• Title/Summary/Keyword: (S)-나프록센

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Measurement of optical purity for commercial naproxen by chiral HPLC (키랄 크로마토그래피에 의한 시판되는 나프록센의 광학순도 측정)

  • Yu, Jeong-Jae;Lee, Won-Doo;Ryoo, Jae-Jeong
    • Analytical Science and Technology
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    • v.24 no.5
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    • pp.360-367
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    • 2011
  • Optical purities of 10 commercialized naproxens prepared from eight Korean drug companies were examined by an optimized chiral HPLC condition. The Chiralcel OD-H column and ChiralHyun-LE(S)-1 column were used as chiral stationary phases and the mixed eluent of hexane/isopropanol/acetic acid as 100:2.85:0.1 was used as a mobile phase for effective enantioseparation. Optical purity values of most samples were higher than 97 percents, only one of them was about 95 percents. The average relative standard deviation of them appeared very small (0.034%).

Measurement of Optical Purity for Commercially Avialable Naproxen Sold in 2013 (2013년 시판된 나프록센의 광학순도 측정)

  • Seo, Hae Chan;Song, Jung Suk;Ryoo, Sang Hyun;Lee, Sang Heon;Ryoo, Dong Hyun;Yu, Jeong Jae;Ryoo, Jae Jeong
    • Journal of the Korean Chemical Society
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    • v.58 no.2
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    • pp.179-185
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    • 2014
  • Commercial (S)-naproxen was racemized under strong basic condition. After checking the peak position of (R)- and (S)-naproxen by analysis the recemized naproxen, optical purity of 19 commercialized naproxens sold in 2013 in Korea were examined by chiral HPLC. The Chiralcel OD-H column, ChiralHyun-LE(S)-1 column and LUX-Cellulose-1 column were used as chiral stationary phases and the mixed eluent of hexane:isopropanol:acetic acid as 100:1:0.1 was used as a mobile phase with a flow rate of 1.0 mL/min. Each data was obtained from an average value of at least three different experiments for each sample and the relative standard deviation of them appeared very small. The average optical purity values obtained from three different chiral columns were very similar and the total average optical purity value (99.32%) of nineteen commercialized naproxens used in this study were larger than those of three years ago (98.17%).

Solid Bases as Racemization Catalyst for Lipase-catalyzed Dynamic Kinetic Resolution of Naproxen 2,2,2-Trifluoroethyl Thioester (리파아제에 의한 나프록센 2,2,2-트리플로로에틸 씨오에스터의 Dynamic Kinetic Resolution을 위한 라세미화 촉매로서의 고체 염기)

  • 김상범;원기훈;문상진;김광제;박홍우
    • KSBB Journal
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    • v.19 no.3
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    • pp.215-220
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    • 2004
  • A variety of solid bases such as inorganic bases, basic anion exchange resins, and resin-bound bases were tested as a catalyst for racemization of (S)-naproxen 2,2,2-trifluoroethyl thioester in isooctane at 45$^{\circ}C$. Among the various bases, DIAIOM WA30, which is a weakly basic anion exchange resin with a tertiary amine based on a highly porous type styrene-divinylbenzene copolymer, showed the highest catalytic activity. The second-order interconversion constant of DIAION WA30 was 8.6${\times}$10$\^$-4/ mM$\^$-1/h$\^$-1/ and about 3 times higher than that of trioctylamine under the same conditions. The rate of DIAION WA30-catalyzed racemization decreased with increasing an amount of water added to the reaction medium. Lipase-catalyzed kinetic resolution of racemic naproxen 2,2,2-trifluoroethyl thioester was successfully carried out under in situ racemization of substrate with DIAION WA30 in isooctane at 45$^{\circ}C$. More than 60% conversion and 99% enantiomeric excess for the desired (S)-naproxen product were obtained. Furthermore, such a solid base catalyst could be easily separated and reused in contrast to trioctylamine.

Pharmaceutical Characteristics of Korean Lumbricus rubellus Lumbrokinase (한국산 지렁이[Lumbricus rubellus]에서 분리한 Lumbrokinase의 약리학적 특성)

  • 조일환;이철규;임헌길;이형환
    • KSBB Journal
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    • v.19 no.4
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    • pp.274-283
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    • 2004
  • Six lumbrokinase (LK) fractions from Lumbricus rubellus lysates were purified by a series of column chromatographies. The molecular weights of the six LK fractions appeared to range from 24.6 to 33.1 kDa. In the experimental model of rat venous thrombosis, the thrombus weight and PAI activity decreased significantly when the LK was administered orally. However, the activities of APTT, PT and plasmin showed a significant increase. The aggregation of rat platelets pretreated with various LK doses was inhibited by thrombin, and the MDA generation decreased. The rat thoracic aorta and mesentric arteries contracted with phenylephrine relaxed due to the treatment of the LK fractions. These results suggest that the fibrinolytic effects of LK were mediated not only by proteolytic activity, but also by the inhibition of platelet agregation and the relaxation of blood vessels. It is concluded that the LK may be useful as a hemolytic agent for treatment of fibrin clot.

Biopharmaceutical Studies on the Alkanol Esters of Naproxen (II) -Pharmaceutical Characteristics of 3 Kinds of the Alkanol Esters of Naproxen- (나프록센의 Alkanol 에스테르류에 관한 생물약제학적 연구 II -3종의 Alkanol 에스테르의 약제학적 특성-)

  • 백우현;김종갑
    • YAKHAK HOEJI
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    • v.30 no.3
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    • pp.128-138
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    • 1986
  • Three newly synthesized alkanol esters of d-2-(6-methoxy-2-naphthyl) propionic acid, NAPROXEN were examined for physicochemical properties and biopharmaceutical characteristics. These esters were very stable in solid state, but more than 90% of these esters were hydrolysed to the parent, naproxen in rabbit's liver hornogenates. They showed higher dissolution rate in the artificial gastric and intestinal juice, and significantly greater partition coefficient in n-octanol, when compared with naproxen. The absorption rate constants of these esters were increased, while the elimination rate constants were decreased, comparing with naproxen. The ulcerogenic doses on gastric and intestinal mucosa were increased remarkably, and the antiinflammatory dose against carrageenininduced edema on rat hind paw was decreased markedly in these esters, and thus the safety indexes of these esters were higher than that of naproxen.

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A Methocarbamol Combination to Prevent Toxicity of Non-steroidal Anti Inflammatory Drugs (비스테로이드성 항염증제의 약물독성 예방을 위한 Methocarbamol의 약물조합)

  • Yeom, Seung-Min;Kim, Min-Seok;Lingenfelter, Eric;Broadwell, Jonathan
    • Korean Journal of Clinical Laboratory Science
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    • v.49 no.2
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    • pp.88-98
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    • 2017
  • To prevent toxicity from both robax platinum (methocarbamol, ibuprofen) and robaxacet (methocarbomol, acetaminophen), separately, we used stretches and naproxen as a non-steroidal anti-inflammatory drug (NSAID) to compare each effectiveness. This study used the United States Forces Korea Prescription form (Annex A-Over-The-Counter Prescription) and Alice Rich's Pain scale with robax platinum, robaxacet including narproxen. The IBM SPSS statics version 24 was used to calculate the data. The combined methocarbamol 500 mg, acetaminophen 325 mg tablet, and ibuprofen 200 mg (or naproxen) tablet can work as well as the combined methocarbamol 500 mg tablet with acetaminophen 325 mg tablet with stretches. Both methods were successful in managing pain. The drug combination of methocarbamol 500 mg, acetaminophen 325 mg and ibuprofen 200 mg tablets yielded similar benefits as the methocarbamol 500 mg and acetaminophen 325 mg tablets paired with physical stretching exercises regarding managing overall pain.

Quantification of Naproxen in Pharmaceutical Formulation using Near-Infrared Spectrometry (근적외 분광분석법을 이용한 나프록센 정제의 정량분석)

  • Kim Do Hyung;Woo Young Ah;Kim Hyo Jin
    • YAKHAK HOEJI
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    • v.49 no.1
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    • pp.1-5
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    • 2005
  • Near-infrared (NIR) spectroscopy has been widely applied in various field, since it is nondestructive and no sample preparation is required. In this paper, NIR spectroscopy was used for the determination of naproxen in a commercial pharmaceutical preparation. NIR spectroscopy was used to determine the content of naproxen in intact naproxen tablets containing 250 mg ($65.8\%$ nominal concentration) by collecting NIR spectra in the range of $1100{\sim}1750nm$. The laboratory-made samples had $46.1{\sim}85.5\%$ nominal naproxen concentration. The measurements were made by reflection using a fiber-optic probe and calibration was carried out by partial least square regression (PLSR). Model validation was performed by randomly splitting the data set into calibration and validation data set (63 samples as a calibration data set and 42 samples as a validation data set). The developed NIR calibration gave results comparable to the known values of tablets in a laboratorial manufacturing process with standard error of calibration (SEC) and standard error of prediction (SEP) of $1.06\%\;and\;1.04\%$, respectively. The NIR method showed good accuracy and repeatability. NIR spectroscopic determination in intact tablets allowed the potential use of real time monitoring for a running production process.

Formulation and Evaluation of Controlled Release Patch Containing Naproxen (나프록센 함유 방출제어형 패취의 제제설계 및 평가)

  • Rhee, Gye-Ju;Hong, Seok-Cheon;Hwang, Sung-Joo
    • Journal of Pharmaceutical Investigation
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    • v.29 no.4
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    • pp.343-348
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    • 1999
  • The purpose of this study is to prepare the controlled release adhesive patch containing naproxen. Pressuresensitive adhesive (PSA)-type patch was fabricated by casting of polyisobutylene (PIE.) and mineral oil in toluene. Membrane-controlled release (MCR)-type patch was prepared by the attachment of the controlled release membrane on the PSAtype patch. The membrane was mainly composed of Eudragit, polyethylene glycol(PEG) and glycerin. The drug release profile and skin permeation test with various patches were evaluated in vitro. The release of naproxen from PIE-based PSAtype patch with various loading doses fitted Higuchi's diffusion equation. However, the permeation of naproxen through hairless mouse skin from PSA-type patch followed zero-order kinetics. In MCR-type patch, thickness of controlled release membrane affected on the drug release rate highly. In the composition of membrane, the release rate was decreased as the ratio of Eudragit increased. The drug release from the MCR-type patch followed zero order kinetics. The permeation of naproxen through hairless mouse skin from MCR-type patch showed lag time for the intial release period and didn't fit the zero-order kinetics

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Physical Environmental Factors Affecting Job Satisfaction - Focused on Office Environment of Oklahoma State University′s Faculty Members- (직업 만족도에 영향을 미치는 물리적 환경 요소들 - 오클라호마 주립대학 교수의 연구환경을 중심으로 -)

  • Hye-Sun, Han
    • Korean Institute of Interior Design Journal
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    • v.13 no.5
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    • pp.206-214
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    • 2004
  • 본 연구는 사무공간에 영향을 주는 물리적 환경 요소 (공간, 가구배치, 미, 주변요소)를 제시하고 각 환경 요소들과의 관계를 파악하며 각 물리적 환경요소들과 직업 만족도 (급여, 진급, 책무, 상사와의 관계, 물리적 공간과 배치, 수업방법의 향상, 현재 직업 만족도)와의 관계를 분석하는데 연구의 목적이 있다. 또한 물리적 환경 요소들, 직업 만족도와 개인 신상 (나이, 성별, 지위, 교육수준, 교육 경력) 의 특성들과의 상관관계를 알아보고자 한다. 본 연구는 오클라호마 주립대학교의 종신 재직권을 가진 교육대학 교수들을 대상으로 세 가지 가설을 바탕으로 작성된 설문지를 배포하여 조사되었다. 각 교수들의 사무공간은 1997년에 개보수를 마치고 그 해 여름부터 사용하고 있다. 설문은 현재 사용하고 있는 사무공간에 대한 평가, 직업 만족도에 대한 평가와 개인 신상의 특성에 대한 질문으로 조사되었다. 조사 결과 사무공간에 영향을 주는 물리적 환경 요소들 간에 밀접한 관계가 있다는 가설이 입증되었고, 또한 조사 결과 물리적 환경의 만족도가 증가할수록 직업만족도가 증가하는 것으로 물리적 사무환경에 대한 만족도와 직업에 대한 만족도가 직접적인 관계가 있다는 가설 또한 확증되었다. 물리적 환경요소, 직업 만족도와 개인 신상의 특성들과의 상관관계가 있다는 가설은 전체적으로는 입증되지는 않았지만 부분적으로 요소들 간에 관계를 보여주고 있다. 남성이 여성보다 가구배치에 대해 불만족스러웠고 교육경력이 적을수록 사무공간의 냉난방과 환기에 대한 불만족을 보였다. 본 연구의 결과는 교수들의 사무환경의 부정적, 긍정적 견해를 지각하여 사무 환경의 질을 높이는데 도움이 되는데 중요한 역할을 할 수 있겠다. 본 연구는 교육대학의 교수들에 국한되어 있었던 바 추후에는 전체 교육자들을 대상으로 장기간의 관찰을 통한 연구가 요구되어 진다.신만의 고유한 해결책으로 발전시키는지를 고찰하고자 한다. 본 논문의 목적은 서울을 사례분석 중 하나로 사용하여 인테리어 디자인 분야의 경계를 대도시로 확장하는 동시에 새로운 적용영역의 가능성을 탐구하는데 있다 하겠다.[C/N]의 값을 나타내었다.다.다.화 기술, 구동방법등에 대한 기술개요와 국내외 기술동향에 대하여 소개하고자 한다.었다.다._{2}$가 0.25[wt%] 첨가된 시편의 20[.deg.C]에서의 유전상수는 16,700으로 최대값을 유전손실을 1.28[%]로 최소값을 나타내었다. 또한 모든 시편은 온도 및 주파수에 따라 유전상수가 완만하게 변화하는 유전이완 특성을 나타내었다.다.수적인 물의 양에 따른 DIAION WA30의 라세미화 효율에 관하여 실험한 결과, 물의 양이 증가할수록 그 효율은 감소하였다. DIAION WA30을 라세미화 촉매로 사용하여 아이소옥탄 내에서 라세믹 나프록센 2,2,2-트리플로로에틸 씨오에스터의 효소적 DKR 반응을 수행해 보았다. 그 결과 DIAION WA30을 사용하지 않은 경우에 비해 반응 전환율과 생성물의 광학 순도는 급격히 향상되었다. 전통적 광학분할 반응의 최대 50%라는 전환율의 제한이 본 연구에서 찾은 DIAION WA30을 첨가함으로써 성공적으로 극복되었다. 또한 고체 염기촉매인 DIAION WA30의 사용은 라세미화 촉매의 회수 및 재사용이 가능하게 해준다.해준다.다. TN5 세포주를 0.2 L 규모 (1 L spinner flask)oJl에서 세포간의 응집현상 없이 부유배양에 적응,배양시킨 후 세포성장 시기에 따른 발현을 조사한 결과 1 MOI의 감염조건 하에서는 $0.6\times10^6$cell/mL의 early exponential시기의 세포밀도에서 72시간 배양하였을 대 최대 발현양을 나타내었다. 나타내었다.

Optimization of the Reaction Conditions and the Effect of Surfactants on the Kinetic Resolution of [R,S]-Naoroxen 2,2,2-Trifluoroethyl Thioester by Using Lipse (리파아제를 이용한 라세믹 나프록센 2,2,2-트리플로로에틸 씨오에스터의 Kinetic Resolution에서 반응조건 죄적화와 계면활성제 영향)

  • Song, Yoon-Seok;Lee, Jung-Ho;Cho, Sang-Won;Kang, Seong-Woo;Kim, Seung-Wook
    • KSBB Journal
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    • v.23 no.3
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    • pp.257-262
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    • 2008
  • In this study, the reaction conditions for lipase-catalyzed resolution of racemic naproxen 2,2,2-trilfluoroethyl thioester were optimized, and the effect of surfactants was investigated. Among the organic solvents tested, the isooctane showed the highest conversion (92.19%) in a hydrolytic reaction of (S)-naproxen 2,2,2-trifluoroethyl thioester. In addition, the isooctane induced the highest initial reaction rate of (S)-naproxen 2,2,2-trifluoroethyl thioester ($V_s=2.34{\times}10^{-2}mM/h$), the highest enantioselectivity (E = 36.12) and the highest specific activity ($V_s/(E_t)=7.80{\times}10^{-4}mmol/h{\cdot}g$) of lipase. Furthermore, reaction conditions such as temperature, concentration of the substrate and enzyme, and agitation speed were optimized using response surface methodology (RSM), and the statistical analysis indicated that the optimal conditions were $48.2^{\circ}C$, 3.51 mM, 30.11 mg/mL and 180 rpm, respectively. When the optimal reaction conditions were used, the conversion of (S)-naproxen 2,2,2-trifluoroethyl thioester was 96.5%, which is similar to the conversion (94.6%) that was predicted by the model. After optimization of reaction conditions, the initial reaction rate, lipase specific activity and conversion of (S)-naproxen 2,2,2-trifluoroethyl thioester increased by approximately 19.54%, 19.12% and 4.05%, respectively. The effect of surfactants such as Triton X-100 and NP-10 was also studied and NP-10 showed the highest conversion (89.43%), final reaction rate of (S)-naproxen 2,2,2-trifluoroethyl thioester ($V_s=1.175{\times}10^{-2}mM/h$) and enantioselectivity (E = 59.24) of lipase.