• Title/Summary/Keyword: Mefenamic acid

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Effect of Surfactants on Dissolution Rate of Mefenamic Acid Capsules (메페남산 캅셀의 용출에 미치는 계면활성제의 영향)

  • Jun, Young-Bin;Kim, Seung-In;Kim, Young-Il
    • Journal of Pharmaceutical Investigation
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    • v.20 no.3
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    • pp.121-127
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    • 1990
  • Mefenamic acid has been widely used clinically as an anti-inflammatory analgesic. It has poor solubility in water $(41\;{\mu}g/ml)$ and there is the difficulty of dissolution in the mefenamic acid capsules. A study was made to investigate the effect of various surfactants on the dissolution of mefenamic acid capsules. The surfactants used were sodium lauryl sulfate (SLS), Pluronic F-68, F-77, and F-127. Mefenamic acid capsule containing surfactant showed significantly improved dissolution characteristics. The dissolution rate was fast in the order of SLS > F-77 > F-68 > F-127 in mefenamic acid capsules containing 0.2 w/w % surfactant. SLS was selected for further study on the bioavailability in rabbits. The area under the plasma concentration-time curve $(AUC_{0-24})$ of mefenamic acid capsule containing SLS was higher than one of mefenamic acid capsule not containing surfactant.

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Synthesis of Mefenamic Acid Derivatives and Antioxidative and Anticoagulant Activities

  • Cha, Bae-Cheon
    • Biomolecules & Therapeutics
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    • v.8 no.4
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    • pp.349-353
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    • 2000
  • Mefenamic acid has been widely used as clinical drug for anti-inflammatory and analgesic. This drug was known to non-steroidal anti-inflammatory drugs (NSAIDs) such as aspirin, ibuprofen and indomethacin. Although the drugs which comprise this group are of diverse chemical structures, they all share the antipyretic, analgesic and anti-inflammatory actions which are characteristic of aspirin. Action of this drugs is caused by inhibitory effect of biosynthesis of prostaglandin that are synthesized from arachidonic acid via the endoperoxide biosynthesis pathway, the initial step of which is catalysed by cyclooxygenase. Mefenamic acid has more potent inhibitory action of prostaglandin biosynthesis than aspirin. Therefore, mefenamic acid is expected to have anticoagulant activity as aspirin-like drugs. This study was carried out to investigate the sinthesis of mefenamic acid derivatives from mefenamic acid and aromatic compound of antioxidant and its antioxidative and anticoagulant activities. Synthesis of mefenamic acid derivatives was conformed by conjugation as using esterification method. Biological activities was examined using effect of anticoagulant on bleeding time and effect of antioxidant by TBA method. As a result, SJ-202 showed strong antioxidative activity and anticoagulant activity among tested 4 compounds and exhibited similar activity to aspirin at anticoagulant activity.

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Treatment of PDA in Premature Newborns with Mefenamic Acid (Mefenamic acid를 이용한 미숙아 동맥관 개존증 치험)

  • Lee, Jae-Joon;Lee, Young-Hwan;Shin, Son-Moon
    • Journal of Yeungnam Medical Science
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    • v.10 no.2
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    • pp.506-511
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    • 1993
  • This study was conducted to examine the effect of mefenamic acid for treatment of PDA in premature newborns. Ductus arteriosus is reopened by locally produced prostaglandin $E_2$ in a premature newborn during hypoxia. Mefenamic acid is one of non-steroidal antiinflammatory drugs acting by inhibition of cyclo-oxygenase in the prostaglandin synthesis pathway. For three premature newborns with PDA, we administered mefenamic acid and evaluated them with echocardiography to study the effect of mefenmic acid for closure of PDA. In all three babies, ductus arteriosus was closed successfully. We feel that mefenamic acid is safe and effective medication for treatment of PDA in premature newborns, but further study need to be conducted with larger numbers of cases to confirm this effect.

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A Simple Spectrofluorimetric Method for Determination of Mefenamic Acid in Pharmaceutical Preparation and Urine

  • Tabrizi, Ahad Bavili
    • Bulletin of the Korean Chemical Society
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    • v.27 no.8
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    • pp.1199-1202
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    • 2006
  • A simple, sensitive and rapid spectrofluorimetric method was developed for determination of mefenamic acid in pharmaceutical preparation and human urine. The procedure is based on the oxidation of mefenamic acid with cerium (IV) to produce cerium (III), and its fluorescence was monitored at 354 nm after excitation at 255 nm. The variables affecting oxidation of drug were studied and optimized. Under the experimental conditions used, the calibration graphs were linear over the range 0.03-1.5 mg $L^{-1}$. The limit of detection was 0.009 mg $L^{-1}$ and the relative standard deviation for 5 replicate determinations of mefenamic acid at 1.0 mg $L^{-1}$ concentration level was 1.72%. Good recoveries in the range of 102-107 and 102-109% were obtained for pharmaceutical preparation and human urine, respectively. The proposed method was applied to the determination of MF in one pharmaceutical preparation and human urine. The amounts of mefenamic acid found are very similar to those obtained by a standard method.

Improvement of Dissolution Rate of Mefenamic Acid by Roll Mixing with Sodium Lauryl Sulfate (라우릴황산나트륨과의 Roll 혼합에 의한 메페남산의 용출성 개선)

  • Park, Seong-Yeon;Seo, Seong-Hoon
    • Journal of Pharmaceutical Investigation
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    • v.22 no.4
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    • pp.307-315
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    • 1992
  • Dissolution rate of practically insoluble mefenamic acid was improved by roll mixing with sodium lauryl sulfate (SLS) or polyvinylpyrrolidone (PVP). The dissolution rate of the drug roll mixtures with SLS was superior to that of roll mixtures with PVP. The maximal dissolution rate was found in the roll mixtures system with SLS content of 60%. The dissolution rate of mefenamic acid roll mixtures with SLS content of 60% reached to the maximum value after 10 min of roll mixing. The transport of roll mixtures with SLS across rat jejunum was studied by the perfusion method using everted rat jejunum in vitro. The absorption rate of roll mixtures was superior to that of mefanamic acid.

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Determination of Acidic Drug with ISEs Using Ternary Complex of Metal-di-2-pyridyl Ketone Oxime-acidic Drug as Ion-Exchanger (이온교환체로서 금속-디-2-피리딜케톤옥심-산성의약품 3원 착물을 이용한 산성의약품의 정량)

  • 안문규;오원정;이언경;이순영;이재윤;정문모;허문회
    • YAKHAK HOEJI
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    • v.46 no.5
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    • pp.320-323
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    • 2002
  • A method for the determination of acidic drug, mefenamic acid and ibuprofen with ion-selective electrode(ISE) using Fe(II)-di-2-pyridyl ketone oxime complex as a counter ion were developed. Benzyl-2-nitrophenyl ether(BNPE) plasticized membrane was more selective and sensitive than the other tested membranes. The acidic drug selective electrode exhibits a linear response for 10$^{-2}$ M 510$^{-5}$ M of acidic drugs, mefenamic acid and ibuprofen with a slope of -55.9 and -56.3 mV/dec. in borate buffer solution (pH 8.9). Potentiometric selectivity measurements revealed negligible interferences from aromatic and aliphatic carboxylic acid salts. The electrodes were found to be useful for the direct determination of mefenamic acid and ibuprofen in pharmaceutical preparations.

Influence of Compression and Granule Size on Dissolution Rate of Acetaminophen, Fenbufen, and Mefenamic Acid Tablets (정제(錠劑)의 과립도(顆粒度) 및 임계타정압(臨界打錠壓)이 용출속도(溶出速度)에 미치는 영향(影響))

  • Ryu, Jang-Ha;Kim, Johng-Kap
    • Journal of Pharmaceutical Investigation
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    • v.13 no.4
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    • pp.191-195
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    • 1983
  • Acetaminophen, fenbufen, and mefenamic acid tablets were formulated with the same additives, granulated to different sizes, ranging $30{\sim}200mesh$, and compressed by pressure of $0.5{\sim}2.0\;ton{\cdot}cm^{-2}$. The hardness and disintegration time of the three tablets were determined. The dissolution rates of the three tablets at critical point of pressure were investigated. The results showed that fenbufen, and mefenamic acid tablet had critical compression pressure of $1.0\;ton{\cdot}cm^{-2}$, but acetaminophen tablet had that of $1.5\;ton{\cdot}cm^{-2}$. Neverthless, three tablets were disintegrated within 5 min. Among the three tablets, mefenamic acid tablet followed zero order of dissolution and the rate constants were as fellows; $1.68 \;mg{\cdot}min^{-1}\;(30{\sim}50mesh),\;1.76mg{\cdot} min^{-1}\;(50{\sim}80\;mesh)\;and\;4.85\;mg{\cdot}min^{-1}\;(80{\sim}200mesh)$.

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Soft Ionization of Metallo-Mefenamic Using Electrospray Ionization Mass Spectrometry

  • Abdelhamid, Hani Nasser;Wu, Hui-Fen
    • Mass Spectrometry Letters
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    • v.6 no.2
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    • pp.43-47
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    • 2015
  • Detection of mefenamic acid (M, non-steroidal anti-inflammatory drug, NSAIDs) and its metallodrug was investigated using electrospray ionization mass spectrometry (ESI-MS) and fluorescence spectroscopy. ESI-MS data (500 µL, 1×10-3 M) revealed high detection sensitivity for the drug and metallodrug. ESI-MS spectra revealed peaks at 242, 580, and 777 Da corresponding to [M+H]+, [63Cu(M-H)2(H2O)2+H]+, and [56Fe(M-H)3+H]+, respectively. The metal:mefenamic ratios of ESIMS spectra are in complete agreement with the fluorescence spectroscopy results (1:2 for Cu(II) and 1:3 for Fe(III)). ESI is a soft ionization technique that can be used on labile metallo-mefenamic acids and is promising for the detection of these species in environmental samples and biological fluids.

Inhibiton of MMP-13 mRNA expression by Doxycycline combination with Mefenamic Acid in the rat Periodontal ligament cells (백서 치주인대세포에서 Doxycycline의 Mefenamic Acid 병용사용 시 MMP-13mRNA 발현 억제 효과)

  • Seo, Jin-Hee;Ciu, De-Zhe;Kim, Young-Joon
    • Journal of Periodontal and Implant Science
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    • v.35 no.1
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    • pp.99-109
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    • 2005
  • It has been focused on the importance of the host inflammatory response in periodontal pathogenesis and progression, treatment has been introduced to control the host response and the method, which diminishes production and activity of MMP by doxycycline, has been used in periodontal field. MMP is a proteolytic enzyme which plays a major role in tissue destruction and MMP-1 is secreted in the periodontally healthy tissue, while MMP-8, 9, 13, etc in the inflammatory state. Among these, MMP-13 has been discovered lately and reported to degrade primarily type II collagen. Periodontal ligament (PDL) cell plays a role in destruction of periodontal tissue. This study was to evaluate the effect of doxycycline and mefenamic acid, non-steroidal antiinflammatory drug on MMP-13 mRNA expression in the rat PDL cell. Doxycycline concentration of $1{\sim}100\;{\mu}g/ml$ was added rat PDL cell and cell activity was measured by MIT assay at day 1 and 3. MMP-13 gene expression was evaluated by RT-PCR after PDL cells were pre-treated for 1hour with doxycycline (50 ${\mu}g/ml$) alone or with mefenamic acid ($10^{-6}M$), then added $IL-1{\beta}$(1.0 ng/ml) and incubated for 16-18 hours. The results are as follows: 1. Cell activity decreased Significantly at 24 and 72 hours in 100 ${\mu}g/ml$ (p<0.05). 2. Level of MMP-13 mRNA was in 20.2% increase by $IL-1{\beta}$ and in pre-treating doxycycline group, expression of $IL-1{\beta}$ induced MMP-13 mRNA was inhibited by 31% than $IL-1{\beta}$ treated only. 3. Mefenamic acid did not inhibit on the expression of $IL-1{\beta}$ induced MMP-13 mRNA, while mefenamic acid in combination with doxycycline inhibited the expression by 41% compared to only $IL-1{\beta}$ stimulation. These results suggest that doxycycline synergistically inhibit the expression of $IL-1{\beta}$ induced MMP-13 mRNA in combination with mefenamic acid.

Determination of Mefenamic acid with ISEs Using Ternary Complex of Metal -phenanthroline -mefenamate as Ion-exchanger (이온교환체로서 금속 -페난드롤린 -메페남산 3원 작물을 이용한 메페남산의 정량)

  • 허문회;김대병;남수자;문현숙;이미나;정문모;안문규
    • YAKHAK HOEJI
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    • v.45 no.1
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    • pp.29-33
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    • 2001
  • A method for the determination of anionic drug, mefenamate with ion-selective electrode using Fe(II)-1,10-phenanthroline chelate as a counter ion was developed. Benzyl nitrophenyl ether (BNPE) plasticized membrane was more selective and sensitive than the other tested membranes. This membrane electrode exhibits a linear response for 10$^{-2}$ M~5 $\times$ 10$^{-5}$ M of mefenamic acid with a slope of -61.4 mV/dec. in borate buffer solutions (pH 9.0). Potentiometric selectivity measurements revealed negligible interferences from various organic and ionorganic anions. Direct potentiometry and potentiometric titration method of mefenamic acid in capsule preparations are presented and compared.

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