• 제목/요약/키워드: Screen Concentration

검색결과 283건 처리시간 0.028초

혈장 시료 풀링을 통한 신약 후보물질의 흡수율 고효율 검색기법의 평가 (Evaluation of a Sample-Pooling Technique in Estimating Bioavailability of a Compound for High-Throughput Lead Optimazation)

  • 이인경;구효정;정석재;이민화;심창구
    • Journal of Pharmaceutical Investigation
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    • 제30권3호
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    • pp.191-199
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    • 2000
  • Genomics is providing targets faster than we can validate them and combinatorial chemistry is providing new chemical entities faster than we can screen them. Historically, the drug discovery cascade has been established as a sequential process initiated with a potency screening against a selected biological target. In this sequential process, pharmacokinetics was often regarded as a low-throughput activity. Typically, limited pharmacokinetics studies would be conducted prior to acceptance of a compound for safety evaluation and, as a result, compounds often failed to reach a clinical testing due to unfavorable pharmacokinetic characteristics. A new paradigm in drug discovery has emerged in which the entire sample collection is rapidly screened using robotized high-throughput assays at the outset of the program. Higher-throughput pharmacokinetics (HTPK) is being achieved through introduction of new techniques, including automation for sample preparation and new experimental approaches. A number of in vitro and in vivo methods are being developed for the HTPK. In vitro studies, in which many cell lines are used to screen absorption and metabolism, are generally faster than in vivo screening, and, in this sense, in vitro screening is often considered as a real HTPK. Despite the elegance of the in vitro models, however, in vivo screenings are always essential for the final confirmation. Among these in vivo methods, cassette dosing technique, is believed the methods that is applicable in the screening of pharmacokinetics of many compounds at a time. The widespread use of liquid chromatography (LC) interfaced to mass spectrometry (MS) or tandem mass spectrometry (MS/MS) allowed the feasibility of the cassette dosing technique. Another approach to increase the throughput of in vivo screening of pharmacokinetics is to reduce the number of sample analysis. Two common approaches are used for this purpose. First, samples from identical study designs but that contain different drug candidate can be pooled to produce single set of samples, thus, reducing sample to be analyzed. Second, for a single test compound, serial plasma samples can be pooled to produce a single composite sample for analysis. In this review, we validated the issue whether the second method can be applied to practical screening of in vivo pharmacokinetics using data from seven of our previous bioequivalence studies. For a given drug, equally spaced serial plasma samples were pooled to achieve a 'Pooled Concentration' for the drug. An area under the plasma drug concentration-time curve (AUC) was then calculated theoretically using the pooled concentration and the predicted AUC value was statistically compared with the traditionally calculated AUC value. The comparison revealed that the sample pooling method generated reasonably accurate AUC values when compared with those obtained by the traditional approach. It is especially noteworthy that the accuracy was obtained by the analysis of only one sample instead of analyses of a number of samples that necessitates a significant man-power and time. Thus, we propose the sample pooling method as an alternative to in vivo pharmacokinetic approach in the selection potential lead(s) from combinatorial libraries.

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영화 흥행 집중도와 상영 스크린 집중도로 살펴본 한국 영화산업 10년 (Last Ten Years of Korean Movie Industry through the Analysis on the Concentrations of Film Admission and Screening)

  • 김정호
    • 한국콘텐츠학회논문지
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    • 제15권5호
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    • pp.151-167
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    • 2015
  • 한국 영화의 시장 점유율은 최저 2008년 42.1%에서 최고 2013년 59.7%로 높은 점유율을 유지하고 있다. 그러나 멀티플렉스와 와이드 릴리스 전략, 4대 메이저 배급 회사와 3대 멀티플렉스 체인의 독과점의 영향으로 한국 영화 흥행의 양극화 현상은 심화되고 있다. 한국 영화 흥행 집중도는 2004년 0.53에서 2014년 0.85로 심화되었다. 흥행 순위 상위 10%의 한국 영화가 차지하는 관객 수 비중은 2004년 30.28%에서 2014년 71.2%로 급격히 높아진 반면에, 흥행 순위 하위 50%는 2004년 11.03%에서 2014년 0.08%로 아주 낮아졌다. 상영 스크린 집중도도 2004년 0.36에서 2014년 0.67로 심화되었고, 상영 횟수 집중도도 2004년 0.46에서 2014년 0.78로 높아졌다. 좌석 수의 집중도도 2004년 0.50에서 2014년 0.79이다. 많은 관객이 선택하는 영화라서 상영 스크린 수를 늘리고, 상영 횟수를 늘리고, 많은 좌석 수를 확보한다면, 이는 자연스러운 시장의 선택 결과라고 하겠다. 하지만 이들 영화들의 좌석 점유율 집중도를 보면 그렇지 않음을 알 수 있다. 좌석 점유율 집중도는 2004년 0.22에서 2014년 0.38로 다른 집중도와는 달리 완만한 증가세를 유지하고 있다. 상위 10% 영화들의 좌석 점유율은 2004년 38.2%에서 2014년 32.3%이며, 하위 50%는 2004년 23.5%에서 2014년 23.8%로 나타났다.

급성 중독환자에서 삼투압 계산식으로 추정된 에탄올 농도의 유효성 검증 (Discrepancies and Validation of Ethanol Level Determination with Osmolar Gap Formula in Patients with Suspected Acute Poisoning)

  • 정해원;이미진;조재완;안재윤;김창호
    • 대한임상독성학회지
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    • 제17권2호
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    • pp.47-57
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    • 2019
  • Purpose: Osmolar gap (OG) has been used for decades to screen for toxic alcohol levels. However, its reliability may vary due to several reasons. We validated the estimated ethanol concentration formula for patients with suspected poisoning and who visited the emergency department. We examined discrepancies in the ethanol level and patient characteristics by applying this formula when it was used to screen for intoxication due to toxic levels of alcohol. Methods: We retrospectively reviewed 153 emergency department cases to determine the measured levels of toxic ethanol ingestion and we calculated alcohol ingestion using a formula based on serum osmolality. Those patients who were subjected to simultaneous measurements of osmolality, sodium, urea, glucose, and ethanol were included in this study. Patients with exposure to other toxic alcohols (methanol, ethylene glycol, or isopropanol) or poisons that affect osmolality were excluded. OG (the measured-calculated serum osmolality) was used to determine the calculated ethanol concentration. Results: Among the 153 included cases, 114 had normal OGs (OG≤14 mOsm/kg), and 39 cases had elevated OGs (OG>14). The mean difference between the measured and estimated (calculated ethanol using OG) ethanol concentration was -9.8 mg/dL. The 95% limits of agreement were -121.1 and 101.5 mg/dL, and the correlation coefficient R was 0.7037. For the four subgroups stratified by comorbidities and poisoning, the correlation coefficients R were 0.692, 0.588, 0.835, and 0.412, respectively, and the mean differences in measurement between the measured and calculated ethanol levels were -2.4 mg/dL, -48.8 mg/dL, 9.4 mg/dL, and -4.7 mg/dL, respectively. The equation plots had wide limits of agreement. Conclusion: We found that there were some discrepancies between OGs and the calculated ethanol concentrations. Addition of a correction factor for unmeasured osmoles to the equation of the calculated serum osmolality would help mitigate these discrepancies.

$CCl_4$로 독성유발시킨 초대배양 간세포를 이용하여 간세포 보호효과를 나타내는 생약류의 검색 (Screening of Medicinal Plants Having Hepatoprotective Activity Effects with Primary Cultured Hepatocytes Intoxicated Using Carbon tetrachloride Cytotoxicity)

  • 이준우;최준한;강상모
    • 생약학회지
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    • 제23권4호
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    • pp.268-275
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    • 1992
  • We studied to screen medicinal plants having hepatoprotective activity with the primary cultured rat hepatocytes intoxicated with carbon tetrachloride cytotoxicity. The lowest concentration and treatment time of carbon tetrachloride giving the greatest intoxication to the primary cultured hepatocytes were observed in 10mM and 60 minutes, respectively. GTP and GOT activity of culture broth of the primary cultured rat hepatocytes intoxicated by $CCl_4$ cytotoxicity at this condition were increased 135.9% and 178.3% compared with that of the primaries cultured hepatocytes not treated with $CCl_4$, respectively. This increased GPT activity was inhibited by glycyrrizin, which was known to have hepatoprotective activity, and the inhibition activity was dependent on the concentration of glycyrrhizin. Forty species among the extracts obtained from 117 species of medicinal plants were shown to have the hepatoprotective activity. Among these 40 species, Prunus persica, Scutellaria baicalensis, Astragalus membranaceus, Tribulus terrestris, Caragana chamlagu, Acanthopanax sessiliflorum and Achyranthes japonica were indicated a lower GPT activity than that of Glycyrrhiza uralensis containing glycyrrhizin and GPT activity of these were indicated 75.5%, 70.0%, 59.0%, 77.5%, 60.0%, 75.0% and 79.0%, respectively.

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수경재배용 배양액의 이온성분 분석을 위한 고체형 센서 모듈 개발 (Development of a Solid State Ion Sensor Module for Analysis of Hydroponic Nutrients)

  • 김기영;이상봉;장영창
    • Journal of Biosystems Engineering
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    • 제32권5호
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    • pp.348-353
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    • 2007
  • A solid state ion sensor module has been developed and evaluated for hydroponic nutrients analysis. The sensor module consisted of five ion-selective electrodes (ISE) fabricated by screen-printing technology. The electrochemical responses of ion sensors for nitrate, ammonium, potassium, calcium, and pH were measured with specially designed 7-channel low voltage signal transducers. The analytical characteristics of the sensors were comparable with those of conventional ISE sensors. The solid state ion sensors exhibit linear relationships over five concentration decades. Detection limit of the sensors were $5.6{\times}10^{-5}{\sim}1.6{\times}10^{-7}M$ depends on ions. Performance test results showed that relative errors of measured ion concentrations were less than 5% for $NO_3{^-},\;K^+,\;Ca^{2+}$ ion, and pH. The concentration of $NO_3{^-},\;NH_4{^+},\;K^+,\;Ca^{2+}$, and pH ion in standard solution and nutrient solutions could be determined by direct potentiometric measurements without any conditioning before measurements.

Solution 코팅에 따른 Pb(Zr,Ti)$O_3$ 후막의 강유전 특성 (Ferroelectric Properties of Pb(Zr,Ti)$O_3$ Thick Films with Solution Coatings)

  • 박상만;이성갑;노현지;이영희;배선기
    • 한국전기전자재료학회:학술대회논문집
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    • 한국전기전자재료학회 2006년도 추계학술대회 논문집 Vol.19
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    • pp.35-36
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    • 2006
  • The influence of the concentration of precursor solution and the number of solution coatings on the densification of the Pb($Zr_xTi_{1-x}$)$O_3$(PZT) thick films was studied. PZT powder and PZT precursor solution were prepared by sol-gel method and PZT thick films were fabricated by the screen-printing method on the alumina substrates. The powder and solution of composition were PZT(70/30) and PZT(30/70), respectively. The coating and drying procedure was repeated 4 times. And then the PZT precursor solution was spin-coated on the PZT thick films. A concentration of a coating solution was 0.5 to 2.0 mol/L[M] and the number of coating was repeated from 0 to 6. The relative dielectric constant of the PZT thick film was increased with increasing the number of solution coatings and the thick films with 15M, 6-time coated showed the 698. The remanent polarization of the 1.5M, 6-time coated PZT thick films was 38.3 ${\mu}C/cm^2$.

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Screening methods for drought and salinity tolerance with transgenic rice seedlings

  • Song, Jae-Young;Song, Seon-Kyeong;Yu, Dal-A;Kim, Me-Sun;Kang, Kwon Kyoo;Cho, Yong-Gu
    • 한국작물학회:학술대회논문집
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    • 한국작물학회 2017년도 9th Asian Crop Science Association conference
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    • pp.165-165
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    • 2017
  • Abiotic stress is one of the major serious limiting factors in rice (Oryza sativa) and caused rice production losses. It is important to precisely screen valuable genetic resources for improving stress tolerance and understanding tolerance mechanism to abiotic stresses. Because there are differences of experiment designs for screening of tolerant plant in several studies related to abiotic stress, this study has performed to provide the rapid and efficiency screening method for selection of tolerance rice to drought and salinity stresses. Two week-old rice seedlings that reached about three leaf stage were treated with drought and salinity stresses and examined tolerant levels with tolerant and susceptible control varieties, and transgenic plants. To determine the optimum concentration for the selection of drought and salinity condition, tolerant, susceptible and wild-type plants were grown under three soil moisture contents (5, 10 and 20% water contents) and three NaCl concentrations (100, 200 and 250 mM) for 10 days at seedling stage. 200 mM NaCl concentration and 5% moisture content soil were determined as the optimum conditions, respectively. The described methodologies in this study are simple and efficiency and might help the selection of drought and salinity tolerance plants at the 3,4-leaf-seedling stage.

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인삼포장에 발생하는 당근뿌리혹선층의 방제를 위한 길항식물의 탐색 (Screening and Utilization of Antagonistic Plants to Control Northern root-knot Nematode in Ginseng Fields)

  • 양계진;도은수;김광호
    • Journal of Ginseng Research
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    • 제20권3호
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    • pp.331-338
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    • 1996
  • This study was conducted to screen the antagonistic plants on northern root-knot nematode (Meloidogyne) and to utilize those in its control. Egg hatching of M. hapla was found to be inhibited by 17 plant methanol extracts, and 11 plant extracts among them were also toxic to M. hapla second stage juvenile. Egg hatching of iW. hapla was also found to be inhibited by squeezed extracts of Cassia tora and Zea mays, and they were also toxic to M. hapla second stage juvenile. Extracts of Achyranthes japonica, Melia axedrach and Acorus graminens were toxic to M. hapla second stage with a juvenile mortality above 70clc at the 10 folds diluted concent ration and A. graminens was toxic to tested juvenile mortality above 50% at the 100 folds diluted concentration. The toxicity was directly propotional to the diluted concentration of the plant extracts and to the exposure period. Punica granatum, Acorns graminens and Melia axedrach were effective in inhibiting root penetration of JW. hapla juveniles, among of them p. granatum is most effective Percent inhibition of penetration by second and third stage juveniles into tomato slants penetrating by it was 72.7 and 82.4%, respectively.

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염료감응형 태양전지의 효율 향상을 위한 하이브리드 구조 광전극의 코팅특성 (Coating Property of Hybrid Structured Photo-Electrode to Increase Dye-Sensitized Solar Cells Efficiency)

  • 김민희;이형우;정영근
    • 한국분말재료학회지
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    • 제17권6호
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    • pp.449-455
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    • 2010
  • The hybrid structured photo-electrode for dye-sensitized solar cells was fabricated based on the composites of $TiO_2$ nanoparticles and nanowires. Three samples with different hybrid structures were prepared with 17 vol%, 43 vol%, and 100 vol% nanowires. The energy conversion efficiency was enhanced from 5.54% for pure nanoparticle cells to 6.01% for the hybrid structure with 17 vol% nanowires. For the hybrid structured layers with high nanowires concentration (43 vol% and 100 vol%), the efficiency decreased with the nanowire concentration, because of the decrease of specific surface area, and of thus decreased current density. The random orientations of $TiO_2$ nanowires can be preserved by the doctor blade process, resulted in the enhanced efficiency. The hybrid structured $TiO_2$ layer can possess the advantages of the high surface area of nanoparticles and the rapid electron transport rate and the light scattering effect of nanowires.

Artificial neural fuzzy system and monitoring the process via IoT for optimization synthesis of nano-size polymeric chains

  • Hou, Shihao;Qiao, Luyu;Xing, Lumin
    • Advances in nano research
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    • 제12권4호
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    • pp.375-386
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    • 2022
  • Synthesis of acrylate-based dispersion resins involves many parameters including temperature, ingredients concentrations, and rate of adding ingredients. Proper controlling of these parameters results in a uniform nano-size chain of polymer on one side and elimination of hazardous residual monomer on the other side. In this study, we aim to screen the process parameters via Internet of Things (IoT) to ensure that, first, the nano-size polymeric chains are in an acceptable range to acquire high adhesion property and second, the remaining hazardous substance concentration is under the minimum value for safety of public and personnel health. In this regard, a set of experiments is conducted to observe the influences of the process parameters on the size and dispersity of polymer chain and residual monomer concentration. The obtained dataset is further used to train an Adaptive Neural network Fuzzy Inference System (ANFIS) to achieve a model that predicts these two output parameters based on the input parameters. Finally, the ANFIS will return values to the automation system for further decisions on parameter adjustment or halting the process to preserve the health of the personnel and final product consumers as well.