data Exchange (ETDEWEB)

    Roerig, D.L.; Bunke, S.S.; Kotrly, K.J.; Dawson, C.A.; Kampine, J.P.

    1986-03-01

    Previously the authors reported less than 5% of M was taken up during the first pass through the human lung. The low uptake of this basic lipophilic amine was further investigated in a single pass isolated perfused rat lung (IPL) in comparison to uptake of radiolabelled H/sub 2/O, antipyrine (A), aminopyrine (AM), nicotine (N) and phenylethylamine (P). The IPL was perfused for 5 min with each drug (5nmol/ml) and effluent collected in 10 sec fractions. Pulmonary extraction was calculated using indocyanine green dye as a non-extractable reference indicator. Accumulation of all compounds in the IPL reached an apparent equilibrium within 4 min. At equilibrium lung/perfusate conc. ratios for H/sub 2/O, A, AM, N, P and M were 1.04, 0.84, 0.85, 1.44, 2.57 and 1.13 respectively. The time course of M uptake differed from the other compounds since initial extraction of M was low (23%) compared to 75%, 53%, 35%, 82% and 86% for H/sub 2/O, A, AM, N and P respectively. Also, the half time to equilibrium for M was longer (50 sec) compared to 18, 21, 26, 19 and 22 sec for H/sub 2/O, A, AM, N and P respectively. The low initial pulmonary extraction of M compared to these compounds followed by greater M extraction during the remainder of drug infusion suggests uptake mechanisms for M different than the flow limited uptake for water and other basic amine drugs.

  17. Enantioselective analysis of 4-hydroxycyclophosphamide in human plasma with application to a clinical pharmacokinetic study.

    Science.gov (United States)

    de Castro, Francine Attié; Scatena, Gabriel dos Santos; Rocha, Otávio Pelegrino; Marques, Maria Paula; Cass, Quézia Bezerra; Simões, Belinda Pinto; Lanchote, Vera Lucia

    2016-02-01

    Cyclophosphamide (CY) is one of the most common immunosuppressive agents used in autologous hematopoietic stem cell transplantation. CY is a prodrug and is metabolized to active 4-hydroxycyclophosphamide (HCY). Many authors have suggested an association between enantioselectivity in CY metabolism and treatment efficacy and/or complications. This study describes the development and validation of an analytical method of HCY enantiomers in human plasma by high-performance liquid chromatography-tandem mass spectrometry (LC-MS/MS) that can be applied to pharmacokinetic studies, filling this gap in the literature. HCY enantiomers previously derivatized with phenylhydrazine were extracted from 200-μL plasma aliquots spiked with antipyrine as internal standard and a mixture of hexane and dichloromethane (80:20, v/v) was used as the extraction solvent. The derivatized HCY enantiomers were resolved on a Chiracel(®) OD-R column using water:acetonitrile:formic acid (55:45:0.2, v/v) as the mobile phase. No matrix effect was observed and the analysis of HCY enantiomers was linear for plasma concentrations of 5-5000ng of each enantiomer/mL plasma. The coefficients of variation and inaccuracy calculated in precision and accuracy assessments were less than 15%. HCY was stable in human plasma after three successive freeze/thaw cycles, during 3h at room temperature, and in the autosampler at 4°C for 24h after processing, with deviation values less than 15%. The method was applied to evaluate the kinetic disposition of HCY in a patient with multiple sclerosis who was pretreated with intravenous racemic CY for stem cell transplantation. The clinical study showed enantioselectivity in the pharmacokinetics of HCY. PMID:26760223

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

    Energy Technology Data Exchange (ETDEWEB)

    Kissen, I.

    1989-01-01

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

  19. Simultaneous measurement of blood flow and glucose metabolism by autoradiographic techniques

    Energy Technology Data Exchange (ETDEWEB)

    Mies, G.; Niebuhr, I.; Hossmann, K.A.

    A double tracer autoradiographic technique using 131I-iodo-antipyrine and 14C-deoxyglucose is presented for the simultaneous measurement of blood flow and cerebral glucose utilization in the same animal. 131I is a gamma emitting isotope with a half life of 8.06 days and can be detected with adequate resolution on standard autoradiographic films. Autoradiograms are made before and after decay of 131I; the time interval between the 2 exposures and the concentration of the 2 tracers is adjusted to avoid significant cross-contamination. In this way, 2 film exposures are obtained which can be processed quantitatively like single tracer autoradiograms. The validity of the method for the investigation of local coupling of flow and metabolism was tested under various physiological and pathophysiological conditions. Coupling was tight in barbiturate-anesthetized healthy animals, but not under halothane anesthesia where uncoupling occurred in various subcortical structures. Focal seizures induced by topical application of penicillin on the cortical surface led to a coupled increase of metabolism and flow in thalamic relay nuclei but not at the site of penicillin administration where increased glucose utilization was not accompanied by similar increase in blood flow. Both coupled and uncoupled increases in local glucose utilization were observed in spreading depression and in circumscribed areas of experimental brain tumors. The results obtained demonstrate that double tracer autoradiography allows allows the very precise local assessment of cerebral blood flow and glucose utilization, and, therefore, is particularly suited to the study of regional coupling processes under various experimental conditions.

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

    Science.gov (United States)

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

    2016-09-01

    4-Antipyrine [4-amino-1,5-dimethyl-2-phenyl-1H-pyrazol-3(2H)-one] and its derivatives exhibit a range of biological activities, including analgesic, antibacterial and anti-inflammatory, and new examples are always of potential interest and value. 2-(4-Chlorophenyl)-N-(1,5-dimethyl-3-oxo-2-phenyl-2,3-dihydro-1H-pyrazol-4-yl)acetamide, C19H18ClN3O2, (I), crystallizes with Z' = 2 in the space group P\\overline{1}, whereas its positional isomer 2-(2-chlorophenyl)-N-(1,5-dimethyl-3-oxo-2-phenyl-2,3-dihydro-1H-pyrazol-4-yl)acetamide, (II), crystallizes with Z' = 1 in the space group C2/c; the molecules of (II) are disordered over two sets of atomic sites having occupancies of 0.6020 (18) and 0.3980 (18). The two independent molecules of (I) adopt different molecular conformations, as do the two disorder components in (II), where the 2-chlorophenyl substituents adopt different orientations. The molecules of (I) are linked by a combination of N-H...O and C-H...O hydrogen bonds to form centrosymmetric four-molecule aggregates, while those of (II) are linked by the same types of hydrogen bonds forming sheets. The related compound N-(1,5-dimethyl-3-oxo-2-phenyl-2,3-dihydro-1H-pyrazol-4-yl)-2-(3-methoxyphenyl)acetamide, C20H21N3O3, (III), is isomorphous with (I) but not strictly isostructural; again the two independent molecules adopt different molecular conformations, and the molecules are linked by N-H...O and C-H...O hydrogen bonds to form ribbons. Comparisons are made with some related structures, indicating that a hydrogen-bonded R2(2)(10) ring is the common structural motif. PMID:27585929

  1. Transdermal permeation of drugs with differing lipophilicity: Effect of penetration enhancer camphor.

    Science.gov (United States)

    Xie, Feng; Chai, Jia-Ke; Hu, Quan; Yu, Yong-Hui; Ma, Li; Liu, Ling-Ying; Zhang, Xu-Long; Li, Bai-Ling; Zhang, Dong-Hai

    2016-06-30

    The aim of the present study was to investigate the potential application of (+)-camphor as a penetration enhancer for the transdermal delivery of drugs with differing lipophilicity. The skin irritation of camphor was evaluated by in vitro cytotoxicity assays and in vivo transdermal water loss (TEWL) measurements. A series of model drugs with a wide span of lipophilicity (logP value ranging from 3.80 to -0.95), namely indometacin, lidocaine, aspirin, antipyrine, tegafur and 5-fluorouracil, were tested using in vitro transdermal permeation experiments to assess the penetration-enhancing profile of camphor. Meanwhile, the in vivo skin microdialysis was carried out to further investigate the enhancing effect of camphor on the lipophilic and hydrophilic model drugs (i.e. lidocaine and tegafur). SC (stratum corneum)/vehicle partition coefficient and Fourier transform infrared spectroscopy (FTIR) were performed to probe the regulation action of camphor in the skin permeability barrier. It was found that camphor produced a relatively low skin irritation, compared with the frequently-used and standard penetration enhancer laurocapram. In vitro skin permeation studies showed that camphor could significantly facilitate the transdermal absorption of model drugs with differing lipophilicity, and the penetration-enhancing activities were in a parabola curve going downwards with the drug logP values, which displayed the optimal penetration-enhancing efficiency for the weak lipophilic or hydrophilic drugs (an estimated logP value of 0). In vivo skin microdialysis showed that camphor had a similar penetration behavior on transdermal absorption of model drugs. Meanwhile, the partition of lipophilic drugs into SC was increased after treatment with camphor, and camphor also produced a shift of CH2 vibration of SC lipid to higher wavenumbers and decreased the peak area of the CH2 vibration, probably resulting in the alteration of the skin permeability barrier. This suggests that

  2. Simultaneous measurement of blood flow and glucose metabolism by autoradiographic techniques

    International Nuclear Information System (INIS)

    A double tracer autoradiographic technique using 131I-iodo-antipyrine and 14C-deoxyglucose is presented for the simultaneous measurement of blood flow and cerebral glucose utilization in the same animal. 131I is a gamma emitting isotope with a half life of 8.06 days and can be detected with adequate resolution on standard autoradiographic films. Autoradiograms are made before and after decay of 131I; the time interval between the 2 exposures and the concentration of the 2 tracers is adjusted to avoid significant cross-contamination. In this way, 2 film exposures are obtained which can be processed quantitatively like single tracer autoradiograms. The validity of the method for the investigation of local coupling of flow and metabolism was tested under various physiological and pathophysiological conditions. Coupling was tight in barbiturate-anesthetized healthy animals, but not under halothane anesthesia where uncoupling occurred in various subcortical structures. Focal seizures induced by topical application of penicillin on the cortical surface led to a coupled increase of metabolism and flow in thalamic relay nuclei but not at the site of penicillin administration where increased glucose utilization was not accompanied by similar increase in blood flow. Both coupled and uncoupled increases in local glucose utilization were observed in spreading depression and in circumscribed areas of experimental brain tumors. The results obtained demonstrate that double tracer autoradiography allows allows the very precise local assessment of cerebral blood flow and glucose utilization, and, therefore, is particularly suited to the study of regional coupling processes under various experimental conditions

  3. Physiologically based synthetic models of hepatic disposition.

    Science.gov (United States)

    Hunt, C Anthony; Ropella, Glen E P; Yan, Li; Hung, Daniel Y; Roberts, Michael S

    2006-12-01

    Current physiologically based pharmacokinetic (PBPK) models are inductive. We present an additional, different approach that is based on the synthetic rather than the inductive approach to modeling and simulation. It relies on object-oriented programming. A model of the referent system in its experimental context is synthesized by assembling objects that represent components such as molecules, cells, aspects of tissue architecture, catheters, etc. The single pass perfused rat liver has been well described in evaluating hepatic drug pharmacokinetics (PK) and is the system on which we focus. In silico experiments begin with administration of objects representing actual compounds. Data are collected in a manner analogous to that in the referent PK experiments. The synthetic modeling method allows for recognition and representation of discrete event and discrete time processes, as well as heterogeneity in organization, function, and spatial effects. An application is developed for sucrose and antipyrine, administered separately and together. PBPK modeling has made extensive progress in characterizing abstracted PK properties but this has also been its limitation. Now, other important questions and possible extensions emerge. How are these PK properties and the observed behaviors generated? The inherent heuristic limitations of traditional models have hindered getting meaningful, detailed answers to such questions. Synthetic models of the type described here are specifically intended to help answer such questions. Analogous to wet-lab experimental models, they retain their applicability even when broken apart into sub-components. Having and applying this new class of models along with traditional PK modeling methods is expected to increase the productivity of pharmaceutical research at all levels that make use of modeling and simulation. PMID:17051440

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

    International Nuclear Information System (INIS)

    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 mmHg, 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. The difference in failure rate is highly significant (P<0.01). Four out of 30 diabetic patients required reamputation as against 10 out of 30 non-diabetics (0.05< P<0.10) The average SPP was higher in the diabetic group: 57 mmHg (range 18-93 mmHg) compared with 34 mmHg (range 8-68 mmHg) in the non-diabetic group (P<0.001). The postoperative SPP measured on the stumps was on average 8 mmHg higher than the preoperative SPP (P<0.001). The increase took place mainly in stumps with an SPP above 20 mmHg explaining why the preoperative SPP values related so 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. (author)

  5. Bio-inspired Design of Electrocatalysts for Oxalate Oxidation: a Combined Experimental and Computational Study of Mn–N–C Catalysts

    Energy Technology Data Exchange (ETDEWEB)

    Matanovic, Ivana; Babanova, Sofia; Perry, Albert; Serov, Alexey; Artyushkova, Kateryna; Atanassov, Plamen

    2015-05-28

    We report a novel non-platinum group metal (non-PGM) catalyst derived from Mn and amino- antipyrine (MnAAPyr) that shows electrochemical activity towards the oxidation of oxalic acid comparable to Pt with an onset potential for oxalate oxidation measured to be 0.714 * 0.002 V vs. SHE at pH = 4. The material has been synthesized using a templating Sacrificial Support Method with manganese nitrate and 4-aminoantipyrine as precursors. This catalyst is a nano-structured material in which Mn is atomically dispersed on a nitrogendoped graphene matrix. XPS studies reveal high abundance of pyridinic, Mn–Nx, and pyrrolic nitrogen pointing towards the conclusion that pyridinic nitrogen atoms coordinated to manganese constitute the active centers. Thus, the main features of the MnAAPyr catalyst are it exhibits similarity to the active sites of naturally occurring enzymes that are capable of efficient and selective oxidation of oxalic acid. Density functional theory in plane wave formalism with Perdew, Burke and Ernzerhof functional was further used to study the stability and activity of different one-metal active centers that could exist in the catalyst. The results show that the stability of the Mn–Nx sites changes in the following order: MnN4 4 MnN3C 4 MnN2C2 4 MnN3. Based on the overpotentials of 0.64 V and 0.71 V vs. SHE, calculated using the free energy diagrams for the oxalate oxidation mechanism, we could conclude that the MnN3C and MnN2C2 sites are most probable Mn–Nx sites responsible for the reported catalytic activity of the new catalyst.

  6. Transformation of phenazone-type drugs during chlorination.

    Science.gov (United States)

    Rodil, Rosario; Quintana, José Benito; Cela, Rafael

    2012-05-01

    Chlorination is one of the most popular disinfection steps for water treatment in Europe. However, chlorine can react with pharmaceuticals and other micropollutants leading to either their elimination or by-products being formed. These by-products are frequently not identified and therefore the consequences of chlorination can be underestimated. In this work, the degradation of two analgesics and antipyretics, phenazone (antipyrine) and propyphenazone, during chlorination was investigated by liquid chromatography-mass spectrometry (LC-MS). A quadrupole-time-of-flight (Q-TOF) system was used to follow the time course of the pharmaceuticals, and also used in the identification of the by-products. The degradation kinetics was investigated at different concentrations of chlorine (1-10 mg/L), bromide (0-100 μg/L) and sample pH (5.7-8.3) by means of a Box-Behnken experimental design. Depending on these factors, half-lives were in the ranges: 0.9-295 s for phenazone and 0.4-173 s for propyphenazone. Also, it was observed that chlorine concentration was a significant factor for propyphenazone, resulting in increased degradation rate as it is increased. The transformation path of these drugs consisted mainly of halogenations, hydroxylations and dealkylations. After several days of reaction two derivatives remained stable for phenazone: chloro-hydroxy-phenazone and N-demethyl-chloro-hydroxy-phenazone and two for propyphenazone: N-demethyl-hydroxy-propyphenazone and N-demethyl-chloro-hydroxy-propyphenazone. Moreover, experiments conducted with real water matrices, tap and surface water, showed that reaction, and formation of by-products, can take place both at the emission source point (household) and during drinking water production. PMID:22381982

  7. Development of an Abuse- and Alcohol-Resistant Formulation Based on Hot-Melt Extrusion and Film Coating.

    Science.gov (United States)

    Jedinger, Nicole; Schrank, Simone; Fischer, Johannes M; Breinhälter, Karlheinz; Khinast, Johannes; Roblegg, Eva

    2016-02-01

    This study focused on the development of flexible (i.e., deformable) multiple-unit pellets that feature (i) a prolonged drug release, (ii) drug abuse deterrence, and (iii) a minimal risk of alcohol-induced dose dumping (ADD). Deformable pellets were prepared via an advanced continuous one-step hot-melt extrusion (HME) technique, with the drug (i.e., antipyrine and codeine phosphate) fed as an aqueous solution into the molten matrix material (i.e., cornstarch, gum arabic, and xanthan). Formulations that had suitable mechanical characteristics (i.e., high compression strength) were coated with a flexible Aquacoat(®) ARC film to ensure prolonged release and to avoid ADD. The pellets were characterized in terms of their mechanical properties and in vitro drug release behavior in alcoholic media. All formulations were abuse deterrent: they had a high compression strength and grinding the pellets into powder was impossible. Since the pellets comprising gum arabic and xanthan as a matrix did not remain intact during dissolution testing, they had a very fast drug release rate. Cornstarch-based pellets that swelled but remained intact in the dissolution media had a slower drug release. Coated cornstarch-based pellets had a prolonged release over 8 h and resistance to dose dumping in 20 and 40% ethanol. Our results indicate that cornstarch-based pellets manufactured via the advanced HME process followed by coating are a promising formulation that makes tampering difficult due to a high compression strength combined with robustness in alcoholic media. PMID:26206403

  8. Pharmacokinetic drug interactions of macrolides.

    Science.gov (United States)

    Periti, P; Mazzei, T; Mini, E; Novelli, A

    1992-08-01

    , carbamazepine, phenazone (antipyrine) and triazolam. Troleandomycin can cause ergotism in patients receiving ergot alkaloids and cholestatic jaundice in those taking oral contraceptives. Erythromycin and its different prodrugs appear to be less potent inhibitors of drug metabolism. Case reports and controlled studies have, however, shown that erythromycins may interact with theophylline, carbamazepine, methylprednisolone, warfarin, cyclosporin, triazolam, midazolam, alfentanil, disopyramide and bromocriptine, decreasing drug clearance. The bioavailability of digoxin appears also to be increased by erythromycin in patients excreting high amounts of reduced digoxin metabolites, probably due to destruction of enteric flora responsible for the formation of these compounds. These incriminated macrolide antibiotics should not be administered concomitantly with other drugs known to be affected metabolically by them, or at the very least, combined administration should be carried out only with careful patient monitoring.(ABSTRACT TRUNCATED AT 400 WORDS) PMID:1511528

  9. Subcutaneous blood flow in psoriasis

    International Nuclear Information System (INIS)

    The simultaneously recorded disappearance rates of 133xe 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 133Xe was therefore measured--using a double isotope washout method (133Xe and [131I]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

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

    International Nuclear Information System (INIS)

    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

  11. Analysis of the photo catalytic degradation of the 4-chloro phenol and endosulfan by gas chromatography

    International Nuclear Information System (INIS)

    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 TiO2 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)

  12. Influencia de la formulación de la glutamina en sus efectos sobre los sistemas antioxidantes y de destoxificación hepática en la rata Effects of glutamine on antioxidants systems and hepatic detoxification in rats: influence of formulation

    Directory of Open Access Journals (Sweden)

    J. J. Ortiz de Urbina

    2004-03-01

    diets with L-glutamine or with L-alanyl-L-glutamine has on the balance of oxidants/antioxidants in the liver and on detoxification systems mediated by P-450 cytochrome in rats. Material and methods: Central catheters were inserted in the animals (n = 60 and they were randomly assigned to one of the following groups: a control group (C with oral feeding and I.V. infusion of saline solution, a total parenteral nutrition group without glutamine (TPN without GLN, a parenteral nutrition group with glutamine supplement (TPN GLN, and a total parenteral nutrition group with a supplement of alanine-gluta-mine dipeptide (20 g/L (TPN ALA-GLN. The parenteral nutrition provided was all isocaloric and isonitrogenated, and the infusions were administered at a speed of 2 ml/h over 5 days. Results: In the animals of the group without GLN, the liver concentration of glutathione was reduced while the levels of thiobarbituric acid reaction products (TBARS increased. Supplementing with either glutamine or ala-nine-glutamine normalized the levels of glutathione but the TBARS levels only fell in the group with the dipeptide. This effect was parallel to the partial recovery of the antioxidant enzyme activities analyzed. The liver concentrations of P-450 cytochrome, P-450 cytochrome dependent mono-oxygenases and the clearance of antipyrine were not modified by the supplements of glutamine or alanine-glutamine. Conclusions: Our data suggest a greater protection by alanine-glutamine supplements against the injury produced by free radicals during TPN and the absence of any effect with either glutamine or alanine-gluta-mine supplements on the oxidative metabolism of the liver.