• 제목/요약/키워드: N release rate

검색결과 245건 처리시간 0.024초

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

  • 서보연;박기배;이광표
    • Journal of Pharmaceutical Investigation
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    • 제26권2호
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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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흰쥐 해마에서 Norepinephrine 유리에 미치는 Adenosine Receptor의 Post-Receptor 기전에 관한 연구 (A Study on the Post-Receptor Mechanism of Adenosine Receptor on Norepinephrine Release in the Rat Hippocampus)

  • 최봉규;김도경;양경무
    • 대한약리학회지
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    • 제32권1호
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    • pp.1-11
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    • 1996
  • 흰쥐 해마(hippocampus)에서 norepinephrine(NE) 유리에 미치는 $A_1-adenosine$ 수용체의 post-receptor 기전에 관한 지견을 얻고자 하여 $^3H-norepinephrine$으로 평형시킨 해마 절편을 사용하여 adenosine의 $^3H-NE$ 유리에 미치는 여러가지 약물의 영향을 관찰하였다. Adenosine($1{\sim}30{\mu}M$)은 전기자극(3 Hz, 2 ms, 5 Vcm-1, 구형파)에 의한 NE 유리를 용량 의존적으로 감소시켰고, 이 효과는 선택적인 $A_1-adenosine$ 수용체 차단제인 $8-cyclopentyl-1,3-dipropylxanthine(2{\mu}M)$에 의해 차단되었다. G-단백 억제제인 N-ethylmaleimide(NEM, 10과 $30{\mu}M$)는 그 자체로써 전기자극으로 유발시킨 NE 유리를 증가시켰으며, adenosine의 NE 유리 억제효과는 NEM 전처리에 의하여 완전히 소실되었다. Protein kinase C 활성화제인 $4{\beta}-phorbol$ 12,13-dibutyrate(PDB, $1{\mu}M$)는 NE 유리 증가를 일으켰고, 이 효소 억제제인 $4{\beta}-polymyxin$ B(PMB, 0.1 mg)는 NE 유리감소를 일으켰으며, adenosine에 의한 NE 유리 감소효과는 PDB에 의해 억제되었고, PMB 전처리하에서는 감소효과가 출현하지 않았다. $Ca^{2+}$-통로 차단제인 $nifedipine(1{\mu}M$)은 adenosine의 NE 유리 억제효과에 영향을 미치지 못하고, ATP에 의존적인 $K^+-$통로 차단제인 glibenclamide역시 adenosine의 NE 유리 억제효과에 영향을 미치지 못하였다. 그러나 delayed rectifier $K^+-$통로 차단제인 tetraethylammonium(TEA, 3 mM)은 그 자체로 NE 유리를 증가 시켰으며, adenosine의 NE 유리 억제효과를 차단함을 볼 수 있었다. 8-bromo-cAMP(100과 $300{\mu}M$) 그 자체로는 NE 유리에 별다른 영향을 미치지 못하였으나 8-bromo-cAMP 전처리에 의하여 adenosine의 NE 유리 억제효과가 억제됨을 볼 수 있었다. 이상의 실험결과로 흰쥐 해마에서 $A_1-adenosine$ 수용체를 통한 adenosine의 NE 유리 감소는 G-단백에 의존적이며, 이러한 효과에 protein kinase C, TEA에 예민한 $K^+-$통로 및 adenylate cyclase계가 복합적으로 관여하고 nifedipine에 예민한 $Ca^{2+}-$통로와 glibenclamide에 예민한 $K^+-$통로는 관여하지 않는 것으로 사료된다.

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

  • 김진현;이해철;이민호;박종남;차경옥
    • 대한기계학회:학술대회논문집
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    • 대한기계학회 2001년도 추계학술대회논문집B
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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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비위생매립지 토양의 매립종료기간에 따른 오염특성 및 산소소비율 평가 (Contaminant Release from and Oxygen Uptake Rate of Landfill Soils of Different Age)

  • 신언빈;김종호;배우근
    • 한국지하수토양환경학회:학술대회논문집
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    • 한국지하수토양환경학회 2001년도 추계학술발표회
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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
    • 대한화학회지
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    • 제56권4호
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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
    • 한국재료학회지
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    • 제24권3호
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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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    • 제19권2호
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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 $[Ca^{2+}]_{Lu}$.

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

  • 정덕영;이영한;이진호;박미숙
    • 한국토양비료학회지
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    • 제43권4호
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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.

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

  • 금진화;최정훈;박홍선;구재민;석창성
    • 대한기계학회논문집A
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    • 제34권6호
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    • pp.717-723
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    • 2010
  • 많은 연구자들이 평직 탄소섬유강화플라스틱에 대해서 연구해왔지만 피로 균열 진전에 관한 연구는 아직도 미지한 상태이다. 그리고 하중과 섬유 배열 각도에 따라 균열 진전 양상이 다름을 알 수 있다. 본 연구에서는 서로 다른 두 개의 섬유 배열각도($0^{\circ}$, $45^{\circ}$)에서 평직 탄소섬유강화플라스틱의 피로 균열 진전에 대해 연구하였다. 평직 탄소섬유강화플라스틱의 피로 균열 진전 테스를 하중비 0.1에 10Hz로 수행하였다. 그 시험 결과로써, 피로 균열 진전 속도(da/dN)와 에너지해방률(${\Delta}G$)과의 그래프를 도출하였고, 섬유 배열 각도에 따른 균열 진전 양상을 $0^{\circ}$의 경우에는 Mode I를 적용하였고, $45^{\circ}$의 경우에는 Mixed Mode를 적용하였다.

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

  • 윤준규;임종한
    • 에너지공학
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    • 제16권3호
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    • pp.120-127
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    • 2007
  • 본 연구의 목적은 디젤연소장의 분위기조건에 따라 다성분 혼합연료의 질량분률이 분무착화 및 연소특성에 미치는 영향을 실험적으로 고찰하는데 있다. 착화 및 연소특성은 화학발광계측법 및 직접촬영법을 이용하여 분석되었다. 실험은 광계측기를 사용하여 RCEM에서 이루어졌으며, 이소옥탄, 노말 도데칸, 노말 헥사데칸으로 혼합한 다성분연료는 커먼레일 인젝터의 전자제어에 의해 RCEM의 연소실 내로 분사된다. 실험조건은 분사압력 42, 72, 112 MPa과 분위기온도 700, 800, 900 K로 하였다. 그 결과로서 착화지연은 고세탄가성분에 의존하고, 분위기온도가 낮을 경우 저비점성분 혼합비율의 증가에 따라 휘도영역이 현저하게 낮아지며, 열발생률이 증가하면서 확산연소기간을 단축시킨다.