Relationship between selective COX-2 inhibition and tissue selectivity of prostaglandin biosynthesis inhibition of zaltoprofen

Nishioka, K.; Uchida, Aoi; Kunigami, Minako; Matsukura, Hitoshi; Hirate, Kenji; Saitoh, Terunobu

doi:10.2492/jsir1981.20.247

Ensho

2000

DOI: 10.2492/jsir1981.20.247

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Relationship between selective COX-2 inhibition and tissue selectivity of prostaglandin biosynthesis inhibition of zaltoprofen

K. Nishioka¹,

Aoi Uchida²,

Minako Kunigami³

et al.

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Cited by 3 publications

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“…with a good safety margin (UD 50 , 50–100 mg/kg, p.o.) 6, 7. In addition, zaltoprofen has been shown to inhibit bradykinin‐induced nociceptive responses more potently than indomethacin 5…”

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confidence: 99%

“…with a good safety margin (UD 50 , 50-100 mg/kg, p.o.). 6,7 In addition, zaltoprofen has been shown to inhibit bradykinin-induced nociceptive responses more potently than indomethacin. 5 Earlier publications have described high-performance liquid chromatography/ultraviolet (HPLC-UV) and a column-switching HPLC-UV method for the analysis of zaltoprofen in biological samples.…”

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Determination of zaltoprofen in human plasma by liquid chromatography with electrospray tandem mass spectrometry: application to a pharmacokinetic study

Lee

Seo

Kim

et al. 2006

Rapid Comm Mass Spectrometry

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In the present study, we developed a method coupling liquid-liquid extraction (LLE) to high-performance liquid chromatography (HPLC) with positive ion electrospray ionization tandem mass spectrometry (ESI-MS/MS) to determine zaltoprofen levels in human plasma, using enalapril as internal standard (IS). The high sensitivity and specificity of MS/MS detection enabled the use of small plasma volumes (250 microL) and a simple LLE procedure. Furthermore, the short run-times (2 min) involved are compatible with the requirements of large-scale clinical studies. Ion acquisition was performed in multiple reaction monitoring (MRM) mode by monitoring the transitions m/z 299.3 > 225.0 for zaltoprofen and m/z 377.4 > 234.2 for the IS enalapril. The limit of detection (LOD) was 0.01 microg/mL and the lower limit of quantitation (LLOQ) was 0.05 microg/mL. The devised method was linear over the studied range (0.05-20 microg/mL), with r2 > 0.99 and a run-time of 2 min. Intra-day precisions fell in the range 2.0-13.8%, inter-day precisions in the range 2.1-3.9%, and intra- and inter-day accuracies in the range 102.8-114.1%. The described method provides a fast and sensitive analytical tool for zaltoprofen and was successfully applied to a 24-subject pharmacokinetic study.

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mentioning

confidence: 99%

mentioning

confidence: 99%

Determination of zaltoprofen in human plasma by liquid chromatography with electrospray tandem mass spectrometry: application to a pharmacokinetic study

Lee

Seo

Kim

et al. 2006

Rapid Comm Mass Spectrometry

View full text Add to dashboard Cite

show abstract

Enhancement of S(+)-zaltoprofen oral bioavailability using nanostructured lipid carrier system

Pham

Lee

et al. 2022

Arch. Pharm. Res.

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Fabrication and Characterization of Zaltoprofen Loaded Lyotropic Liquid Crystalline Gel

Pande¹,

Nayak²,

Kendre³

et al. 2016

IND. DRU.

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In recent years, most of the non-steroidal anti-inflammatory drugs (NSAID’s) have been designed to deliver the drug in the form of topical gels, to avoid GIT irritation and to maximize drug concentration at the site of action. Liquid crystal phase has emerged as a novel material for the preparation of topical drug delivery system. For the preparation of liquid crystals, we have selected glycerol monooleate (GmO) because it is biocompatible, bioadhesive, a penetration enhancer and sustained release agent. It was proposed to develop zaltoprofen loaded lyotropic liquid crystalline gel. The optimized formulation of this system shows hexagonal phase identified by polarized microscopy and transmission electron microscopy. In vitro drug release kinetics shows that there was 70.45% drug release within 48 hrs. Textural properties like adhesiveness, cohesiveness, hardness and gumminess and texture profile analysis (TPA) of zaltoprofen loaded lyotropic liquid crystalline gel could be evaluated with the help of cT3 texture analyzer. In vivo evaluation of this formulation was done by carrageenan induced rat paw edema anti-inflammatory model.

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Relationship between selective COX-2 inhibition and tissue selectivity of prostaglandin biosynthesis inhibition of zaltoprofen

Cited by 3 publications

References 0 publications

Determination of zaltoprofen in human plasma by liquid chromatography with electrospray tandem mass spectrometry: application to a pharmacokinetic study

Determination of zaltoprofen in human plasma by liquid chromatography with electrospray tandem mass spectrometry: application to a pharmacokinetic study

Enhancement of S(+)-zaltoprofen oral bioavailability using nanostructured lipid carrier system

Fabrication and Characterization of Zaltoprofen Loaded Lyotropic Liquid Crystalline Gel

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