• Archives of Pharmacal Research
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• v.14 no.2
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• pp.181-187
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• 1991

The muscarinic antagonist 1-[benzilic 4, 4'-$[^3H]$ QUINUCLIDINYL BENZILATE $([^3H]$ QNB) bound to a single class of muscarinic receptors with high affinity in rabbit ileal membranes. The $K_D\;and\;B_{ max}$ values for $([^3H]$ QNB calculated from analysis of saturation isotherms were 52.5 pM AND 154 fmol/mg, respectively. Chlopheniramine (CHP), histamine $H_1$ blocker, increased $K_D$ vlue for $([^3H]$QNB without affecting the binding site concentrations and Hill coefficient. The $K_i$ value of CHP for inhibition of $([^3H]$QNB binding in ileal membranes was 1.44\mu{M}$ and the pseudo-Hill coefficient for CHP was close to unit. In the functional assay carbachol, muscarinic agonist, increased the contractile force of ileum with $ED_{50}$ value of $0.11\mu{M}$. CHP caused the rightward shift of the dose-response curve to carbachol. The $pA_2$ value of CHP determined from Schild analysis of carbacholinduced contraction was 5.77 and the slope was unity indicating competitive antagonism with carbachol. The dissociation constant $(K_i)$ of CHP obtained in competitive experiments with $([^3H]$ QNB was similar to the $K_A$ value (1.69 \mu{M)}$ of CHP as inhibitor of carbachol induced contraction in rabbit ileum. This result suggest that the binding of $H_i$ blocker. CHP, vs $([^3H]$QNB to muscarinic receptors in ileal membranes represents an interaction with a receptor of physiological relevance.

• Archives of Pharmacal Research
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• v.26 no.4
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• pp.264-269
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• 2003

5-Aminosalicylic acid (5-ASA) is an active ingredient of therapeutic agents used for Crohn s disease and ulcerative colitis. Because it is absorbed rapidly and extensively in the upper intestine, delivery of the agent specifically to the colon is necessary. We selected taurine as a colon-specific promoiety and designed 5-aminosalicyltaurine (5-ASA-Tau) as a new colon-specific prodrug of 5-aminosalicylic acid (5-ASA). It was expected that introduction of taurine would restrict the absorption of the prodrug and show additive effect to the anti-inflammatory action of 5-ASA after hydrolysis. 5-ASA-Tau was prepared in good yield by a simple synthetic route. The apparent partition coefficient of 5-ASA-Tau in 1-octanol/pH 6.8 phosphate buffer or $CHCl_3$/pH 6.8 phosphate buffer was 0.10 or 0.18, respectively, at $37^{\circ}C$. To determine the chemical and biochemical stability in the upper intestinal environment, 5-ASA-Tau was incubated in pH 1.2 and 6.8 buffer solutions, and with the homogenates of tissue and contents of stomach or small intestine of rats at $37^{\circ}C$. 5-ASA was not detected from any of the incubation medium with no change in the concentration of 5-ASA-Tau. On incubation of 5-ASA-Tau with the cecal and colonic contents of rats, the fraction of the dose released as 5-ASA was 45% and 20%, respectively, in 8 h. Considering low partition coefficient and stability in the upper intestine, 5-ASA-Tau might be nonabsorbable and stable in the upper intestine. After oral administration, it would be delivered to the colon in intact form and release 5-ASA and taurine. These results suggested 5-ASA-Tau as a promising colon-specific prodrug of 5-ASA.

• YAKHAK HOEJI
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• v.37 no.6
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• pp.638-646
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• 1993

A cepfialosporin with an aminothiazoiylmethoxyimino-type side chain at the 7 position and bicyclic quinolone dithicarbamate at the 3' position was synthesized. It has broad and potent antivacterial activity in vitro. The antibacterial spectrum reflects contributions of both the cephalosporin moiety and the quinolone moiety. Thus, this compound was named DACD implying a dualaction cephalosporin derivative. In this paper, the physicochemical proper-ties (lipid-water partition, pKa), stability and pharmacokinetics of DACD were determined and compared with cefotaxime 3'-norfloxacin dithiocarbamate (CENO). Stability tests were studied in pH 1.20, 6.80 and 8.00 buffers and in the presence of AB type human plasma, rat liver homogenate and its .betha.-lactamase. The pharmacokinetic parameters of DACD were evaluated in mice after a single intravenous dose of 40 mg/kg. The results are as follows. The lipid-water partition coefficient of DACD was higher than that of CENO. The calculated pKa values of CENO and DACD, were 6.82$\pm$0.03, 7.53$\pm$0.21, respectively. In the hydrolysis test, half-lives (t$^{1/2}$) of CENO and DACD was 66.0 hr and 80.0 hr in pH 6.80 buffer, 190 hr and 91.4 hr in pH 8.00 buffer. CENO and DACD were rapidly hydrolyzed in human plasma and in rat liver hornogenate. Half-lives (t$_{1/2}$ of CENO and DACD were 1.29 hr and 1.15 hr in hyman plasma, 0.62 hr and 0.71 hr rat liver homogenate. In $\beta$-lactamase stability test, CENO and DACD were very stable to the .betha.-lactamases obtained from three different strains. Half-life (t$_{1/2}$) and areas under the curve (AUC) in mice were 2.33 hr and 15.97 (mg.h/1), respectively.

• Journal of the Korean Society of Radiology
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• v.13 no.5
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• pp.773-778
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• 2019

Images using X-rays are essential to diagnosis, but noise is inevitable in the image. To compensate for this, a total variation (TV) algorithm was presented to reduce the patient's exposure dose while increasing the quality of the images. The purpose of this study is to verify the effect on the image quality in radiographic imaging according to the thickness of the additional filtration plate through simulation, and to evaluate the usefulness of the TV algorithm. By using the Geant4 Application for Tomographic Emissions (GATE) simulation image, the actual size, shape and material of the Polymethylmethacrylate (PMMA) phantom were identical, the contrast to noise ratio (CNR) and coefficient of variation (COV) were compared. The results showed that the CNR value was the highest and the COV the lowest when applying the TV algorithm. In addition, we can acquire superior CNR and COV results with 0 mm Al in all algorithm cases.

• Journal of Radiation Industry
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• v.12 no.4
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• pp.267-276
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• 2018

A Hoffman 3D Brain Phantom was used to evaluate two PET/CT scanners, BIO_40 and D_690, according to the radiation dose of CT (low, medium and high) at a fixed kilo-voltage-peak (kVp) with the tube current(mA) varied in 17~20 stages(Bio_40 PET/CT scanner: the tube voltage was fixed to 120 kVp, the effective tube current(mAs) was increased from 33 mAs to 190 mAs in 10 mAs increments, D_690 PET/CT scanner: the tube voltage was fixed to 140 kVp, tube current(mA) was increased from 10 mAs to 200 mAs in 10 mAs increments). After obtaining the PET image, an attenuation correction was conducted based on the attenuation map, which led to an analysis of the difference in the image. First, the ratio of white to gray matter for each scanner was examined by comparing the coefficient of variation (CV) depending on the average ratio. In addition, a blind test was carried out to evaluate the image. According to the study results, the BIO_40 and D_690 scanners showed a <1% change in CV value due to the tube current conversion. The change in the coefficients of white and gray matter showed that the Z value was negative for both scanners, indicating that the coefficient of gray matter was higher than that of white matter. Moreover, no difference was observed when the images were compared in a blind test.

• Nuclear Engineering and Technology
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• v.51 no.3
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• pp.755-760
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• 2019

Compound samples based on the mineral-like magnesium potassium phosphate matrix $MgKPO_4{\times}6H_2O$ were synthesized by solidification of high level waste surrogate. Phase composition and structure of synthesized samples were studied by XRD and SEM methods. Compressive strength of the compounds is $12{\pm}3MPa$. Coefficient of thermal expansion of the samples in the range $250-550^{\circ}C$ is $(11.6{\pm}0.3){\times}10^{-6}1/^{\circ}C$, and coefficient of thermal conductivity in the range $20-500^{\circ}C$ is $0.5W/(m{\times}K)$. Differential leaching rate of elements from the compound, $g/(cm^2{\times}day)$: $Mg-6.7{\times}10^{-6}$, $K-3.0{\times}10^{-4}$, $P-1.2{\times}10^{-4}$, $^{137}Cs-4.6{\times}10^{-7}$; $^{90}Sr-9.6{\times}10^{-7}$; $^{239}Pu-3.7{\times}10^{-9}$, $^{241}Am-9.6{\times}10^{-10}$. Leaching mechanism of radionuclides from the samples at the first 1-2 weeks of the leaching test is determined by dissolution ($^{137}Cs$), wash off ($^{90}Sr$) or diffusion ($^{239}Pu$ and $^{241}Am$) from the compound surface, and when the tests continue to 90-91 days - by surface layer depletion of compound. Since the composition and physico-chemical properties of the compound after irradiation with an electron beam (absorbed dose of 1 MGy) are constant the radiation resistance of compound was established.

• Imaging Science in Dentistry
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• v.50 no.4
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• pp.299-307
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• 2020

Purpose: The diagnosis of chronic rhinosinusitis requires a comprehensive knowledge of the signs and symptoms of the disease and an accurate radiographic assessment. Computed tomography (CT) is the superior imaging modality for diagnosis of chronic rhinosinusitis. However, considering the lower dose and higher resolution of cone-beam computed tomography (CBCT) compared to CT, this study aimed to assess the agreement between the findings of CBCT and functional endoscopic sinus surgery (FESS). Materials and Methods: This descriptive prospective study evaluated 49 patients with treatment-resistant chronic rhinosinusitis who were candidates for FESS. Preoperative CBCT scans were obtained before patients underwent FESS. The agreement between the CBCT findings and those of FESS was determined using the kappa correlation coefficient. The frequency of anatomical variations of the paranasal sinuses was also evaluated on CBCT scans. Results: Significant agreement existed between pathological findings on CBCT scans and those of FESS, such that the kappa correlation coefficient was 1 for mucosal thickening, 0.644 for nasal deviation, 0.750 for concha bullosa, 0.918 for nasal polyp, 0.935 for ostiomeatal complex (OMC) obstruction, and 0.552 for infundibulum thickening. Furthermore, 95.9% of patients had 1 or more and 79.6% had 2 or more anatomical variations, of which nasal deviation was the most common (67.3%). Conclusion: Considering the significant agreement between the findings of CBCT and FESS for the detection of pathological changes in the paranasal sinuses, CBCT can be used prior to FESS to detect chronic rhinosinusitis and to assess anatomical variations of the OMC.

• Journal of Microbiology and Biotechnology
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• v.33 no.10
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• pp.1390-1401
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• 2023

In this study, a 12-week feeding experiment was conducted to characterize the effects of exogenous α-amylase on the growth, feed utilization, digestibility, plasma α-amylase activity, feed degradation rate, and fecal particle size of olive flounder (Paralichthys olivaceus). Diet was supplemented with 0 (AA₀; control), 100 (AA₁₀₀), 200 (AA₂₀₀), or 400 (AA₄₀₀) mg/kg of α-amylase, respectively. Fish (273.1 ± 2.3 g) were stocked into 12 tanks (25 fish/1,000-L tank) and 3 tanks were randomly selected for each diet group. As a result, α-amylase was found to have no significant effects (p ≥ 0.05) on the growth, feed utilization parameters, and whole-body proximate compositions. α-Amylase-treated fish exhibited only a significant increase in the apparent digestibility coefficient of carbohydrates compared to the controls. In addition, in vitro analyses revealed that α-amylase dose-dependently increased (p < 0.05) the feed degradation rate, while photographs of the intestinal content after 2, 4, and 8 h of feeding demonstrated an improved degradation rate in the α-amylase-treated groups. Plasma α-amylase content was higher in the AA₂₀₀ and AA₄₀₀ groups, whereas the control group produced significantly larger-sized fecal particles (90% size class) than these two groups. In the intestine, no changes were observed in the expression levels of the immune-related TNF-α, IL-1β, IL-2, immunoglobulin-M, HSP-70, lysozyme, and amylase alpha-2A. However, growth-related genes IGF-1, IGF-2, TGF-β3, and growth hormone genes were upregulated in muscle tissues. Collectively, exogenous α-amylase has positive roles in the modulation of the digestibility coefficient, blood α-amylase concentration, growth-related gene expression, and diet degradation for improved digestion in olive flounder.

• Korean Journal of Radiology
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• v.22 no.7
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• pp.1034-1043
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• 2021

Objective: The purpose of this meta-analysis was to investigate the pooled agreements of the coronary artery calcium (CAC) severities assessed by electrocardiogram (ECG)-gated and non-ECG-gated CT and evaluate the impact of the scan parameters. Materials and Methods: PubMed, EMBASE, and the Cochrane library were systematically searched. A modified Quality Assessment of Diagnostic Accuracy Studies-2 tool was used to evaluate the quality of the studies. Meta-analytic methods were utilized to determine the pooled weighted bias, limits of agreement (LOA), and the correlation coefficient of the CAC scores or the weighted kappa for the categorization of the CAC severities detected by the two modalities. The heterogeneity among the studies was also assessed. Subgroup analyses were performed based on factors that could affect the measurement of the CAC score and severity: slice thickness, reconstruction kernel, and radiation dose for non-ECG-gated CT. Results: A total of 4000 patients from 16 studies were included. The pooled bias was 62.60, 95% LOA were -36.19 to 161.40, and the pooled correlation coefficient was 0.94 (95% confidence interval [CI] = 0.89-0.97) for the CAC score. The pooled weighted kappa of the CAC severity was 0.85 (95% CI = 0.79-0.91). Heterogeneity was observed in the studies (I² > 50%, p < 0.1). In the subgroup analysis, the agreement between the CAC categorizations was better when the two CT examinations had reconstructions based on the same slice thickness and kernel. Conclusion: The pooled agreement of the CAC severities assessed by the ECG-gated and non-ECG-gated CT was excellent; however, it was significantly affected by scan parameters, such as slice thickness and the reconstruction kernel.

• Progress in Medical Physics
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• v.22 no.1
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• pp.52-58
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• 2011

Our goal is to assess the suitability of a glass dosimeter on detection of high-energy electron beams for clinical use, especially for radiation therapy. We examined the dosimetric characteristics of glass dosimeters including dose linearity, reproducibility, angular dependence, dose rate dependence, and energy dependence of 5 different electron energy qualities. The GD was irradiated with high-energy electron beams from the medical linear accelerator andgamma rays from a cobalt-60 teletherapy unit. All irradiations were performed in a water phantom. The result of the dose linearity for high-energy electron beams showed well fitted regression line with the coefficient of determination; $R^2$ of 0.999 between 6 and 20 MeV. The reproducibility of GDs exposed to the nominal electron energies 6, 9, 12, 16, and 20 MeV was ${\pm}1.2%$. In terms of the angular dependence to electron beams,GD response differences to the electron beam were within 1.5% for angles ranging from $0^{\circ}$ to $90^{\circ}$ and GD's maximum response differencewas 14% lower at 180o. In the dose rate dependence, measured dose values were normalized to the value obtained from 500 MU/min. The uncertainties of dose rate were measured within ${\pm}1.5%$ except for the value from 100 MU/min. In the evaluation of the energy dependence of the GD at nominal electron energies between 6 and 20 MeV, we obtained lower responses between 1.1% and 4.5% based on cobalt-60 beam. Our results show that GDs have a considerable potentiality for measuring doses delivered by high-energy electron beams.