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1.
In order to develop a possible C-X-C chemokine receptor type 4 (CXCR4) imaging agent for oncological scintigraphy, [62Zn]labeled 1,1′-[1,4-phenylenebis(methylene)]bis-1,4,8,11-tetraazacyclotetradecane ([62Zn]-AMD3100) was prepared using in-house made [62Zn]ZnCl2 and AMD-3100 for 1 h at 50 °C (radiochemical purity: >97 % ITLC, >96 % HPLC, specific activity: 20–22 GBq/mmol) in acetate buffer. The complex showed highly hydrophilic properties (log P = ?1.114). Stability of the complex was checked in presence of human serum (37 °C) and in final formulation for 1 day. The biodistribution of the labeled compound in vital organs of wild-type Sprague–Dawdley rats were determined and compared with that of free Zn2+ cation up to 6 h. Co-incidence imaging of the complex was consistent with the distribution data up to 3 h. The complex can be a possible in vivo generator compound for PET imaging in CXCR4 positive tumors.  相似文献   

2.
A mild and simple technique for preparing of 4-benzyl-1-(3-[125I]iodobenzylsulfonyl)piperidine, 4-(3-[125I]iodobenzyl)-1-(benzylsulfonyl)piperazine and their derivatives, as sigma-1 receptor ligands, with relatively high radiochemical yields via nucleophilic substitution reaction by means of isotopic and non-isotopic exchange reactions is described. Some factors affecting the radiochemical yield were commonly studied in presence of acidic medium at elevated temperature. Unfortunately, the radiochemical yields were weak. Some attempts were carried out in presence of polar aprotic solvents to enhance the radiochemical yield. N,N-Dimethylformamide was proved highly efficient for preparing of radioiodinated 4-benzyl-1-(3-iodobenzylsulfonyl)piperidine (4-B-[125I]-IBSP, 70 ± 5.7 %) and 4-(3-iodobenzyl)-1-(benzylsulfonyl)piperazine (4-[125I]-IBBSPz, 72 ± 6.0 %) at moderate temperature (100–105 °C) within 8 h. The specific activities of 4-B-[125I]-IBSP and 4-[125I]-IBBSPz (6,534.2 and 5,927.4 MBq/mmol) were obtained respectively.  相似文献   

3.
Precipitation of radiotellurium, containing trace radioimpurities, has been carried out from sulfate media at different pH-values. The highest precipitation yield was achieved at the region of pH ~4–6. Quantitative uptake by the formed precipitate was noticed for (i) 54Mn, 110mAg and 125Sb over all the pH-range of study (pH 1.7–9.2), (ii) for 65Zn and 60Co in the regions of pH ~6–8 and pH 6–8.8, respectively, and (iii) for 134Cs in the region of pH 1.7–2.8, while its percent uptake fluctuated around 60.5 % in the region of pH 4.4–6.4. Further precipitation studies have been conducted for a mixture of 125I and radiotellurium from sulfate, nitrate and chloride media at pH-values of 6.0 and 7.5. The highest 125I recovery yield in the obtained supernatant was 95.0 ± 1.3 %, which was achieved with sulfate medium at pH 6.0 with percent uptake values of 5.0 ± 1.3, 98.9 ± 0.9 and 62.0 ± 4.6 % of 125I, 123mTe and 134Cs, respectively, and quantitative uptake of 54Mn, 110mAg, 125Sb, 60Co and 65Zn by the precipitated tellurium. Thereafter, the supernatant was further acidified with H2SO4 and boiled, after adding H2O2, for 3 h. >99 % of 125I was distilled off from the acidified supernatant. The distilled of 125I was received in 0.1 M NaOH + 1 % Na2S2O3 solution, with a radionuclidic purity of >99.99 %, radiochemical purity of >99.8 % as I? and pH ~13.  相似文献   

4.
In the present study synthesis of the 99mTc?CCNN complex and its efficacy as a prospective Staphylococcus aureus (S. aureus) infection imaging agent was assessed. The 99mTc?CCNN complex was characterized in terms of stability in saline, serum, in vitro binding with S. aureus and in vivo percent absorption in male Wister rats (MWR) infected with live and heat killed S. aureus. Radiochemically the 99mTc?CCNN complex showed stable behavior in saline and serum at different intervals. At 30 min after reconstitution the complex showed maximum radiochemical purity (RCP) yield of 97.55 ± 0.22%. The RCP yield decreased to 90.50 ± 0.18% within 240 min. In serum, 18.15% unwanted side product was appeared within 16 h of the incubation. In vitro saturated binding with S. aureus was observed at different intervals with a 62.00% maximum at 90 min. Normal percent in vivo uptake was observed in MWR artificially infected with live S. aureus with a five times higher in the infected muscle as compared to the inflamed and normal muscles. No difference in the percent uptake of the complex in MWR infected with heat killed S. aureus in the infected, inflamed and normal muscles were observed. Based on the promising in vitro and in vivo radiochemical and biological characteristics, we recommend the 99mTc?CCNN complex for in vivo localization of the S. aureus infectious foci.  相似文献   

5.
Khellin, 4,9-dimethoxy-7-methyl-5H-furo[3,2-g]chromen-5-one, the most biologically active furochromone present in Ammi visnaga fruits indigenous to Egypt. A procedure for radioiodination of khellin with 125I is carried out via an electrophilic substitution reaction. The reaction parameters studied were khellin amount, pH of the reaction mixture, reaction time, temperature, different oxidizing agents and different organic media to optimize the conditions for the labeling of khellin and to obtain a high radiochemical yield of the 125I-khellin (125I-Khel). Using 3.7 MBq of Na125I, 100 μg (0.96 mM) of khellin as substrate, 100 μg (1 mM) of chloramine-T as oxidizing agent in ethanol at 60 °C for 10 min, a maximum radiochemical yield of 125I-Khel (78 %) was obtained. The specific activity of 125I-Khel was 3 MBq/0.5 mM. The biological distribution in normal mice indicates that radioiodinated khellin is a novel agent for urinary tract infection imaging.  相似文献   

6.
Ritodrine (a beta-2 adrenergic receptor agonist) was successfully labeled with 125I via direct electrophilic substitution reaction at ambient temperature. 125I-ritodrine was obtained with a maximum labeling yield of 97 ± 0.163 % and in vitro stability up to 24 h. Biodistribution studies showed that maximum in vivo uptake of 125I-ritodrine in lungs was 20.4 ± 0.22 % injected activity/g tissue at 1 h post-injection, whereas the clearance from mice appeared to proceed mainly via the renal pathway. 125I-ritodrine is not a blood product and so it is more safe than the currently available 99mTc-MAA, and its lung uptake is higher than that of the recently discovered 99mTc(CO)5I and 99mTc-DHPM. As a conclusion, radioiodinated ritodrine could be used as a novel radiopharmaceutical for lung perfusion scan safer than the currently available 99mTc-MAA and more potential than the recently discovered 99mTc(CO)5I and 99mTc-DHPM.  相似文献   

7.
A radiochemical method was investigated for separation and preconcentration of radioiodine from alkaline radiotellurium waste solution as Ag125I followed by recovery of 125I into aqueous NH3 solution and final purification by wet distillation. 125I–123mTe radiotracer solution (5 M NaOH) was equilibrated with prepared silver granules for different times and it was found that 125I was quantitatively removed from the aqueous phase after 7.0 h. The 125I-loaded silver was then equilibrated with ammonia solution in the presence of one of different reducing agents (namely, sodium borohydride, dextrose and zinc dust). Different concentrations of NH3 solution and reducing agents were studied. Quantitative recovery of 125I in the aqueous phase was achieved after 1.0 h of equilibration of 125I-loaded silver granules with 2.7M NH3 solution in the presence of Zn dust with a Zn:Ag molar ratio of 0.5. Purification of the recovered 125I was carried out by wet distillation from 20 % H2SO4 in the presence of H2O2. The distilled off 125I was received in a mixture solution of 0.1M NaOH and 0.01M Na2S2O3 with a radionuclidic purity of ≥99.99 %, radiochemical purity of ~98.8 % (as I? anions) and pH-value of ~13.  相似文献   

8.
P. D. Bari  A. R. Rote 《Chromatographia》2009,69(11-12):1469-1472
Two new, rapid, precise, accurate and specific chromatographic methods were described for the simultaneous determination of olmesartan medoxomil and hydrochlorothiazide in combined tablet dosage forms. The first method was based on reversed phase liquid chromatography using an Eurosphere 100 RP C18 column (250 × 4.6 mm ID, 5 μm). The mobile phase was methanol–0.05% o-phosphoric acid (60:40 v/v) at a flow rate of 1.0 mL min?1. Commercially available tablets and laboratory mixtures containing both drugs were assayed and detected using a UV detector at 270 nm. The second method involved silica gel 60 F254 high performance thin layer chromatography and densitometric detection at 254 nm using acetonitrile–ethyl acetate–glacial acid (7:3:0.4 v/v/v) as the mobile phase. Calibration curves ranged between 200–600 and 125–375 ng spot?1 for olmesartan and hydrochlorothiazide, respectively.  相似文献   

9.
The Fe2O3/lignite semi-coke sorbent was prepared by co-precipitation method with assistance of ultrasonic irradiation and underwent 4 sulfidation–regeneration cycles with O2/N2 as regeneration gases. The fresh, sulfided, and regenerated sorbents were characterized using XRD, SEM, XPS, and BET technologies in this paper. The regeneration mechanism was also discussed. It was found that in the oxygen atmosphere, FeS in the sulfided sorbent reacted with oxygen to produce Fe2O3 and SO2, the sulfate formed in regeneration process is easy to decompose at higher temperature. Regeneration kinetic studies were also performed at regeneration temperatures of 625–700 °C. It was found that the reaction order of regeneration with respect to O2 is first order. The equivalent grain model can be effectively used to correlate with the experimental data. In the early stage of reaction (x < 65 %), the regeneration is controlled by the chemical reaction, while it is controlled by the diffusion through the product layer in the latter stage (x > 70 %). According to the model, the apparent activation energy and the corresponding frequency factor for two different stages are 14.73 kJ mol?1 and 4.43 × 10?2 m s?1, 31.32 kJ mol?1 and 5.77 × 10?4 m2 s?1, respectively.  相似文献   

10.
In this study the bioleaching of a low-grade uranium ore containing 480 ppm uranium has been reported. The studies involved extraction of uranium using Acidithiobacillus ferrooxidans derived from the uranium mine samples. The maximum specific growth rate (µ max) and doubling time (t d) were obtained 0.08 h?1 and 8.66 h, respectively. Parameters such as Fe2+ concentration, particle size, temperature and pH were optimized. The effect of pulp density (PD) was also studied. Maximum uranium bio-dissolution of 100 ± 5 % was achieved under the conditions of pH 2.0, 5 % PD and 35 °C in 48 h with the particles of d 80 = 100 μm. The optimum concentration of supplementary Fe2+ was dependent to the PD. This value was 0 and 10 g of FeSO4·7H2O/l at the PD of 5 and 15 %, respectively. The effects of time, pH and PD on the bioleaching process were studied using central composite design. New rate equation was improved for the uranium leaching rate. The rate of leaching is controlled with the concentrations of ferric and ferrous ions in solution. This study shows that uranium bioleaching may be an important process for the Saghand U mine at Yazd (Iran).  相似文献   

11.
A new strategy for the early diagnosis of triple-negative breast cancer (TNBC) is urgently needed however specific targets are lacking. EphA2 has been reported to be over-expressed in a variety of tumors, including TNBC, and is closely related to tumor progression. In this study, we designed a novel peptide, SD01, and tested its potential in the diagnosis of TNBC. FITC-SD01 and FITC-YSA were prepared and found to bind to the 4T1 TNBC cell line, the former showing greater affinity. 125I-SD01 and 125I-YSA were obtained with high radiochemical yield and radiochemical purity, and both showed a high binding affinity to 4T1 cells, with a higher Bmax in 125I-SD01. Whole-body phosphoautoradiography showed clearer imaging of tumors in the group of 125I-SD01 than in 125I-YSA. Biodistribution demonstrated higher tumor accumulation in the 125I-SD01 group. In group of 125I-SD01, the tumor to the opposite muscle tissue (T/NT) ratio was 5.998 ± 0.37, in contrast to 4.69 ± 0.18 in 125I-YSA group. Our results indicated that 125I-SD01 could selectively and specifically target 4T1 cells in vitro and in vivo, and showed higher binding affinity and better imaging compared to 125I-YSA. Therefore, SD01 was deemed to be a novel peptide with more favorable properties in terms of targeting EphA2.  相似文献   

12.
Simultaneous electrochemical generation and functionalization of nano-sized graphite from graphite had been carried out in a non-fluoroanion-based ionic liquid, namely, triethylmethylammonium methylsulfate (TEMAMS) containing water and acetonitrile (AN) in different weight ratios. The oxygen-based functional groups attached with the exfoliated material had been identified using Fourier transform infrared spectroscopy (FTIR), and morphological changes were characterized by scanning electron microscopy (SEM) and transmission electron microscopy (TEM). A symmetrical supercapacitor was fabricated using the exfoliated nano-sized graphite, and the influence of surface functionalities on its performance was investigated using electrochemical impedance spectroscopy (EIS), cyclic voltammetry (CV), and galvanostatic charge–discharge cycles (CC). The highest specific capacitance (C sp) value of 140 F g?1 at 0.25 A g?1 was obtained in 1.0 M H2SO4, followed by aqueous TEMAMS (125 F g?1), TEMAMS/acetonitrile (115 F g?1), and TEMAMS (106 F g?1) at 0.10 A g?1.  相似文献   

13.
Cu-64 was produced via the 68Zn (p,αn)64Cu nuclear reaction (≈200 mCi, >95 % chemical yield at 180 μA for 1.1 h irradiation, (radionuclidic purity >96 %, copper-67 as impurity) followed by purification with amino functionalized nano magnetic oxide, Fe3O4 aiming to remove trace amount of heavy metal ions from aqueous media due to achieve ultra pure [64Cu] CuCl2 for labeling step. [64Cu] labeled 5,10,15,20-tetrakis(penta fluoro phenyl) porphyrin ([64Cu]-TFPP) was prepared using freshly prepared [64Cu] CuCl2 (Cu-64; T 1/2 = 12.7 h) and 5,10,15,20-tetrakis(penta fluoro phenyl)porphyrin (H2TFPP) for 60 min at 100 °C under reflux condition (radiochemical purity: >97 % ITLC, >98 % HPLC, specific activity: 14–16 GBq/mmol). Stability of the complex was checked in final formulation and human serum for 24 h. The partition coefficient was calculated for the compound (log P = 0.73). The biodistribution of the labeled compound in vital organs of wild-type rats was studied using scarification studies and PET imaging up in 2 and 4 h after injection. A detailed comparative pharmacokinetic study performed for 64Cu cation and [64Cu]-TFPP. The complex is mostly washed out from the circulation through kidneys and liver and can be an interesting tumor imaging/targeting agent due to high specific uptake and rapid excretion through the urinary tract.  相似文献   

14.
In this work, capability of the green microalga (MA), Chlorella vulgaris, in treating synthetic anaerobic effluent of municipal wastewater was investigated. While pure C. vulgaris (100 % MA) provided maximum soluble chemical oxygen demand (sCOD) and N???NH 4 + removal efficiencies of 27 and 72 % respectively, addition of activated sludge (AS) to MA in different mass ratios (91, 80, 66.7, 9 % MA) improved wastewater treatment efficiency. Thus giving maximum sCOD and N???NH 4 + removal efficiencies 85 and 86.3 % (for MA/AS?=?10/1), respectively. Utilizing AS without C. vulgaris, for treating the synthetic wastewater resulted in 87 % maximum sCOD and 42 % maximum N???NH 4 + removal efficiencies. Furthermore, algal growth and specific growth rates were measured in the systems with microalga as the dominant cellular population. As a result, faster algal growth was observed in mixed systems. Specific growth rate of C. vulgaris was 0.14 (day?1) in 100 % MA and 0.39 (day?1) in 80 % MA. Finally, data gathered by online measurement of dissolved oxygen indicate that algae-activated sludge mixture improves photosynthetic activity of examined microalga strain during anaerobic effluent treatment.  相似文献   

15.
A simple and rapid HPLC method using phenacetin (PHN) as internal standard has been developed for simultaneous determination of acetaminophen, caffeine, and chlorphenamine maleate in the product compound paracetamol and chlorphenamine maleate granules. Separation and quantitation were achieved on a 250 mm × 4.6 mm, 5 μm particle, C18 column. The mobile phase was methanol 0.05 mol L?1 aqueous KH2PO4 solution, 45:55 (v/v), containing 0.1% triethylamine and adjusted to pH 3.6 by addition of phosphoric acid; the flow rate was 1.0 mL min?1. Detection of all compounds was by UV absorbance at 260 nm and elution of the analytes was achieved in less than 12 min. The linearity, accuracy, and precision of the method were acceptable to good over the concentration ranges 6.4–153.6 μg mL?1 for acetaminophen, 5.0–120.0 μg mL?1 for caffeine, and 9.6–230.4 μg mL?1 for chlorphenamine maleate.  相似文献   

16.
Polyethylene-supported polymethyl methacrylate/poly(vinylidene fluoride-co-hexafluoropropylene) separator for gel polymer lithium-ion battery use was prepared with a mixed solvent of n-butanol and acetone. The prepared separator was characterized with scanning electron spectroscopy and X-ray diffraction, and its performance was investigated by electrochemical impedance spectroscopy and battery charge/discharge test. Compared to the separator prepared with acetone, the separator prepared with the mixed solvent shows an enhanced porosity (from 42 to 49 %) and electrolyte uptake (from 104 to 125 %). The ionic conductivity of the corresponding gel polymer electrolyte is improved from 2.81 to 3.39 mS cm?1, the discharge capacity retention of the LiCoO2/artificial graphite battery is increased from 95 to 98 % after 100 cycles at 0.5 C, and the discharge capacity of the battery at 1 C increases by 4 %.  相似文献   

17.
A novel sensitive and selective liquid chromatography-tandem mass spectrometry (LC-MS-MS) method simultaneously determined buprenorphine (BUP) and its active metabolite, norbuprenorphine (NBUP), and a coformulant, naloxone was developed, validated and applied successfully in humans. Buprenorphine-d 4 and norbuprenorphine-d 3 were used as the internal standard. The analysis was performed on a silica column, and the mobile phase was isocratic and composed of acetonitrile:2 mM ammonium formate in H2O (82:18, v/v). Mass spectrometry employed multiple reaction monitoring modes with transitions of m/z 468.1?C55.2 for BUP, 414.2?C101.2 for NBUP, 328.3?C310.3 for naloxone, 472.1?C59.2 for buprenorphine-d 4 and 417.2?C101.2 for norbuprenorphine-d 3. Lower limit of quantification (LLOQ) of the analytical method was 0.05 ng mL?1 for BUP, 0.1 ng mL?1 for NBUP and 0.025 ng mL?1 for naloxone, respectively. The standard calibration curves of BUP, NBUP and naloxone were linear over the concentration range of 0.05?C20 ng mL?1, 0.1?C20 ng mL?1 and 0.025?C20 ng mL?1, respectively. The precisions (RSD) and accuracies (RE) of LLOQ and other QC samples were in acceptable range, with RSD < 20% and RE ± 20% for LLOQ and RSD < 15% and RE within ±15% for QC samples. The method was accurate, precise and specific, and was applied to the pharmacokinetic study of buprenorphine in healthy volunteers.  相似文献   

18.
High-performance liquid chromatography coupled with tandem mass spectrometry has been used for sensitive and specific quantitative analysis of norethisterone (NE) in human serum. NE and the internal standard fentanil were isolated by solid-phase extraction. Chromatographic separation was achieved on a 4.6 mm × 50 mm, 5-μm particle, C18 column. The mobile phase was 70:30 (v/v) methanol–0.5% aqueous formic acid. NE and the internal standard were detected by multiple-reaction monitoring of precursor/product ion combinations at m/z 299.4/231.2 and 377.1/188.1, respectively; an atmospheric-pressure-photoionization source was used in positive-ion mode. Linearity was established in the concentration range 0.2–49.24 ng mL?1 and the lowest limit of quantification was 0.2 ng mL?1. Recovery of NE ranged from 92.54 to 102.74% and relative standard deviations were <15%. The method was used for a pharmacokinetic study of NE in healthy postmenopausal Chinese female volunteers.  相似文献   

19.
To enhance the capability of LiFePO4 materials, we attempted to coat carbon by incorporating various organic carboxylic acids as carbon sources. The purity of LiFePO4 was confirmed by XRD analysis. Galvanostatic cycling, cyclic voltammetry, electric impedance spectroscopy, and conductivity measurements were used to evaluate the material’s electrochemical performance. The best cell performance was delivered by the sample coated with 60 wt.% malonic acid. Its first-cycle discharge capacity was 149 mA h g?1 at a 0.2 C rate or 155 mA h g?1 at a 0.1 C rate. The presence of carbon in the composite was verified by total organic carbon and Raman spectral analysis. The actual carbon content of LiFePO4 was 1.90 wt.% with the addition of 60 wt.% malonic acid. The LiFePO4/C samples sintered with 60 wt.% various carboxylic acids were measured by Raman spectral analysis. The intense broad bands at 1,350 and 1,580 cm?1 are assigned to the D and G bands of residual carbon in LiFePO4/C composites, respectively. The peak intensity (I D/I G) ratio of the synthesized powders is from 0.907 to 0.935. Carbon coatings of LiFePO4 with low I D/I G ratios can be produced by incorporating carboxylic acid additives before the final calcining process. The use of carboxylic acid as a carbon source increases the overall conductivity (~10?4 S cm?1) of the material.  相似文献   

20.
The radiochemical separation of radiogallium from radiogermanium was studied using ion-exchange chromatography (Amberlite IR-120) and solvent extraction (Aliquat 336 in o-xylene). Both Amberlite IR-120 and Aliquat 336 in o-xylene have been used for the first time in separations involving radiogallium and radiogermanium. For tracer studies the radionuclides 68Ge (t 1/2 = 270.8 days), 69Ge (t 1/2 = 39 h) and 67Ga (t 1/2 = 78.3 h) were used. They were produced by the nuclear reactions natGa(p,xn)68,69Ge and natZn(p,xn)67Ga, respectively, and separated from their target materials in no-carrier-added form. Several factors affecting the separation of radiogallium from radiogermanium were studied and for each procedure the optimum conditions were determined. The solvent extraction using Aliquat 336 was found to be better. The separation yield of radiogallium was >95%, the time of separation short, the contamination from radiogermanium <0.008% and the final product was obtained in 0.5 M KOH. This method was adapted to the separation of n.c.a. 68Ga from its parent n.c.a. 68Ge. The quality of the product thus obtained is discussed.  相似文献   

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