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Water Soluble Cyclosporine Monomethoxy Poly(ethyleneglycol) Conjugates as Potential Prod rugs

  • Cho, Hoon;Chung, Yong-Seog
    • Archives of Pharmacal Research
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    • v.27 no.6
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    • pp.662-669
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    • 2004
  • The highly water-soluble monomethoxypoly(ethyleneglycol) (mPEG) prod rugs of cyciosporin A(CsA) were synthesized. These prod rugs were prepared by initially preparing intermediate in the form of carbonate at the 3'-positions of CsA with chloromethyl chloroformate, in the pres-ence of a base to provide a 3'-carbonated CsA intermediate. Reaction of the CsA intermediate with mPEG derivative in the presence of a base provides the desired water-soluble prod rugs. As a model, we chose molecular weight 5 kDa mPEG in the reaction with CsA to give water soluble prodrugs. To prove that the prod rug is decomposed in the body to produce CsA, the enzymatic hydrolysis test was conducted using human liver homogenate at $37^{\circ}C$. The prodrug was decomposed in human liver homogenate to produce the active material, CsA, and the hydrolysis half-life ($t_{1/2}$) of the prodrug, KI-306 was 2.2 minutes at $37^{\circ}C$. However, a demon-stration of non-enzymatic conversion in pH 7.4 phosphate buffer was provided by the fact that the half-life ($t_{1/2}$) is 21 hours at 37$^{\circ}C$. The hydrolysis test in rat whole blood was also conducted. The hydrolysis was seen with half-life ($t_{1/2}$) of about 9.9, 65.0, 14.2, 3.4, 2.1 9.5, and 1.6 minutes for KI-306, 309, 312, 313, 315, 316, and 317, respectively. This is the ideal for CsA prodrug. The pharmacokinetic study of the prodrug, KI-306, in comparison to the commer-cial product (Sandimmune Neoral Solution) was also carried out after single oral dose. Each rat received 7 mg/kg of CsA equivalent dose. Especially, the prodrug KI-306 exhibits higher AUC and $C_{max}$ than the conventional Neoral. The AUC and $C_{max}$ were increased nearly 1.5 fold. The kinetic value was also seen with $T_{max}$ of about 1.43 and 2.44 hours for KI-306 and Neoral, respectively.

Effect of Some Treatments on the Autolysis of Baker's Yeast (Saccharomyces cerevisiae) (빵효모의 자기분해에 대한 몇가지 처리의 효과)

  • Choi, Im-Soon;Shim, Kyung-Mi
    • Journal of the Korean Society of Food Science and Nutrition
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    • v.13 no.3
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    • pp.313-318
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    • 1984
  • Some chemical, biochemical and physical treatments on the baker's yeasts (Saccharomyces cerevisiae) before 12-hour digestion at $50^{\circ}C$ were made to accelerate their autolysis. Dilute alkali treatment with 0.01N-NaOH solution showed a considerable increase in soluble nitrogen extraction only in the 6-hour initial autolysis. The addition of fresh yeast autolysate, 10% to the yeast slurry, could increase the autolysis rate from 65% to 83%. Microwave treatment of yeast slurry for 40 seconds also raised the autolysis rate by about 15%, while longer exposures to the microwave accompanying high temperatures repressed the autolysis process. Extrusion of the yeast cells with high pressures of 16,000 to 20,000 psi brought about significantly higher autolysis rate until the digestion time of 9 hours, but thereafter it showed a gradual drop in soluble nitrogen extraction.

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Heat treatment induced morphological changes of $Ca^{++}$ implanted single crystal $Al_2O_3$ ($Ca^{++}$를 implant한 단결정 $Al_2O_3$에서 열처리에 의한 형태학적 변화)

  • 김배연
    • Journal of the Korean Crystal Growth and Crystal Technology
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    • v.9 no.3
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    • pp.327-333
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    • 1999
  • Controlled Ca impurity implanted inner crack-like pore in the high purity alumina bi-crystal had been created by micro-fabrication technique, which includes ion implantation, photo-lithography, Ar ion milling, and hot press. The morphological change and the growth od crystals formed by heat treatment in Ca doped high purity single crystal alumina, were observed using optical microscopy. The dot was developed and hexagon like crystal appeared on inner surface of crack-like pore after heat treatment. Bar type crystals, probably CaO . $6Al_2O_3$, were observed on the inner surface of 100ppm Ca implanted specimen after 1 hour heat treatment at $1,500^{\circ}C$, but this bar type crystal disappeared after 1 hour heat treatment at $1,600^{\circ}C$. This disappearance means that there should be little increase of Ca solubility limit to alumina and/or changes of diffusion coefficient of Ca in alumina around this temperature.

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Behavior of New Heribicide Bensulfuron methyl (DPX-F5384) in Soil (토양중(土壤中)에 있어서 신규(新規) 제초제(除草劑) Bensulfuron methyl (DPX-F5384) 의 행동(行動))

  • Jang, I.S.;Moon, Y.H.;Ryang, H.S.
    • Korean Journal of Weed Science
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    • v.7 no.1
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    • pp.74-77
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    • 1987
  • This study was undertaken to elucidate the behavior of herbicide bensulfuron methyl [ methyl 2-[[[[[(4, 6-dimethoxy pryrimidine-2yl) amino] carbonyl] amino] sulfonyl] methyl] benzoate] in soils under flooded conditions using the test plant Monochoria vaginalis Pres 1. Besulfuron methyl moved to 3cm depth in clay loam soil and 4 cm depth in sandy loam soil. Herbicide-treated layer was found 0 to 2 cm profile in the former and 0 to 3 cm profile the latter. The half life (GR50) was 87 days in clay loam soil and 78 days in sandy clay loam soil. The period of inactivation lasted for 110 days in clay loam and 100 days in sandy clay loam soil.

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Rotordynamic Performance Predictions of Tilting Pad Journal Bearing with Rocker-Back Pivots and Comparison with Published Test Results (로커-백 피벗을 갖는 틸팅 패드 저널 베어링의 회전체동역학적 성능 예측 및 기존 결과와의 비교)

  • Kim, Tae Ho;Choi, Tae Gyu;Kim, Choong Hyun
    • Tribology and Lubricants
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    • v.31 no.6
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    • pp.294-301
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    • 2015
  • In this paper, we predict the rotordynamic force coefficients of tilting pad journal bearings (TPJBs) with rocker-back pivots, and we compare the predictions to recently published predictions and test data. The present TPJB model considers the rocker-back pivot stiffness calculated based on the Hertzian contact-stress theory, which is nonlinear with the application of a force . For the five-pad TPJB in load-between-pad and load-on-pad configurations, the predictions show the pressure- and film-thickness distributions, the deflection and stiffness of the individual pivots, and bearing stiffness and damping coefficients. The minimum film thickness and peak pressure occur at the bottom pad on which the applied load is directed. Because of the preload, the pres- sure is positive even at the upper pad in the opposite direction to the applied load. The pivot deflection and stiff- ness are maximum at the bottom pad that receives the heaviest pressure load. The predicted stiffness coefficients increase as the static load and rotor speed increase, while the damping coefficients decrease as the rotor speed increases, but increase as the static load increases. In general, the predicted stiffness coefficients agree well with the test data. The predicted damping coefficients overestimate the test data, particularly for large static loads. In general, the current predictive model considering the pivot stiffness improves the accuracy of the rotordynamic performance compared to previously reported models.

Eruptive mechanisms and processes at Udo tuff cone, Udo Island, Korea (우도응회과의 분출기기구와 분출과정)

  • Hwang, Sang-Koo
    • The Journal of the Petrological Society of Korea
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    • v.1 no.2
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    • pp.91-103
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    • 1992
  • Eruptive mechanisms and processes at Udo tuff cone can be inferred from indicative characters of products, bedforms and lithofacies, and ring faults. In terms of bedforms and lithofa-cies in particular, massive lapilli tuff beds and chaotic lapilli tuff beds are derived from subaerial falls of aggregated tephra of wet tephra finger jets, occurring dominantly at the lower sequences of proximal part at the tuff cone. Crudely stratified lapilli tuff are derived from subaerial falls of slightly aggregated tephra of less wet tephra finger jets, whereas reversely graded lapilli tuff beds are from slightly disaggregated subaerial falls of continuous uprush. Both beds frequently occur in the middle sequences at proximal and near medial part of the tuff cone. Block and lapilli tephra lenses, ash-coated lapilli tephra beds(lenses) and thin-bedded tuff beds are derived from extremely disaggregated subaerial falls of dry tephra in the continuous uprush, frequently occurring at the upper sequences of medial part at the tuff cone. Udo tuff cone is a basaltic volcano emergent through the sea water surface while water could flood across or into the vent area. Emergence of the tuff cone was from the type-Surtseyan eruption characterized by earlier tephra finger jets and later continuous uprush columns of tephra with copious volumes of steam. Explosions began when boiling of wter produced a bubble column reducing the hydrostatic pres-sure, allowing exsolution of gases from the magma. This expansion of magma into a vesiculating froth fragmented the magma and permitted mixing of magma and water so that a more vigorous generation of steam could proceed. Tephra finger jetting explosions continued to build the crater rims, then remove water from the vent that their deposits flowed like slsurries until the continuous uprush explosion ensued. Continuous uprush explosions were associated with most rapid accumula-tion of tephra. The increasing volume rate led to partial removal of water from the vent area by the newly tephra ring so that more vigorous activity could be attended by a reducing water supply. This might restrain surplus of cold water entering the vent and thus enhance the vigour of the eruption by allowing optimal heat exchange. Eventually the crater became so deep and unsuported that piecemeal sliding, or massive subsidence on indipping ring faults, filled and closed the vent, and the cycle of explosions and collapse began anew.

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A Study on Shear Bond Strength of Core-veneer Interface for Bilayered all Ceramics (Bilayered all Ceramics에서 Core와 Veneer 계면의 전단결합강도에 관한 연구)

  • Jung, Yong-Su;Lee, Jin-Han;Lee, Jae-In;Dong, Jin-Keun
    • Journal of Dental Rehabilitation and Applied Science
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    • v.24 no.3
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    • pp.231-242
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    • 2008
  • Purpose: The purpose of this study was to investigate the bond strength of the core-veneer interface in all ceramic systems. Material and Methods: The all ceramic systems tested with their respective veneer were IPS Empress 2 with IPS Eris, IPS e.max Press with IPS e.max Ceram and IPS-e.max ZirCAD with IPS e.max Ceram. Cores (N=36, N=12/group, diameter: 10mm, thickness: 3mm) were fabricated according to the manufacturer's instruction and cleaned with ultrasonic cleaner. The veneer(diameter: 3mm, thickness: 2mm) were condensed in stainless steel mold and fired on to the core materials. After firing, they were again ultrasonically cleaned and embedded in acrylic resin. The specimens were stored in distilled water at $37^{\circ}C$ for 1 week. The specimens were placed in a mounting jig and subjected to shear force in a universal testing machine(Z020, Zwick, Germany). Load was applied at close to the core-veneer interface as possible with crosshead speed of 1.00mm/min until failure. Average shear bond strengths(MPa) were analyzed with a one-way analysis of variance and the Tukey test(${\alpha}=.05$). The failed specimens were examinated by scanning electron microscopy(JSM-6360, JEOL, Japan). The pattern of failure was classified as cohesive in core, cohesive in veneer, mixed or adhesive. Results: The mean shear bond strength($MPa{\pm}SD$) were IPS e.max Press $32.85{\pm}6.75MPa$, IPS Empress 2 $29.30{\pm}6.51MPa$, IPS e.max ZirCAD $28.10{\pm}4.28MPa$. IPS Empress 2, IPS e.max Press, IPS e.max ZirCAD were not significantly different from each others. Scanning electron microscopy examination revealed that adhesive failure did not occur in any all ceramic systems. IPS Empress 2 and IPS e.max Press exhibited cohesive failure in both the core and the veneer. IPS e.max ZirCAD exhibited cohesive failure in veneer and mixed failure.

Antiviral Activity of Korean Traditional Prescriptions against Influenza Virus Type A (한약 처방 (복합체)의 Influenza Virus Type A에 대한 항바이러스 활성 효과)

  • Jung, Jae-Deuk;Ko, Byoung-Seob;Lee, Hyung-Hoan;Choi, Hwan-Soo;Park, Kap-Joo
    • The Journal of Korean Society of Virology
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    • v.26 no.2
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    • pp.273-283
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    • 1996
  • In order to search for anti-influenza virus type A agents from Korean traditional prescriptions (herb complexes), we selected 63 traditional prescriptions, based on a review of the Korean traditional medicine books. Both methanol extracts and boiling-water extracts were tested, by means of the Haemagglutination Inhibition Test (HIT). Three of the 63 methanol extracts: CM-22, CM-26, CM-48 (see explanation of nomenclature below), showed efficacy against influenza virus type ACM-22 showed anti-influenza virus type A activity at the range of $313{\mu}g/ml$ to $9.75{\mu}g/ml$, CM-26 showed antiviral activity at the range of $156{\mu}l/ml$ to $4.87{\mu}g/ml$, CM-48 showed anti-influenza virus type A activity at the range of $625{\mu}g/ml$ to $19.5{\mu}g/ml$, respectively. Three of the water extracts: CW-14, CW-34, CW-61 were active. CW-14 showed anti-influenza virus type A activity at the range of l0mg/ml to $78{\mu}g/ml$, CW-34 showed antiviral activity at the range of 10mg/ml to $625{\mu}g/ml$ and CW-61 showed anti-influenza virus type A activity at the range of l0mg/ml to $313{\mu}g/ml$, respectively. In order to determine cytotoxicity of each extracts, chicken red blood cells were incubated with the various concentration of extracts of Korean traditional prescriptions. CW-14, CW-34 and CW-61 did not show cytotoxic effect against red blood cells whereas CM-22, CM-26 and CM-48 showed cytotoxic effect against red blood cells at the range of l0mg/ml to $625{\mu}g/ml$, 10mg/ml to $313{\mu}g/ml$ and 10mg/ml to $313{\mu}g/ml$, respectively. These results indicated that Korean traditional pres criptions may be inhibit either attachment of virus to cell surface receptor or penetration of the virus into cell during the initial stage of infection.

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Preparation and Properties of Shape-Stabilized Phase Change Materials from UHMWPE and Paraffin Wax for Latent Heat Storage (파라핀과 초고분자량 폴리에틸렌으로 구성된 형태안정성 상 전이 물질의 제조 및 특성)

  • Lee, Hyun-Seok;Park, Jae-Hoon;Yim, Jong-Ha;Seo, Hye-Jin;Son, Tae-Won
    • Polymer(Korea)
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    • v.39 no.1
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    • pp.23-32
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    • 2015
  • Phase change materials based on ultra high molecular weight of polyethylene (UHMWPE) blended with paraffin wax (mp $65^{\circ}C$) were studied in this paper. In addition, this paper reviews recent studies on the preparation of shape stabilized phase change materials (SSPCM), such as SSPCM from UHMWPE and paraffin wax (mp $65^{\circ}C$), their basic properties and possible applications to latent heat storage. The preparation method was an absorption method. Also, SSPCM composites were prepared by using a hot press at $200^{\circ}C$ for 10 min. The analysis for the shape ability of SSPCM to improve heat efficiency was measured by FTIR, SEM, DSC, XRD, and ARES. UHMWPE composites with 30 wt% paraffin wax (mp $65^{\circ}C$) demonstrated less deterioration of physical property and effective thermal property compared with other conditions. As a result, these SSPCMs could be used for the heat storage and release materials for various products.

Development of Forest Volume Estimation Model Using Airborne LiDAR Data - A Case Study of Mixed Forest in Aedang-ri, Chunyang-myeon, Bonghwa-gun - (항공 LiDAR 자료를 이용한 산림재적추정 모델 개발 - 봉화군 춘양면 애당리 혼효림을 대상으로 -)

  • CHO, Seung-Wan;KIM, Yong-Ku;PARK, Joo-Won
    • Journal of the Korean Association of Geographic Information Studies
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    • v.20 no.3
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    • pp.181-194
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    • 2017
  • This study aims to develop a regression model for forest volume estimation using field-collected forest inventory information and airborne LiDAR data. The response variable of the model is forest stem volume, was measured by random sampling from each individual plot of the 30 circular sample plots collected in Bonghwa-gun, Gyeong sangbuk-do, while the predictor variables for the model are Height Percentiles(HP) and Height Bin(HB), which are metrics extracted from raw LiDAR data. In order to find the most appropriate model, the candidate models are constructed from simple linear regression, quadratic polynomial regression and multiple regression analysis and the cross-validation tests were conducted for verification purposes. As a result, $R^2$ of the multiple regression models of $HB_{5-10}$, $HB_{15-20}$, $HB_{20-25}$, and $HBgt_{25}$ among the estimated models was the highest at 0.509, and the PRESS statistic of the simple linear regression model of $HP_{25}$ was the lowest at 122.352. $HB_{5-10}$, $HB_{15-20}$, $HB_{20-25}$, and $HBgt_{25}-based$ models, thus, are comparatively considered more appropriate for Korean forests with complicated vertical structures.