• Title/Summary/Keyword: N release rate

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Hydrophobic Cyclodextrin Derivatives as a Sustained Release Carrier of Azidothymidine (아지도싸이미딘의 지속성방출형담체로서의 소수성시클로덱스트린유도체)

  • Seo, Bo-Youn;Park, Gee-Bae;Lee, Kwang-Pyo
    • Journal of Pharmaceutical Investigation
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    • v.26 no.2
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    • pp.71-82
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    • 1996
  • This study has been undertaken to evaluate hydrophobic cyclodextrin(CD) derivatives as a sustained release carrier of azidothymidine(AZT), AZT, which has potent activity against AIDS and AIDS-related complex as thymidine analogue, has been reported that it has significant toxicity and short half life. Therefore, it is necessary to design sustained release oral dosage form to avoid undesirable side effects attributable to an excessive plasma concentration and to reduce the frequency of administration of AZT. Inclusion complexes of AZT with $acetyl-{\beta}-cyclodextrin\;(AC{\beta}CD)$ and $triacetyl-{\beta}-cyclodextrin(TA{\beta}CD)$ were prepared by solvent evaporation method. Interactions of AZT with CD were investigated by Differential Scanning Calorimetry(DSC) and Infrared Spectrophotometry(IR). The decreasing order of water solubilities of AZT and AZT-CD inclusion complexes were as follows; $AZT\;(27.873{\pm}0.015,mg/ml)\;>\;AZT-AC{\beta}CD\;(3.377{\pm}0.003)\;>\;AZT-TA{\beta}CD\;(2.528{\pm}0.001)$. Partition coefficients of $AZT-AC{\beta}CD\;and;\AZT-TA{\beta}CD$ inclusion complexes were increased by 1.27-fold, 1.54-fold in pH 1.2 and 1.32-fold, 1.47-fold in pH 6.8 in comparison with that of AZT. The mean dissolution time (MDT, min) which represents the rapidity of dissolution rate of AZT, $AZT-AC{\beta}CD,\;AZT-TA{\beta}CD$ were 5.12, 14.02 and 19.38 min in pH 1.2 and 2.52, 15.19 and 18.19 min in pH 6.8. AZT was very rapidly and completely dissolved in pH 1.2 and pH 6.8 within 5 minutes. But AZT-CD inclusion complexes showed the sustained release pattern in comparison with AZT alone. The simultaneous in situ nasal and jejunal recirculation study to compare the intrinsic absorptivity and the property of absorption sites revealed that the absorption of $AZT-TA{\beta}CD\;(N:35.35{\pm}1.08%,\;J:27.47{\pm}1.18%)$ was more than that of $AZT\;(N:16.89{\pm}2.25%,\;J:15.86{\pm}2.33%)$. The above results suggest that $TA{\beta}CD$ which is a hydrophobic cyclodextrin may serve as sustained release carrier with absorption enhancing effect.

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A Study on the Post-Receptor Mechanism of Adenosine Receptor on Norepinephrine Release in the Rat Hippocampus (흰쥐 해마에서 Norepinephrine 유리에 미치는 Adenosine Receptor의 Post-Receptor 기전에 관한 연구)

  • Choi, Bong-Kyu;Kim, Do-Kyung;Yang, Kyung-Moo
    • The Korean Journal of Pharmacology
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    • v.32 no.1
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    • pp.1-11
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    • 1996
  • Since it has been reported that the depolarization-induced norepinephrine (NE) release is inhibited by activation of presynaptic $A_1-adenosine$ heteroreceptor in hippocampus, a large body of experimental data on the post-receptor mechanism of this process has been accumulated. But, the post-receptor mechanism of presynaptic $A_1-adenosine$ receptor on the NE release has not been clearly elucidated yet. Therefore, it was attempted to clarify the post-receptor mechanisms of the $A_1-adenosine$ receptor-mediated control of NE release in this study. Slices from rat hippocampus were equilibrated with $^3H-norepinephrine$ and the release of the labelled products was evoked by electrical stimulation (3 Hz, 5 $Vcm^{-1}$, 2 ms, rectangular pulses), and the influence of various agents on the evoked tritium-outflow was investigated. Adenosine, in concentrations ranging from $1{\sim}30{\mu}M$, decreased the NE release in a dose-dependent manner, without affecting the basal rate of release. The adenosine effects were significantly inhibited by 8-cyclopentyl-1,3-dipropylxanthine (DPCPX, $2{\mu}M$), a selective $A_1-receptor$ antagonist. The responses to N-ethylmaleimide (NEM, 10 & $30{\mu}M$), a SH-alkylating agent of G-protein, were characterized by increments of the evoked NE-release and the basal release, and the adenosine effects were completely abolished by NEM pretreatment. $4{\beta}-Phorbol$ 12,13-dibutyrate (PDB, $1{\mu}M$), a specific protein kinase C (PKC) activator, increased the evoked NE release, whereas polymyxin B sulfate (PMB,0.1 mg), a PKC inhibitor, decreased the release, and the adenosine effects were inhibited by these agents. Nifedipine $(1{\mu}M)$, a $Ca^{2+}-channel$ blocker of dihydropyridine analogue, did not affect the adenosine effect. Tetraethylammonium (TEA, 3 mM) increased the evoked NE release, and inhibited the adenosine effects, but glibenclamide, a ATP dependent $K^+-channel$ blocker, did not. Finally, 8-bromo cyclic AMP (100 & $300{\mu}M$), a membrane-permeable analogue of cAMP, did not alter the NE release, but adenosine effects were inhibited by pretreatment with 8br-cAMP. These results suggest that the decrement of the evoked NE-release by $A_1-adenosine$ receptor is mediated by the C-protein, which is coupled to protein kinase C, adenylate cyclase system and TEA sensitive $K^+-channel$, and that nifedipine-sensitive $Ca^{2+}-channel$ and glibenclamide-sensitive $K^+-channel$ are not involved in this process.

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An Experimental Study on the Effects of the Automotive Cooling Performance by Cooling Airflow rate (II) (냉각 공기량이 자동차 냉각성능에 미치는 영향에 관한 실험적 연구(II))

  • Kim, J.H.;Lee, H.C.;Lee, M.H.;Park, J.N.;Cha, K.O.
    • Proceedings of the KSME Conference
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    • 2001.11b
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    • pp.940-945
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    • 2001
  • Gasoline engine manufacturers are currently considering designs that will result in low combustion air temperature for improvement of fuel consumption and emission levels. There are a variety of cooling systems that can be used to accomplish this goal. Cooling is therefore normally achieved through a balance of ram and fan action. This paper studies the various systems and compare the cooling performance for several conditions, based on a automotive engine. An experimental analysis was developed to predict the interaction of the fan system and the heat exchangers of the engine cooling system. The local temperature induced by the fan on the cooling system is measured. These experimental result were accomplished using airflow management techniques.

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Contaminant Release from and Oxygen Uptake Rate of Landfill Soils of Different Age (비위생매립지 토양의 매립종료기간에 따른 오염특성 및 산소소비율 평가)

  • 신언빈;김종호;배우근
    • Proceedings of the Korean Society of Soil and Groundwater Environment Conference
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    • 2001.09a
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    • pp.57-60
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    • 2001
  • 미생물 활성도와 그에 따른 유기물의 분해율은 미생물의 호흡률과 직접적인 관계가 있다. 본 연구는 매립종료후 경과기간이 1년인 Y 매립지와 10년인 C 매립지의 오염특성을 조사하였고, 오염토양 미생물의 산소소비속도를 이용하여 매립종료기간에 따른 오염토양의 산소소비율을 비교 평가 하고자 하였다. C 매립지의 오염토양에 대한 SCO $D_{cr}$ TOC는 Y 매립지에 비해 낮은 함량으로 나타났으나 T-N, N $H_3$-N의 함량은 큰 차이를 보이지 않았다. TOC/T-N비로 보았을 때 Y 매립지에 비해 C 매립지가 낮은 것으로 나타나 연령이 많은 경우 분해성 유기물의 함량은 적은 것으로 판단된다. 산소소비율 실험결과 Y 매립지가 산소소비율이 높은 것으로 나타났으며, C 매립지도 대조토양에 비해 높은 산소소비율을 보였다. 따라서 매립종료 후 경과기간이 10년인 매립지의 미생물의 산소소비율을 보았을 때 여전히 생물학적 안정화가 종료되지 않은 것을 알 수 있었다.

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Preparation and Drug-releasing Properties of Chitosan-based Thermosensitive Composite Hydrogel

  • Li, Heping;Yu, Tao;Li, Shan;Qin, Long;Ning, Jingheng
    • Journal of the Korean Chemical Society
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    • v.56 no.4
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    • pp.473-477
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    • 2012
  • The novel chitosan-based thermosensitive hydrogels were prepared as control-releasing drug carriers. N-carboxyethyl chitosan (ACS) was synthesized by microwave heating for 1 h through Michael addition of CS to acrylic acid in a grafting yield of 52.97%, which was proved to be a faster and more efficient way than ordinary methods. 5-Fu was modified with formaldehyde to synthesize N,N'-Bis(hydroxymethyl)-5-fluorouracil (5-Fu-OH). Then an esterification was performed using ACS and 5-Fu-OH to give 5-Fu-ACS. The new thermosensitive hydrogels were prepared by adding sodium glycerophosphate to the solution of compounds under a certain constant temperature. Simultaneously, the hydrogels' swelling rate, in vitro drug release rate and thermosensitive were studied, and found that the 5-Fu-ACS composite hydrogel had more excellent releasing effect, higher drug loading and better thermosensitive.

Hydrogen Absorption at a Low Temperature by MgH2 after Reactive Mechanical Grinding

  • Song, Myoung Youp;Lee, Seong Ho;Kwak, Young Jun;Park, Hye Ryoung
    • Korean Journal of Materials Research
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    • v.24 no.3
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    • pp.129-134
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    • 2014
  • Pure $MgH_2$ was milled under a hydrogen atmosphere (reactive mechanical grinding, RMG). The hydrogen storage properties of the prepared samples were studied at a relatively low temperature of 423 K and were compared with those of pure Mg. The hydriding rate of the Mg was extremely low (0.0008 wt% H/min at n = 4), and the $MgH_2$ after RMG had higher hydriding rates than that of Mg at 423 K under 12 bar $H_2$. The initial hydriding rate of $MgH_2$ after RMG at 423 K under 12 bar $H_2$ was the highest (0.08 wt% H/min) at n = 2. At n = 2, the $MgH_2$ after RMG absorbed 0.39 wt% H for 5 min, and 1.21 wt% H for 60 min at 423K under 12 bar $H_2$. At 573 K under 12 bar $H_2$, the $MgH_2$ after RMG absorbed 4.86 wt% H for 5 min, and 5.52 wt% H for 60 min at n = 2. At 573 K and 423 K under 1.0 bar $H_2$, the $MgH_2$ after RMG and the Mg did not release hydrogen. The decrease in particle size and creation of defects by reactive mechanical grinding are believed to have led to the increase in the hydriding rate of the $MgH_2$ after RMG at a relatively low temperature of 423 K.

Endoplasmic Reticulum Ca2+ Store: Regulation of Ca2+ Release and Reuptake by Intracellular and Extracellular Ca2+ in Pancreatic Acinar Cells

  • Kang, Yun Kyung;Park, Myoung Kyu
    • Molecules and Cells
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    • v.19 no.2
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    • pp.268-278
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    • 2005
  • We investigated the effect of cytosolic and extracellular $Ca^{2+}$ on $Ca^{2+}$ signals in pancreatic acinar cells by measuring $Ca^{2+}$ concentration in the cytosol($[Ca^{2+}]_c$) and in the lumen of the ER($[Ca^{2+}]_{Lu}$). To control buffers and dye in the cytosol, a patch-clamp microelectrode was employed. Acetylcholine released $Ca^{2+}$ mainly from the basolateral ER-rich part of the cell. The rate of $Ca^{2+}$ release from the ER was highly sensitive to the buffering of $[Ca^{2+}]_c$ whereas ER $Ca^{2+}$ refilling was enhanced by supplying free $Ca^{2+}$ to the cytosol with $[Ca^{2+}]_c$ clamped at resting levels with a patch pipette containing 10 mM BAPTA and 2 mM $Ca^{2+}$. Elevation of extracellular $Ca^{2+}$ to 10 mM from 1 mM raised resting $[Ca^{2+}]_c$ slightly and often generated $[Ca^{2+}]_c$ oscillations in single or clustered cells. Although pancreatic acinar cells are reported to have extracellular $Ca^{2+}$-sensing receptors linked to phospholipase C that mobilize $Ca^{2+}$ from the ER, exposure of cells to 10 mM $Ca^{2+}$ did not decrease $[Ca^{2+}]_{Lu}$ but rather raised it. From these findings we conclude that 1) ER $Ca^{2+}$ release is strictly regulated by feedback inhibition of $[Ca^{2+}]_c$, 2) ER $Ca^{2+}$ refilling is determined by the rate of $Ca^{2+}$ influx and occurs mainly in the tiny subplasmalemmal spaces, 3) extracellular $Ca^{2+}$-induced $[Ca^{2+}]_c$ oscillations appear to be triggered not by activation of extracellular $Ca^{2+}$-sensing receptors but by the ER sensitised by elevated $[Ca^{2+}]_c$ and $[Ca^{2+}]_{Lu}$.

Prediction of Nitrogen Loading from Forest Stands in Eutrophication of Lake (호소 부영양화에 있어서 산림임반으로부터 질소부하 평가를 위한 조사)

  • Chung, Doug-Young;Lee, Young-Han;Lee, Jin-Ho;Park, Mi-Suk
    • Korean Journal of Soil Science and Fertilizer
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    • v.43 no.4
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    • pp.430-437
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    • 2010
  • The continuous release of nutrient sources into natural water resource can be a continuing problem in eutrophication, as well as severe reductions in water quality. However, any desirable measure is not developed yet even though so many researches and efforts have been done to solve this problem. Forest as one of troublesome nonpoint sources may contributes most to nutrient loading, but the loading of N and P from forest in order to grasp the eutrophication potential of nonpoint sources has not been evaluated. The nutrient sources from the organic litter accumulated on the surface of forest soils can be a critical factor in continuity of eutrophication of a lake. The decomposition rate of litter can be estimated to predict release of N and P from the forest stand. The loss rate of nitrogen is complicated but depends in part upon the physical matrix of the element. Therefore, long-term nutrient budget and flux estimates at stand would be useful tools in calculating potential nutrient fluxes into the watercourses in a sustainable way. The present investigation can give insight to the actual situation of the eutrophication potentials of forest as the practical nonpoint sources.

Evaluation of Fatigue Crack Propagation Depending on Fiber Array Direction in Woven CFRP Composites (평직 CFRP 복합재료의 섬유 배열각도별 피로 균열 성장 평가)

  • Geum, Jin-Hwa;Choi, Jung-Hun;Park, Hong-Sun;Koo, Jae-Mean;Seok, Chang-Sung
    • Transactions of the Korean Society of Mechanical Engineers A
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    • v.34 no.6
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    • pp.717-723
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    • 2010
  • Many researchers have studied woven fabric carbon-fiber-reinforced composite (CFRP) materials but the study of fatigue crack propagation in composites has been insufficient. It has known that the crack propagation behavior differs depending on the load and the fiber direction. In this study, the fatigue crack propagation along two different fiber array directions ($0^{\circ}$, $45^{\circ}$) in plain woven CFRP composite was investigated. Fatigue crack propagation tests were conducted on the woven CFRP composite under a sinusoidal waveform load with stress ratios of 0.1 at a frequency of 10 Hz. Once the results of the tests were obtained, fatigue crack propagation rates (da/dN) were plotted against the energy release rate amplitude (${\Delta}G$), and it was observed that either mode I crack propagation or mixed mode crack propagation occurs depending on the fiber array direction.

A Study on the Characteristics of Ignition and Combustion, in a Diesel Spray Using Multi-Component Mixed Fuels (다성분 혼합연료를 이용한 디젤분무의 착화연소특성에 관한 연구)

  • Yoon, Jun-Kyu;Lim, Jong-Han
    • Journal of Energy Engineering
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    • v.16 no.3
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    • pp.120-127
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    • 2007
  • The purpose of this study is experimentally to analyze that the fuel mass fractions of multi-component mixed fuels have an effect on the characteristics of spray ignition and combustion under the ambient conditions of diesel combustion fields. The characteristics of ignition and combustion were investigated by chemiluminescence images and direct photography. The experiments were conducted in the RCEM(rapid compression expansion machine) with optical access. Multi-component fuels mixed with i-octane, n-dodecane and n-hexadecane are injected in RCEM by the electronic control of common rail injector. Experimental conditions set up 42, 72 and 112 MPa in injection pressure, 700, 800 and 900 K in ambient gas temperature. The results show that the ignition delay was dependent on high cetane number. In case of low ambient temperature, the more low boiling point fuels were mixed, the lower luminance regime had a remarkable effect and also shortened diffusion combustion by increasing heat release rate.