• 제목/요약/키워드: New-Ring Test

검색결과 82건 처리시간 0.036초

로바스타틴 정제의 생물학적 동등성 평가 (Bioequivalence Evaluation of Lovastatin Tablets)

  • 복혜숙;김명민;최경업
    • 한국임상약학회지
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    • 제8권2호
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    • pp.107-112
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    • 1998
  • Lovastatin is a lipid lowering agent for the treatment of hypercholesterolemia and belongs to a new class of pharmacologic compounds called the 3-hydroxy-3-methylglutaryl coenzyme A (HMG CoA) reductase inhibitors. By competitively inhibiting HMG CoA reductase, lovastatin disrupts the biosynthesis of cholesterol in hepatic and peripheral cells and increases the synthesis of high-density-lipoprotein HDL) receptors. Following oral administration, the lactone ring of lovastatin is hydrolysed to the active inhibitor of HMG CoA reductase, lovastatin acid. Lovastatin is known to have poor oral absorption and wide individual variation. In this study, bioequivalence test of two lovastatin formulations, the test drug ($Lovaload^{TM}$, Chong Kun Dang Pharmaceutical Co.) and the reference drug ($Mevacor^{TM}$, Chung Wae Pharmaceutical Co.) were conducted according to the guidelines of Korea Food and Drug Administration (KFDA). A total of 18 healthy male volunteers, $31.90\pm3.60$ years old and $72.17\;7.88$ kg of body weight in average, were evaluated in a randomized crossover manner with a 2-week washout period. Concentrations of lovastatin acid in plasma were measured upto 12 hours following a single oral administration of eight tablets (20 mg of lovastatin per tablet) by high-performance liquid chromatography with UV detection at 238 nm. The area under the concentration-vs-time curve from 0 to 12 hours $(AUC_{0-12h})$ was calculated by the trapezoidal summation method. The statistical analysis showed that there are no significant differences in $AUC_{0-12h),\;C_{max}\;and\;T_{max}$ between the two formulations ($6.72\%,\;1.52\%,\;and\;0.88\$, respectively). The least significant differences between the formulations at $\alpha$=0.05 were less than $20\%\;(11.65\%,\;19.73\%,\;and\;14.81\%\;for\;AUC_{0-12h},\;C_{max}\;and\;T_{max}$, respectively). The $90\%$ confidence intervals for these parameters were also within $\pm20\%\;(-1.50{\leq}{\delta}{\leq}15.00$, $-12.50{\leq}{\delta}{\leq}15.50,\;and\;-9.64{\leq}{\delta]{\leq}11.40{\leq}\;for\;\;AUC_{0-12h}$ ,$C_{max}\;and\;T_{max}$, respectively). In conclusion, the new generic product $Lovaload^{TM}$ was proven to be bioequivalent with the reference drug.

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Imazapyr 유도체의 제초활성에 미치는 3-(N-methyl-N(X)-치환-Phenylaminooxoacetyl) Group의 영향 (Influence of 3-(N-methyl-N-X(Sub.)Phenylaminooxoacetyl) Group on the Herbicidal Activity of Imazapyr Derivatives)

  • 성낙도;유택승;장해성;김대황
    • Applied Biological Chemistry
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    • 제37권6호
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    • pp.516-521
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    • 1994
  • 새로운 17종의 imazapyr 유도체인 3-(N-methyl-N(X)-치환-phenylaminooxoacetyl)-2-(4-isopropyl-5-oxo-2-imidazoline-2-yl)pyridine, 6을 합성하고 3-(N-methyl-N(X)-치환-phenylaminooxoacetyl group중의 X-치환기 변화에 따른 구조와 옥수수(Zea mays L.)와 참비듬(Amaranthus viridis L.)에 대한 발아 전의 제초활성에 미치는 관계(SAR)를 검토 한 바, 옥수수의 경우에는 MR상수의 적정값(optimal value)이 $5.56\;cm^3/mol$이었으므로 이 값보다 크거나 작을수록 제초활성이 작았다. 참비듬의 경우에는 $L_1$상수의 적정값이 3.34 A이므로 이 값에 가까울수록 제초활성이 클 것임을 알 수 있었다. 특히, 2,5-difluoro group 치환체, 6i는 참비듬에 가장 큰 제초활성을 나타내었으나 옥수수에는 가장 작은 제초활성을 미치므로써 현저하게 두 초종간에 선택성을 나타내는 화합물이었다.

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Development and testing of multicomponent fuel cladding with enhanced accidental performance

  • Krejci, Jakub;Kabatova, Jitka;Manoch, Frantisek;Koci, Jan;Cvrcek, Ladislav;Malek, Jaroslav;Krum, Stanislav;Sutta, Pavel;Bublikova, Petra;Halodova, Patricie;Namburi, Hygreeva Kiran;Sevecek, Martin
    • Nuclear Engineering and Technology
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    • 제52권3호
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    • pp.597-609
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    • 2020
  • Accident Tolerant Fuels have been widely studied since the Fukushima-Daiichi accident in 2011 as one of the options on how to further enhance the safety of nuclear power plants. Deposition of protective coatings on nuclear fuel claddings has been considered as a near-term concept that will reduce the high-temperature oxidation rate and enhance accidental tolerance of the cladding while providing additional benefits during normal operation and transients. This study focuses on experimental testing of Zr-based alloys coated with Cr-based coatings using Physical Vapour Deposition. The results of long-term corrosion tests, as well as tests simulating postulated accidents, are presented. Zr-1%Nb alloy used as nuclear fuel cladding serves as a substrate and Cr, CrN, CrxNy layers are deposited by unbalanced magnetron sputtering and reactive magnetron sputtering. The deposition procedures are optimized in order to improve coating properties. Coated as well as reference uncoated samples were experimentally tested. The presented results include standard long-term corrosion tests at 360℃ in WWER water chemistry, burst (creep) tests and mainly single and double-sided high-temperature steam oxidation tests between 1000 and 1400℃ related to postulated Loss-of-coolant accident and Design extension conditions. Coated and reference samples were characterized pre- and post-testing using mechanical testing (microhardness, ring compression test), Thermal Evolved Gas Analysis analysis (hydrogen, oxygen concentration), optical microscopy, scanning electron microscopy (EDS, WDS, EBSD) and X-ray diffraction.

중앙버스전용차로 버스전용신호 도입시 신호 최적화에 관한 연구 (Development of Determining Technique of Optimum Signal Time of Intersections On Median Exclusive Bus Lane using Bus-only Signal)

  • 김보겸;김승일;김영찬;김진태
    • 대한교통학회지
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    • 제24권5호
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    • pp.123-133
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    • 2006
  • 서울시를 포함한 수도권 각 도시는 중앙버스전용차로의 적극적인 도입으로 버스속도 및 정시성 향상을 통해 대중교통우선 처리 전략을 적극 추진 중에 있다. 그러나 이로 인해 중앙부 $1{\sim}2$개 차로를 버스전용차로가 차지함으로써 기존 신호운영체계에 큰 변화를 가져오게 되었다 좌회전 차량과 중앙버스전용차로를 이용해 직진하는 버스간에 새로운 상충이 발생하게 되어 동시신호 기법 등 교차로 신호운영대안이 줄어들게 된 것이다 이 해결방안으로서 버스전용신호를 도입하여 중첩현시 및 동시신호 등 Dual-Ring방식의 다양한 신호 운영을 가능케 하는 방안이 모색되고 있다. 본 연구에서는 이러한 버스전용신호 도입 시 교차로 정체를 최소화할 수 있는 신호설계방법을 제시하였고, 중앙버스전용차로가 운영 중인 양재역사거리에 동 기법을 이용한 최적신호 설계를 적용, 시뮬레이션을 통해 그 효과를 검증하였다.

Pharmacophore Mapping and Virtual Screening for SIRT1 Activators

  • Sakkiah, Sugunadevi;Krishnamoorthy, Navaneethakrishnan;Gajendrarao, Poornima;Thangapandian, Sundarapandian;Lee, Yun-O;Kim, Song-Mi;Suh, Jung-Keun;Kim, Hyong-Ha;Lee, Keun-Woo
    • Bulletin of the Korean Chemical Society
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    • 제30권5호
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    • pp.1152-1156
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    • 2009
  • Silent information regulator 2 (Sir2) or sirtuins are NAD(+)-dependent deacetylases, which hydrolyze the acetyllysine residues. In mammals, sirtuins are classified into seven different classes (SIRT1-7). SIRT1 was reported to be involved in age related disorders like obesity, metabolic syndrome, type II diabetes mellitus and Parkinson’s disease. Activation of SIRT1 is one of the promising approaches to treat these age related diseases. In this study, we have used HipHop module of CATALYST to identify a series of pharmacophore models to screen SIRT1 enhancing molecules. Three molecules from Sirtris Pharmaceuticals were selected as training set and 607 sirtuin activator molecules were used as test set. Five different hypotheses were developed and then validated using the training set and the test set. The results showed that the best pharmacophore model has four features, ring aromatic, positive ionization and two hydrogen-bond acceptors. The best hypothesis from our study, Hypo2, screened high number of active molecules from the test set. Thus, we suggest that this four feature pharmacophore model could be helpful to screen novel SIRT1 activator molecules. Hypo2-virtual screening against Maybridge database reveals seven molecules, which contains all the critical features. Moreover, two new scaffolds were identified from this study. These scaffolds may be a potent lead for the SIRT1 activation.

Pharmacophore Modeling, Virtual Screening and Molecular Docking Studies for Identification of New Inverse Agonists of Human Histamine H1 Receptor

  • Thangapandian, Sundarapandian;Krishnamoorthy, Navaneethakrishnan;John, Shalini;Sakkiah, Sugunadevi;Lazar, Prettina;Lee, Yu-No;Lee, Keun-Woo
    • Bulletin of the Korean Chemical Society
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    • 제31권1호
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    • pp.52-58
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    • 2010
  • Human histamine H1 receptor (HHR1) is a G protein-coupled receptor and a primary target for antiallergic therapy. Here, the ligand-based three-dimensional pharmacophore models were built from a set of known HHR1 inverse agonists using HypoGen module of CATALYST software. All ten generated pharmacophore models consist of five essential features: hydrogen bond acceptor, ring aromatic, positive ionizable and two hydrophobic functions. Best model had a correlation coefficient of 0.854 for training set compounds and it was validated with an external test set with a high correlation value of 0.925. Using this model Maybridge database containing 60,000 compounds was screened for potential leads. A rigorous screening for drug-like compounds unveiled RH01692 and SPB00834, two novel molecules for HHR1 with good CATALYST fit and estimated activity values. The new lead molecules were docked into the active site of constructed HHR1 homology model based on recently crystallized squid rhodopsin as template. Both the hit compounds were found to have critical interactions with Glu177, Phe432 and other important amino acids. The interpretations of this study may effectively be deployed in designing of novel HHR1 inverse agonists.

차로속도역전현상을 고려한 연속류 도로의 차로별 주행 속도 특성 분석 (Lane-wise Travel Speed Characteristics Analysis in Uninterrupted Flow Considering Lane-wise Speed Reversal)

  • 양인철;전우훈;기성환;윤정은
    • 한국ITS학회 논문지
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    • 제15권6호
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    • pp.116-126
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    • 2016
  • 본 연구에서는 차로별 주행 궤적 데이터를 기반으로 차로속도역전현상이라는 개념을 이용하여 연속류 도로의 차로별 교통류 특성을 분석하였다. 1차로의 주행속도가 다른 차로보다 느린 경우를 차로속도역전현상이라고 정의하고, 이를 수식화하였다. 서울외곽순환고속도로(자유로IC~장수IC, 총 18.7km)를 대상으로 주중 5일(월~금) 동안의 오전 첨두시간대 차로별 주행 궤적 자료를 활용하여 거시적 측면과 미시적 측면에서 차로속도역전현상을 분석하였다. 실험구간 전체를 대상으로 차로별 주행속도를 비교한 거시적인 측면의 결과에서는 차로속도역전현상이 발생하지 않았으나, 실험구간을 세분화한 후 단위구간별 주행속도를 이용하여 미시적인 분석을 수행한 결과는 거시적인 분석 결과와 다르게 차로속도역전현상이 많이 발생하는 것으로 나타났다. 보다 혼잡한 구간에서 차로속도역전현상이 두드러지게 나타났고, 고속도로 기본구간보다는 연결로 접속부 구간에서 차로속도현상의 강도가 높게 나타났다. 본 연구의 결과는 머지않아 도래할 차로 교통정보 시대를 대비하여 현재의 교통정보 서비스 링크 단위의 적정성 판단, 차로 기반의 최적 경로 안내 서비스의 방향 결정 등에 기초적인 데이터로 활용이 가능하다.

Corynespora cassiicola에 의한 로즈마리 점무늬병 (Occurrence of Target Spot on Rosemary Caused by Corynespora cassiicola in Korea)

  • 이왕휴;한상준;최인영
    • 식물병연구
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    • 제19권1호
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    • pp.55-59
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    • 2013
  • 이 연구는 국내에 보고되지 않은 로즈마리 점무늬병이 남원과 전주의 재배 온실에서 발생하여 구명하고자 실험하였다. 이 병은 주로 고온 다습한 시기인 장마끝 무렵에 발생이 많았다. 로즈마리의 잎과 줄기에 검은점무늬(직경 3-5 mm) 및 시들음 증상이 나타났다. 병든 조직을 습실 처리하면 분생자경과 분생포자가 형성되었다. 로즈마리 점무늬병균의 분생포자는 체인상의 가늘고 긴 원통형으로, 길이는 $55-275{\times}7-14{\mu}m$이었다. 분생포자는 분생자경 위에 형성되었고, 분생포자의 위격벽의 수는 8-10개이었다. 또한 생장적온은 감자한천 배지와 암흑조건에서 $30^{\circ}C$이었다. 포트 식물에 병원성 검정결과 분리한 병원균은 접종 3일 후에 잎과 줄기에서 자연 병징과 같은 점무늬 및 시들음 증상이 재현되었고, 병든 부위에서 동일한 균이 재 분리되었다. 따라서 병원성이 있음이 확인되었다. rDNA ITS 영역의 염기서열 분석결과 로즈마리에 점무늬병을 일으키는 병원균은 Corynespora cassiicola로 GenBank accession number JQ595296, JQ595297, FJ852715, AY238606와 염기서열이 100% 일치하였고, C. cassiicola와 같은 계통군에 속하였다. 따라서, 로즈마리 잎 및 가지 점무늬병균은 C. cassiicola로 보고하고자 한다.

Geotechnical Engineering Progress with the Incheon Bridge Project

  • Cho, Sung-Min
    • 한국지반공학회:학술대회논문집
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    • 한국지반공학회 2009년도 세계 도시지반공학 심포지엄
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    • pp.133-144
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    • 2009
  • Incheon Bridge, 18.4 km long sea-crossing bridge, will be opened to the traffic in October 2009 and this will be the new landmark of the gearing up north-east Asia as well as the largest & longest bridge of Korea. Incheon Bridge is the integrated set of several special featured bridges including a magnificent cable-stayed girder bridge which has a main span of 800 m width to cross the navigation channel in and out of the Port of Incheon. Incheon Bridge is making an epoch of long-span bridge designs thanks to the fully application of the AASHTO LRFD (load & resistance factor design) to both the superstructures and the substructures. A state-of-the-art of the geotechnologies which were applied to the Incheon Bridge construction project is introduced. The most Large-diameter drilled shafts were penetrated into the bedrock to support the colossal superstructures. The bearing capacity and deformational characteristics of the foundations were verified through the world's largest static pile load test. 8 full-scale pilot piles were tested in both offshore site and onshore area prior to the commencement of constructions. Compressible load beyond 30,000 tonf pressed a single 3 m diameter foundation pile by means of bi-directional loading method including the Osterberg cell techniques. Detailed site investigation to characterize the subsurface properties had been carried out. Geotextile tubes, tied sheet pile walls, and trestles were utilized to overcome the very large tidal difference between ebb and flow at the foreshore site. 44 circular-cell type dolphins surround the piers near the navigation channel to protect the bridge against the collision with aberrant vessels. Each dolphin structure consists of the flat sheet piled wall and infilled aggregates to absorb the collision impact. Geo-centrifugal tests were performed to evaluate the behavior of the dolphin in the seabed and to verify the numerical model for the design. Rip-rap embankments on the seabed are expected to prevent the scouring of the foundation. Prefabricated vertical drains, sand compaction piles, deep cement mixings, horizontal natural-fiber drains, and other subsidiary methods were used to improve the soft ground for the site of abutments, toll plazas, and access roads. Light-weight backfill using EPS blocks helps to reduce the earth pressure behind the abutment on the soft ground. Some kinds of reinforced earth like as MSE using geosynthetics were utilized for the ring wall of the abutment. Soil steel bridges made of corrugated steel plates and engineered backfills were constructed for the open-cut tunnel and the culvert. Diverse experiences of advanced designs and constructions from the Incheon Bridge project have been propagated by relevant engineers and it is strongly expected that significant achievements in geotechnical engineering through this project will contribute to the national development of the longspan bridge technologies remarkably.

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국내 잎들깨에서 발생한 잠두위조바이러스2의 특성 구명 (Characterization of broad bean wilt virus 2 isolated from Perilla frutescens in Korea)

  • 김현선;변희성;최유지;최현용;서장균;최홍수;이봉춘;김미경;곽해련
    • 환경생물
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    • 제41권1호
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    • pp.1-13
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    • 2023
  • 잠두위조바이러스2 (BBWV2)는 경제적으로 중요한 원예, 관상작물에 심각한 피해를 주는 바이러스 중의 하나다. BBWV2의 넓은 기주 범위, 매개충 방제의 어려움 등 효과적인 치료제가 없기 때문에, 병을 예방하거나 저항성 품종의 개발 등을 위해서는 BBWV2의 새로운 분리주들의 특성 조사와 연구가 필요하다. 본 연구에서는 2019년 금산지역의 잎들깨 재배농가에서 분리된 BBWV2 분리주(BBWV2-GS-PF)의 유전학적·생물학적 특성을 구명하고 기존에 보고된 분리주들과의 특성을 비교하였다. 순수 분리된 BBWV2-GS-PF는 기존 분리주와 달리 들깨에서 심한 모자이크 증상과 고추에서 원형 반점 증상을 보였다. BBWV2-GS-PF의 유전자 계통분석 결과, 기존에 알려진 2개의 그룹과 약 76~80%의 비교적 낮은 유전자 상동성을 보이며 계통이 분화된 것을 확인할 수 있었다.