• Title/Summary/Keyword: CLEARANCE

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Pharmacokinetics of a New Antigastritic Agent, Eupatilin, an Active Component of StillenE®, in Rats

  • Jang, Ji-Myun;Park, Kyung-Jin;Kim, Dong-Goo;Shim, Hyun-Joo;Ahn, Byung-Ok;Kim, Soon-Hoe;Kim, Won-Bae
    • Biomolecules & Therapeutics
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    • v.11 no.3
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    • pp.163-168
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    • 2003
  • Pharmacokinetics of eupatilin (an active components of $Stillen^{\circledR}$, a new antigastritic agent) were investigated after both intravenous and oral administration at a dose of 30mg/kg to rats. After intravenous administration, the plasma concentrations of unchanged eupatilin declined rapidly with a mean terminal half-life of 0.101 h. Eupatilin was eliminated fast in rats; the total body clearance was 121 mL/min/kg. Eupatilin was mainly metabolized in rats; the percentage of intravenous dose of eupatilin excreted in 24 h urine and feces as unchanged eupatilin was only 2.5 and 0.919%, respectively. Eupatilin was mainly metabolized to form its glucuronide conjugate; after intravenous administration, 15.9 and 51.7% of intravenous dose was excreted in 24 h urine and feces, respectively, as eupatilin plus its glucuronide. After oral administration, the absolute bioavailability was only 3.86% based on $AUC_{0-24h}$ of eupatilin plus its glucuronide. Approximately 68.5% of oral dose was not absorbed from the entire gastrointestinal tract. Therefore, it could be concluded that the superior effect of eupatilin in experimental animal models of gastric ulcer and inflammatory bowel disease after oral administration could be due to the local action of eupatilin. Further pharmacokinetic studies to elucidate the local action of eupatilin are required.

Effects of Adamantyl Derivatives on Pharmacokinetic Behavior of Paclitaxel in Rats

  • Kim, Kyung Mi;Lee, Kyeong;Jang, Kyusic;Moon, Yae Seul;Lee, Hwa Jeong;Rhie, Sandy Jeong
    • Biomolecules & Therapeutics
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    • v.25 no.5
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    • pp.553-558
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    • 2017
  • Paclitaxel (PTX) is one of the most frequently used anticancer agent for treating refractory ovarian cancer, metastatic breast cancer and non-small cell lung cancer. However, its oral administration is impeded by very low bioavailability (<5%) due to the P-glycopprotein (P-gp) efflux pump effect. This study investigated in vitro and in vivo P-gp inhibitory effects of adamantyl derivatives AC-603 and AC-786 in rats. Two adamantyl derivatives tested in this study increased the cytotoxicity of daunomycin (DNM) in P-gp overexpressed cell line by inhibiting P-gp efflux function. Pharmacokinetics of PTX with orally co-administered P-gp inhibitors were assessed in rats to improve PTX absorption. The pharmacokinetic parameters of PTX were determined in rats after intravenous (2 mg/kg) or oral (25 mg/kg) administration in the presence or absence of verapamil (a positive control), AC-603 or AC-786 (0.5 mg/kg or 5 mg/kg). Compared to control group (PTX alone), experimental groups (PTX with AC-603 or AC-786) significantly increased the area under the plasma concentration-time curve of PTX following oral administration by 1.7-2.2 fold. The volume of distribution and total clearance of PTX were decreased, while other parameters were not significantly changed. In conclusion, co-administration of AC-603 or AC-786 enhanced the relative bioavailability of orally administered PTX as compared to control.

Studies on the Diuretic Action of Oryeongsan and Kami-Oryeongsan (오령산(五笭散) 및 가미오령산(加味五笭散)이 가토이뇨작용(家兎利尿作用)에 미치는 영향(影響))

  • Lee, Sang-In
    • Korean Journal of Pharmacognosy
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    • v.12 no.1
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    • pp.31-43
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    • 1981
  • In order to determine the effect of Oryeongsan reputed to have diuretic action since Han Dynasty and possible synergetic action of Dianthi Semen, Polygonum avicularis Herba, Kochiae Fructus and Akebiae Lignum, herbs with similar reputation, when added to the above prescription, their decoction powders were solved into distilled water and injected into rabbits through the ear vein. Upon the treatment, the excretion of sodium, potassium and chloride ion together with urine volume was kinetically determined. At the same time the clearance of plasma creatinine and sodium ion was determined and the following results were obtained. Every experimental group demonstrated diuretic action, though feable, of relatively long duration. The diuretic mechanism in the case of Oryeongsan made up by mixing the seperate extracts of individual components and Oryeongsan(A) plus Dianthi Semen was found to be inhibitory effect of renal tubular reabsorption in contrast to the case of Oryeongsan(A) plus Polygonum avicularis Herba, Kochiae Fructus or Akebiae Lignum in which case the diuretic mechanism was found to be glomerular vascular dilatation. The urinary excretion of potassium ion was increased in the case of Oryeongsan(A) plus Dianthi Semen, Kochiae Fructus of Akebiae Lignum whereas in the other cases no similar change was registered. The diuretic action was most remarkable in the case of Oryeongsan(A) plus Polygonum avicularis Herba followed by Oryeongsan(A) plus Kochiae Fructus, Oryeongsan(A) plus Dianthi Semen, extract mixture of individual component of Oryeongsan, Oryeongsan(A) and Oryeongsan(A) plus Akebiae Lignum decreasing order. The duration of diuretic action was found to be 90 minutes in the case of Oryeongsan and mixture of individual component of Oryeongsan, and 60 minutes in the case of Oryeongsan(A) plus Dianthi Semen, Kochiae Fructus or Akebiae Lignum in contrast to the case of Oryeongsan(A) plus Polygonum avicularis Herba which lasted up to 120 minutes.

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Identification of Dynamic Stiffness of Squeeze Film Damper using Active Magnetic Bearing System as an Exciter (자기베어링 시스템을 가진기로 이용한 스퀴즈 필름 댐퍼의 동강성 계수 규명)

  • Kim, Keun-Joo;Lee, Chong-Won
    • Proceedings of the Korean Society for Noise and Vibration Engineering Conference
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    • 2002.11b
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    • pp.381-387
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    • 2002
  • In this work, the dynamic characteristics of an oil-lubricated, short SFD with a central feeding groove are derived based on a theoretical analysis considering the effect of a groove. The validity of the analysis is investigated experimentally using an Active Magnetic Bearing (AMB) system as an exciter. For the theoretical solution, the fluid film forces of a grooved SFD are analytically derived so that the dynamic coefficients of a SFD are expressed in terms of its design parameters. For the experimental validation of the analysis, a test rig using AMB as an exciter is proposed to identify the dynamic characteristics of a short SFD with a central groove. As an exciter, the AMB represents a mechatronic device to levitate and position the test journal without any mechanical contact, to generate relative motions of the journal inside the tested SFD and to measure the generated displacements during experiments with fairly high accuracy. Using this test rig, experiments are extensively conducted with different clearance, which is one of the most important design parameters, in order to investigate its effect on the dynamic characteristics and the performance of SFDs. Damping and inertia coefficients of the SFD that are experimentally identified are compared with the analytical results to demonstrate the effectiveness of the analysis. It is also shown that AMB is an ideal device for tests of SFDs.

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The Mechanism of Lotus Root Extract (LRE) as Neuro-Protective Effect in Alzheimer Disease (AD) (연근(蓮根)의 신경 보호 효과 및 기전연구)

  • Hong, Seung-Chul;Lee, Chia-Hung;Kim, Sang-Heon;Lee, Jin-Hee;Koo, Byung-Soo
    • Journal of Oriental Neuropsychiatry
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    • v.24 no.3
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    • pp.309-320
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    • 2013
  • Objectives : There is a possibility LRE as remedy in Alzheimer disease (AD), but it's nerve protection effect and mechanism have to be elucidate. In this research, we applied LRE on $A{\beta}_{25-35}$ pre-treated SH-SY5Y cells, to find out the nerve protection effect and mechanism in AD cell model. Methods : We tried to confirm that effect by experimenting with 20, 50, and $100{\mu}g/ml$ concentration of LRE as a medicine. Next experiment, we assessed damage effect which induced $A{\beta}_{25-35}$, known to cause AD, on SH-SY5Y cell. In addition, cellular viability test is executed under $H_2O_2$ treatment condition in a SH-SY5Y cell. Results : 1. In $A{\beta}_{25-35}$ treated SH-SY5Y cell, LRE exhibited an anti-phosphorylation effect about tau protein, JNK, and IKB. 2. LRE prevent nerve cell apoptosis, which indued $A{\beta}_{25-35}$ and oxidative stress, modify JNK engaged synaptic structure and $NF{\kappa}B$ induced p75-neurotrophin receptor polymorphism. Conclusions : We found that LRE prevented oxidative stress-induced cellular destruction, for example, increased SOD activity of $A{\beta}_{25-35}$ treated SH-SY5Y cell and reduced toxicity of oxygen free radical. Consequently, the ingredients of LRE have a role as a catalyzer for $A{\beta}_{25-35}$ clearance and as scavenger for active oxygen free radical.

Studies on the advanced model for quality control system of oriental medicine (한약재 품질관리체계 선진화 모형에 관한 연구)

  • Choi Sun-Mi;Yoon Yoo-Sik;Choi Hwan-Soo;Lee Mi-Young;Shin Soon-Shik;Lee Key-Nam;Chung Hee-Jin;Kim Hee-Soo;Sung Hyun-Jea
    • Journal of Society of Preventive Korean Medicine
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    • v.4 no.2
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    • pp.193-204
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    • 2000
  • In this study, advanced model for quality control of oriental medicine and methods for practice was suggested through literature inspection, analysis of foreign system such as China and Japan, survey analysis on the current system, quality analysis of randomly selected oriental medicine samples, and intensive discussions among oriental medicine specialists 1. The quality of oriental medicine should be consistently controlled by Ministry of Health and Welfare form its cultivation or import to its circulation process to final consumer 2. All oriental medicines should be circulated as standardized goods which should be marked by lot numbers. The packing material and Packing size should be liberalized. The qualify should be differentialized though free competition among makers. 3. Realistic standards for pesticide, heavy metal and decolorant should be established though long-term monitoring process according to each oriental medicine's origin, therapeutic part, cultivation area, harvesting time, and cultivation method. 4. Ministry of Health and Welfare should educate oriental medicine's quality control personnel regularly or on demand, and establish specialist pool. Ministry of Health and Welfare should also establish oriental medicine information system to provide informations about quality of domestic or foreign oriental medicinal raw materials. 5. The government should provide information about foreign of oriental medicine market to importers. Quality of imported oriental medicine should be inspected before its customs clearance, and all imported oriental medicine should be circulated by standardized oriental medicine makers. 6. Oriental medicine's pharmacopoeia should be Published to provide quality standard of oriental medicine and improve it.

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A Study on the Measurement for the Nano Scale Film Formation of Ultra Low Aspect Ratio

  • Jang Siyoul;Kong Hyunsang
    • Proceedings of the Korean Society of Tribologists and Lubrication Engineers Conference
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    • 2004.11a
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    • pp.283-288
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    • 2004
  • The measurement of ultra low aspect ratio fluid film thickness is very crucial technique both for the verification of lubrication media characteristics and for the clearance design in many precision components such as MEMS, precision bearings and other slideways. Many technologies are applied to the measurement of ultra low aspect ratio fluid film thickness (i.e. elastohydrodynamic lubrication film thickness). In particular, in-situ optical interferometric method has many advantages in making the actual contact behaviors realized with the experimental apparatus. This measurement method also does the monitoring of the surface defects and fractures happening during the contact behavior, which are delicately influenced by the surface conditions such as load, velocity, lubricant media as well as surface roughness. Careful selection of incident lights greatly enhances the fringe resolutions up to $\~1.0$ nanometer scale with digital image processing technology. In this work, it is found that coaxial aligning trichromatic incident light filtering system developed by the author can provide much finer resolution of ultra low aspect ratio fluid film thickness than monochromatic or dichromatic incident lights, because it has much more spectrums of color components to be discriminated according the variations of film thickness. For the measured interferometric images of ultra low aspect ratio fluid film thickness it is shown how the film thickness is finely digitalized and measured in nanometer scale with digital image processing technology and space layer method. The developed measurement system can make it possible to visualize the contact deformations and possible fractures of contacting surface under the repeated loading condition.

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Thermal Deformation Induced Preload Changein the Tilting Pad Journal Bearing (열변형으로 인한 틸팅패드 저널베어링의 예압 변화)

  • Suh, Junho;Hwang, Cheolho
    • Tribology and Lubricants
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    • v.32 no.1
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    • pp.1-8
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    • 2016
  • This paper focuses on the thermal deformation induced preload change in the tilting pad journal bearing, using a three-dimensional (3D) thermo-hydro-dynamic (THD) approach. Preload is considered as a critical factor in designing the tilting pad journal bearing. The initial preload measured under nil external load and nil thermal gradient is influenced by two factors, namely, the thermal deformation and elastic deformation. Thermal deformation is due to a temperature distribution in the bearing pads, whereas the elastic deformation is due to fluid forces acting on the pads. This study focuses on the changes induced in preload and film clearance due to thermal deformation. The generalized Reynolds equation is used to evaluate the force of the fluid and the 3D energy equation is used to calculate the temperature of the lubricant. The abovementioned equations are combined by establishing a relationship between viscosity and temperature. The heat transfer within the bearing pads, the lubricant, and the spinning journal is calculated using the heat flux boundary condition. The 3D Finite Element Method (FEM) is used in modeling the (1) heat conduction in the spinning journal and bearing pads, (2) thermal gradient induced thermal distortion of the spinning journal and pads, and (3) viscous shearing, and heat conduction and convection in a thin film. This evaluation method has an increased fidelity, and it can prove to be a cost-effective tool that can be used by designers to predict the dynamic behavior of a bearing.

Effect of Oil Supply Direction on Power Loss and Bearing Temperature of Elliptical Bearing (오일공급 방향에 따른 타원형 베어링 손실 및 온도 특성)

  • Bang, Kyungbo;Choi, Yonghoon;Cho, Yongju
    • Tribology and Lubricants
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    • v.34 no.4
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    • pp.138-145
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    • 2018
  • Elliptical bearings are widely used for large steam turbines owing to their excellent load carrying capacity and good dynamic stability. Power loss in bearings is an extremely important parameter, especially for high turbine capacities. Optimization of operation conditions and design variables such as bearing clearance and bearing length can reduce the power loss in elliptical bearings. Although changes in the oil supply method have served to increase the efficiency of the tilting pad journal bearing, it has not explicitly improved elliptical bearings. In this study, we verify the static characteristics of an elliptical bearing by changing the direction of oil supply. We evaluate the bearing power loss and bearing metal temperature, and compare the bearing performance and reliability in different test cases. The direction of oil supply is $90^{\circ}$ (9 o'clock) and $270^{\circ}$ (3 o'clock) when the rotor rotates in a counterclockwise direction. We use an elliptical bearing with an inner diameter and active length of 220.30 and 110.00 mm, respectively. Bearing power loss and bearing metal temperatures are measured and evaluated by rotor rotational speed, oil flow rate, and bearing load. The results reveal a 20 reduction in the power loss when the direction of oil supply is 90. Furthermore, the oil film on the upper part of the bearing has a high temperature when the direction of oil supply is $90^{\circ}$. In contrast, when the direction of oil supply is $270^{\circ}$, the oil film on the upper part of the bearing is relatively cold.

The Withdrawal Loads on The Effect of Dried Wooden Dowel (나무못 유지력에 나무못의 건조가 미치는 영향)

  • Cha, JaeKyung;Kim, Birm-June
    • Journal of the Korean Wood Science and Technology
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    • v.45 no.5
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    • pp.613-621
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    • 2017
  • This study was performed to determine the withdrawal loads and strengths on the effect of dried wooden dowel. The test block was manufactured from 15 mm thick domestic wood and particleboard. Dowels of 6, 8 and 10 mm in diameter are made of korean castanea, korean pine and tulip wood. Research reported here indicates that withdrawal loads increase, but withdrawal strengths decrease, as the dowel diameter increases. This study also indicates that withdrawal load and strength of dried wooden dowel showed over 10% increase compared to those of normal conditioned dowel. However, there was an exception for the case of korean pine test block with dried tulip wood dowel. Meanwhile, the dried wooden dowel withdrawal loads and strengths for particleboard test blocks show 6~14.4% and 6.2~18.2% increase, compared to those of normal conditioned dowel, respectively.