• Title/Summary/Keyword: naproxen

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Preparation of a New Chiral Stationary Phase Bearing Both $\pi$-Acidic and -Basic Sites from (S)-Naproxen for the Liquid Chromatographic Resolution of Enantiomers

  • Hyun Myung Ho;Jin Jong Sung;Ryoo Jae-Jeong;Jyung Kyung Kyu
    • Bulletin of the Korean Chemical Society
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    • v.15 no.6
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    • pp.497-502
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    • 1994
  • A new chiral stationary phase (CSP) for the liquid chromatographic resolution of enantiomers was prepared from (S)-naproxen and 3,5-dinitroaniline. The 6-alkoxy-2-naphthyl group of the CSP was presumed to act as a ${\pi}$-basic interaction site for resolving ${\pi}$-acidic racemates while the 3,5-dinitroanilide group of the CSP was presumed to play a role as a ${\pi}$-acidic interaction site for resolving ${\pi}$-basic racemates. From the chromatographic resolution trends of N-alkylamide derivatives of ${\alpha}$-arylalkylamines on the CSP prepared, the chiral recognition mode involving the intercalation of the amide alkyl chain of the less retained enantiomers between the connecting tethers of the CSP was proposed.

Effect of Phenobarbital on the Nonlinear Pharmacokinetics of Naproxen (나프록센의 비선형 체내동태에 미치는 페노바르비탈의 영향)

  • Lee, Yong-Bok;Chae, Myung-Ae;Koh, Ik-Bae
    • Journal of Pharmaceutical Investigation
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    • v.27 no.2
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    • pp.109-117
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    • 1997
  • In order to elucidate the effect of phenobarbital (PB) on the nonlinear pharmacokinetic behavior of naproxen (NAP), we compared the dose dependent hepatic intrinsic clearance, biliary excretion and protein binding of NAP in control rats to those in the PB-pretreated rats which were intraperitoneally pretreated with PB sodium (75 mg/kg) once a day for four days. NAP was injected via femoral (1.5 mg/kg) and portal(0.25, 0.5, 1.5, 15 and 30 mg/kg) vein to the control and PB-pretreated rats, respectively. And also, we measured the plasma free fraction of NAP with the equilibrium dialysis method and the biliary excreted total amounts of NAP in both rats. Plasma free fraction of NAP was decreased in lower concentration than $150\;{\mu}g/ml$ of NAP due to PB pretreatment. In higher concentration, however, plasma free fraction was increased. These in vitro results suggest that the total protein concentration was increased but the total binding capacity of NAP to protein was decreased by PB-pretreatment. The total plasma clearance and the hepatic intrinsic clearance of NAP had similar values in both groups, respectively. And, both clearances of NAP were significantly increased by PB-pretreatment. Even though the plasma free fractions of NAP in both groups were constantly remained within the concentration range according to the increase of administration dose, the hepatic intrinsic clearances of NAP were significantly increased in both groups with the increased dose. And, the biliary excreted total amounts of NAP were significantly increased by PB-pretreatment at the lower dose, but decreased at the higher dose. These in vivo results suggest that NAP represents the uncommon nonlinear pharmacokinetic behavior that the hepatic intrinsic clearance was enhanced with the increased dose, and that PB enhances further the hepatic intrinsic clearance of NAP with the increased dose due to its enzyme induction effect.

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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.

Evaluation on the removal efficiency of pharmaceutical compounds in conventional drinking water treatment processes (정수처리 공정에서 잔류의약물질 제어 효율 평가)

  • Seo, Hee-Jeong;Park, Yong-Hoon;Kang, In-Sook;Myong, Hwa-Bong;Song, Yang-Suk;Kang, Yeong-Ju
    • Analytical Science and Technology
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    • v.29 no.3
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    • pp.126-135
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    • 2016
  • In the present study, we evaluated the efficiency of the drinking water treatment unit processes controlled by targeting high pharmaceutical compounds that are likely to be released into the water supply. In the coagulation process, the removal rate of sulfonamide, an antibiotic, amounted to 22.6~42.1 %, that of naproxen to 28.2 %, and that of acetaminophen to 20 %. Trimethoprim has demonstrated a low removal rate (4.4 %), while the removal rate of erythromycin was 2.4 %; aspirin was not removed at all. When applying a mixture of chlorination and the coagulation process, the removal rate was increased with increasing the chlorine dosage. When the chlorine injection with the concentration of 3 mg/L was applied, sulfonamide antibiotics, acetaminophen and naproxen, were completely removed. Trimethoprim exhibited a high removal efficiency of ca. 98%, while the removal efficiency of erythromycin was about 55 %; at the same time, aspirin showed a lower removal ratio (ca. 10 %). When applying the powdered activated carbon adsorption process, the removal rate was increased with increase of the concentration of the powder activated carbon injection. Sulfonamide antibiotics showed about 18~50 % removal efficiency in the 1 mg/L, the removal rate was increased by at least 80 % in 25 mg/L. The evaluation results of the titration injection concentration of chlorine treatment and adsorption, coagulation process for the efficient processing of the remaining pharmaceutical compounds in the water treatment process, when applying the chlorine 3 mg/L, powdered activated carbon 10 mg/L and coagulant 15 mg/L were removed more than 90 %.

Preparation and Drug Release Properties of Naproxen Imprinted Biodegradable Polymers Based Multi-Layer Biomaterials (나프록센이 각인된 생분해성 고분자 기반 다층 바이오소재의 제조 및 약물 방출 특성)

  • Eun-Bi Cho;Han-Seong Kim;Min‑Jin Hwang;Soon-Do Yoon
    • Applied Chemistry for Engineering
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    • v.34 no.2
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    • pp.161-169
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    • 2023
  • In this study, we prepared naproxen (NP) imprinted biodegradable polymer based multi-layer biomaterials using allbanggae starch (ABS), polyvinyl alcohol (PVA), and alginic acid (SA), and investigated their physicochemical properties and the controlled drug release effects. In addition, the prepared multi-layer biomaterials were characterized by FE-SEM and FT-IR. In order to confirm the controlled drug release effect for the transdermal drug delivery system (TDDS), the NP release properties of NP imprinted multi-layer biomaterials were investigated using various pH buffer solutions and artificial skin at 36.5 ℃. The results of NP release in various pH buffer solutions indicated that the NP release at high pH was about 1.3 times faster than that at low pH. In addition, NP release in multi-layer biomaterials was about 4.0 times slower than that in single-layer biomaterials. It was confirmed that the NP release rate in triple-layer biomaterials was 4.0 times slower than that in single-layer biomaterials while using artificial skin. Also, it could be found that NP in double-layer biomaterials and triple-layer biomaterials was released sustainably for 12 h. The NP release mechanism in pH buffer solutions followed the Fickian diffusion mechanism, but followed the non-Fickian diffusion mechanism with artificial skin.

Development of Antiinflammatory Agents(II) - Fused Heterocycles - (소염진통제 개발 (II) - 접합 헤테로고리 화합물 -)

  • 박노상;김현숙;임희종;정영식;최중권;함원훈
    • YAKHAK HOEJI
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    • v.35 no.2
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    • pp.73-84
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    • 1991
  • Quinoline, pyrazolo-[5, 4-b]-pyridine, isoxazolo-[5, 4-b]-pyridine, pyrazolo-[4, 3-c]-quinoline, isoxazolo-[5, 4-e]-thiazine, and isothiazolo-[5, 4-e]-thiazine derivatives were prepared as possible antiinflammatory agents. Some of the synthesized compounds showed antiinflammatory activities comparable to Aspirin and Naproxen.

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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%).

Pharmaceutical Studies on the Inclusion Complexes of Non-Steroidal Antiinflammatory Drugs with ${\beta}-Cyclodextrin$ (I) (비(非)Steroid 성소염약물(性消炎藥物)과 ${\beta}-Cyclodextrin$과의 Inclusion Complex에 관(關)한 약제학적(藥劑學的) 연구(硏究) (제1보)(第一報))

  • Han, Kun;Lee, Min-Hwa;Kim, Shin-Keun
    • Journal of Pharmaceutical Investigation
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    • v.13 no.1
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    • pp.10-22
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    • 1983
  • The interactions of ${\alpha}-cyclodextrin({\alpha}-CyD)$ and ${\beta}-cyclodextrin({\beta}-CyD)$ with several non-steroidal antiinflammatory drugs were studied on the effects of ${\alpha}-$ and ${\beta}-CyD$ on the solubility of the drugs in aqueous medium. Indoprofen, niflumic acid, alclofenac, and naproxen were chosen as representatives of antiinflammatory drugs. The solubility of all drugs studied increased with the addition of ${\beta}-CyD$, while not with glucose or ${\alpha}-CyD$. The increase of the solubility with ${\beta}-CyD$ was considered due mainly to the formation of inclusion complexes between ${\beta}-CyD$ and drugs. From the solubility data, the apparent stability constants K of the complex could be calculated. Ultraviolet absorption and circular dichroism confirmed the inclusion of indoprofen, niflumic acid and naproxen with ${\beta}-CyD$ in the molar ratio of 1 : 1. Inclusion complexes in solid powder form were obtained by the freeze-drying method and the inclusion formation was confirmed again by infrared, diffential thermal analysis, and X-ray diffraction measurements.

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Characteristic Occurrence and Distributions of Pharmaceuticals in the Nakdong River (낙동강 수계 내 의약물질 발생 및 분포 특성)

  • Lee, Heon-Jun;Kim, Hee-Young;Kim, Ki Yong;Yang, Duk-Seok;Lee, Injung;Lim, Young-Kyong;Kim, Jae-Hyuk;Oh, Jeong-Eun
    • Journal of Korean Society of Environmental Engineers
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    • v.39 no.7
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    • pp.403-411
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    • 2017
  • In this study, the occurrence and temporal variation of eight pharmaceuticals comprising antibiotics (clarithromycin, sulfathiazole, sulfamethazine, sulfamethoxazole, trimethoprim), scabicide (carbamazepine) and nonsteroidal anti-inflammatory drugs (acetylsalicylic acid, naproxen) in main stream and its tributary of the Nakdong River basin, were investigated. Concentrations of the target compounds ranged from $1.076{\mu}g/L$. The highest average concentration was observed for clarithromycin ($0.0316{\mu}g/L$), followed by sulfamethazine ($0.0170{\mu}g/L$), sulfamethoxazole ($0.0161{\mu}g/L$), naproxen ($0.0129{\mu}g/L$), carbamazepine ($0.0093{\mu}g/L$), acetylsalicylic acid ($0.0047{\mu}g/L$), sulfathiazole ($0.0024{\mu}g/L$) and trimethoprim ($0.0022{\mu}g/L$). The decreasing pattern of pharmaceutical concentrations was observed along with Nakdong River and the higher concentrations in downstream were observed than those in upstream. There was no temporal variation of the target compounds although the highest level was found in February. The calculated hazard quotients (HQs) for eight pharmaceuticals were below 1, indicating no environmental hazard in Nakdong River. However, further monitoring is still needed due to the other pharmaceuticals widely used in Korea.

Selection of analgesics for the management of acute and postoperative dental pain: a mini-review

  • Kim, Sung-Jin;Seo, Jeong Taeg
    • Journal of Periodontal and Implant Science
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    • v.50 no.2
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    • pp.68-73
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    • 2020
  • Pain management is an important part of dental practice, and dentists frequently prescribe analgesics to improve clinical outcomes. Dentists should be aware of the pharmacological characteristics of the analgesics commonly used in dentistry and should choose appropriate analgesics to treat and prevent pain associated with inflammation or surgery. In this article, we review the potential benefits and risks of the analgesics frequently used in dental practice and provide a stepwise approach for pain management.