• Title/Summary/Keyword: non-steroidal

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Simultaneous Chiral Discrimination of Nine Non-Steroidal Antiinflammatory Drugs by Cyclodextrin-Modified Capillary Electrophoresis in Normal and Reversed Polarity Modes

  • Kim, Ji-Yung;La, Sook-Ie;Kim, Jung-Han;Kim, Kyoung-Rae
    • Proceedings of the PSK Conference
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    • 2003.04a
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    • pp.276.2-276.2
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    • 2003
  • Simultaneous enantioseparation of nine racemic non-steroidal antiinflammatory drugs (NSAIDs) for their accurate chiral discrimination was achieved by cyclodextrin (CO) modified capillary electrophoresis in the normal polarity (NP) mode and in the reversed polarity (RP) mode. The NP mode employed neutral tri-O-methyl-${\beta}$-cyclodextrin (TM${\beta}$CD) as a selector dissolved in MES buffer (PH 6.0). (omitted)

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Inhibition of Human Leukocyte Cathepsin G by NSAIDs (Non-Steroidal Anti-Inflammatory Drugs) (NSAIDs (Non-Steroidal Anti-Inflammatory Drugs)에 의한 사람 중성구 Cathepsin G의 활성도 억제)

  • Bae, Sung-Jun;Ghim, Sa-Youl;Kang, Koo-Il
    • The Korean Journal of Pharmacology
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    • v.26 no.1
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    • pp.51-54
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    • 1990
  • Human leukocyte cathepsin-Gs are active participant in the active phase of inflammations like rheumatoid arthritis, emphysema and glomerular injury. Non-steroidal anti-inflammatory drugs (NSAIDs) are widely used for treatment of these inflammatory diseases. Mechanism of action of NSAIDs for treatment of inflammatory diseases, especially like rheumatoid arthritis, are known as the inhibitors of prostaglandin synthesis. Inhibitions of the activities of human leukocyte cathepsin-Gs by non-steroidal anti-inflammatory drugs, however, were not same as the known pharmacological effects (inhibition of cyclooxygenase) of these drugs. Among them, especially, sulindac, salicylate, phenylbutazone, oxyphenbutazone, and salicyluric acid inhibited human leukocyte cathepsin-Gs effectively. $IC_{50}s$ of each drug were 4.3mM, 14.3mM, 6.5mM, 11mM and 15mM respectively. The drugs which have same chemical structure and same degree of inhibition effect on cyclooxygenase showed different degree or no effect on inhibition of cathepsin G. These inhibition effect might be, beside of inhibition of cyclooxygenase in the prostaglandin synthesis pathway, another benefitial antiinflammatory effect of NSAIDs by direct protection against tissue destruction in inflammatory diseases.

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Simultaneous Analysis of Several Non-Steroidal Anti-Inflammatory Drugs in Urine by Gas Chromatograph/Negative Chemical Ionization-Mass Spectrometry (기체 크로마토그래프-질량분석법을 이용한 뇨중 비스테로이드성 소염진통제 (NSAIDs)의 동시 분석법)

  • Myung, Seung-Woon;Park, Joon-Ho;Kim, Myung-Soo;Cho, Hyun-Woo
    • Analytical Science and Technology
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    • v.12 no.6
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    • pp.571-576
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    • 1999
  • Screening method for NSAIDs (Hon-Steroidal Anti-Inflammatory Drugs) in urine was developed using GC/NCI-MS. Derivatized six fenamates with pentafluoropropionic anhydride showed high sensitivity in NCI-MS. The conditions of the derivatization reaction and chromatographic conditions were established for screening with a trace analysis. Limit of detection was in the range of 4-25 pg/mL. This method may be used to the equine doping analysis for NSAIDs and forensic analysis.

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Prasaplai: An essential Thai traditional formulation for primary dysmenorrhea treatment

  • Tangyuenyongwatana, Prasan;Gritsanapan, Wandee
    • CELLMED
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    • v.4 no.2
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    • pp.10.1-10.8
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    • 2014
  • Affecting more than half of menstruating women, dysmenorrhea is a cramp which causes abdominal or lower back pain just before or during a menstruation. In western medicine, non-steroidal anti-inflammatory drugs (NSAIDs) are normally used to treat primary dysmenorrheal symptoms. Despite their rapidity in relieving pain, NSAIDs have many serious side effects on the liver, kidney, and gastrointestinal tract. Thai traditional medicines comprise many preparations for treating dysmenorrhea, especially Prasaplai preparation which has been listed in the Thai traditional common household drug list since 2006. The use of Prasaplai was originated about 100 years ago and is still being used in the present time to treat dysmenorrhea. This review focuses on the history of the preparation, active ingredients, and biological activities especially on cyclooxygenase inhibitor, artifacts occurred in the preparation, quantitative analysis, and clinical trial of Prasaplai formulation.

High Performance Liquid Chromatographic Assay of Non-steroidal Anti-inframmatory Drugs in Plasma (혈장중 비스테로이드성 소염진통제의 HPLC분석)

  • Baek Chai-Sun
    • Korean Journal of Clinical Pharmacy
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    • v.5 no.2
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    • pp.71-74
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    • 1995
  • A high performance liquid chromatographic method has been developed for the simultaneous analysis of non-steroidal anti-inflammatory drugs in plasma. The simultaneous determination of ibuprofen, fenoprofen and ketoprofen is performed by RP-HPLC with UV detection. The chromatographic system consisted of Spherisorb octyl column$(5{\mu}m)$ ; the mobile phase was $acetonitrile\;-\;0.5\%$ phosphoric acid(55 : 45, v/v) and the detection wavelength was 230nm. Tolmetin was employed as an internal standard. The method described is rapid and simple with sensitivity limits of $2.0{\mu}g/ml$ ibuprofen, $0.5{\mu}g/ml$ fenoprofen and $0.3{\mu}g/ml$ ketoprofen and is suitable for routine clinical and pharmacokinetic studies.

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Facile Synthesis of 2-(p-Methylallylaminophenyl)propionic Acid (Alminoprofen) (2-(p-메틸알릴아미노페닐)프로판산의 합성)

  • Choi, Hong-Dae;Yun, Ho-Sang;Kang, Byung-Won;Ma, Jung-Joo;Son, Byeng-Wha
    • YAKHAK HOEJI
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    • v.36 no.1
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    • pp.12-16
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    • 1992
  • A new method for the synthesis of alminoprofen, which is a non-steroidal antiinflammatory agent, was described. Ethyl 2-phenyl-propionate(4) was prepared by Friedel-Crafts reaction of benzene with ethyl ${\alpha}-chloro-{\alpha}(methylthio)acetate(1)$, followed by methylation and desulfurization of the resultant ethyl 2-(methylthio)phenylacetate(2). Ethyl 2-(p-aminophenyl)propionate(6) was obtained by nitration of (4) and successive reduction of ethyl 2-(p-nitrophenyl)propionate(5). Alminoprofen was synthesized by reaction of (6) with methallyl chloride, followed by hydrolysis of the resultant ethyl 2-(p-methylallylaminophenyl)propionate (7).

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Acute kidney injury caused by administration of zaltoprofen in a cat

  • Baek, Woon-Bum;Kim, Hak-Hyun;Kang, Byeong-Teck;Kang, Ji-Houn;Yang, Mhan-Pyo
    • Korean Journal of Veterinary Research
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    • v.57 no.1
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    • pp.55-57
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    • 2017
  • A 5-year-old, 2.7 kg, spayed female Scottish Fold cat presented with hematemesis after administration of oral zaltoprofen, a non-steroidal anti-inflammatory drug, by the owner. Diagnostic imaging and blood analyses indicated development of acute kidney injury (AKI) resulting from zaltoprofen ingestion. To correct dehydration and anemic conditions, the cat received intravenous fluid therapy with whole blood transfusion and peroral N-acetylcysteine. Clinical signs resolved, but persistent azotemia was unresolved indicating that AKI could progress to chronic kidney disease. This case suggests that although zaltoprofen may have low adverse effects on humans, administration of zaltoprofen in cats can have serious adverse effects.

Rapid Gas Chromatographic Profiling and Screening of Acidic Non-Steroidal Antiinflammatory Drugs in Biological Samples

  • Kim, Kyoung-Rae;Shin, You-Jin;Shim, Won-Hee;Myung, Seoung-Won
    • Archives of Pharmacal Research
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    • v.17 no.3
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    • pp.175-181
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    • 1994
  • The solid-phase extraction (SPF) with subsequent tert-butyldimethylsilyl (TBDMS) derivatization was investigated for the rapid profiling and screening of various carboxylated non-steroidal antiinflammatory drugs (NSAIDs) simultaneously in biological fluid samples. Compared to the conventional SPF in adsorption mode using Chromosorb 102, Chromosorb 107, Carbopak B and Thermosorb, the SPF in partition mode using Chromosorb P as the adsorbent, and ethyl acetate/methylene chloride as the eluting solvents provided hightest overall recovenies of the NSAIDs from aqueous solutions with good precision. The solid-phase extracted NASIDs were silylated with N-methyl-N-(tert-butyldimethylsily)trifuoroacetamide to TBDMS derivatives and directly analyzed by capillary gas chromatography and gs chromatography-mass spectrometry. The usefulness of the present method was examined for the profilling and screening of saliva, serum and urine samples for various NSAIDs simultaneously.

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Effect of Glutamine on the Diclofenac Induced Bacterial Translocation and Lipid Peroxidation (Diclofenac에 의해 유발된 장내세균전위와 지질과산화에 대한 글루타민의 효과)

  • Kim, Eun-Jeong;Kim, Jeong-Wook
    • YAKHAK HOEJI
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    • v.49 no.2
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    • pp.128-133
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    • 2005
  • The aim of this study was to examine whether administration of glutamine are able to prevent the NSAID induced bacterial translocation and lipid peroxidation in the rats. The an imals with glutamine were fed with L-glutamine for 5 days before diclofenac administration (100 mg/kg orally). 48 hour after diclofenac administration, intestinal permeability, serum biochemical profiles, and malondialdehyde levels of ileum were measured for evaluation of gut damage. Also, enteric aerobic bacterial counts, number of gram-negatives in mesenteric Iymph nodes, liver, spleen and kidney and malondialdehyde levels in liver, spleen, kidney and plasma were measured. Diclofenac caused the gut damage, enteric bacterial overgrowth, increased bacterial translocation and increased lipid peroxidation. Co-administration of glutamine reduced the gut damage, enteric bacterial overgrowth, bacterial translocation and lipid peroxidation induced by diclofenac. This study suggested that glutamine might effectively prevent non-steroidal anti-inflammatory drug induced bacterial translocation and lipid peroxidation in the rat.

The Crystal Structure of Cinmetacin ($C_{21}H_{19}NO_4$), A Non-steroidal Antiinflammatory Agent

  • Kim, Yang-Bae;Park, Il-Yeong;Park, Yang-Hwan
    • Archives of Pharmacal Research
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    • v.12 no.1
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    • pp.52-57
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    • 1989
  • The structure of cinmetacin was determined by single crystal X-ray diffraction analysis. The compound was recrystallized from a mixture of acetone and water in orthorhombic, space group $P2_12_12_1$, with Z=4, a=35.681(8), b=9.482(2), c:5.071(1) ${\AA}$, $D_x=1.352 g/cm^3$, and $D_m=1.35g/cm^3$. The structure was solved by direct method and refined by least-squares procedure to the final R value of 0.036 for 1441 observed reflections ($F{\geq}3{\sigma}(F)$). The carboxyl group of the molecule is nearly perpendicular to the indole ring. The dihedral angle between indole ring and phenyl group is $64.5^{\circ}$. The molecules are linked together via O(1)-H ----O(3) hydrogen bonds, and arranged along 2-fold screw axis in the crystal. The intermolecular contacts are the normal van der Waals' forces.

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