Bioavailability of naproxen sodium and its relationship to clinical analgesic effects.

Sevelius, Hilli; Runkel, Richard; Segre, Eugene J.; Ss, Bloomfield

doi:10.1111/j.1365-2125.1980.tb01753.x

Cited by 85 publications

(35 citation statements)

References 16 publications

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“…Pharmacokinetic differences between the formulations are restricted to the slightly earlier and higher plasma concentrations achieved with naproxen sodium, which result in a slightly faster onset of action; in other respects the 2 formulations are pharmacokinetically, pharmacologically, and therapeutically equivalent at comparable doses (38,48,52). Naproxen and naproxen sodium are generally considered to be efficacious, safe, and well tolerated in humans, although renal and gastrointestinal side effects similar to those observed with other NSAIDs are occasionally seen (15,18,52).…”

Section: Introductionmentioning

confidence: 99%

Renal Changes Associated with Naproxen Sodium Administration in Cynomolgus Monkeys

Leach¹,

Frank²,

Berardi³

et al. 1999

Toxicol Pathol

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Naproxen sodium was administered to cynomolgus monkeys (Macaca fascicularis) by oral gavage at daily doses of 44, 88, or 176 mg/kg for 2 wk (2 monkeys/gender) or of 44 mg/kg for 13 wk (4 monkeys/gender). Body weight loss occurred in at least one monkey in all naproxen sodium-dosed groups in the 2-wk (up to 16% loss) and 13-wk (up to 22% loss) studies. Increases in plasma naproxen concentrations were dose proportional between 44 and 88 mg/kg but were less than dose proportional between 88 and 176 mg/kg. Up to 2-fold increases in creatinine and/or serum urea nitrogen values as well as higher renal weights occurred in monkeys receiving 176 mg/kg for 2 wk or 44 mg/kg for 13 wk. Microscopically, renal changes were observed in all naproxen sodium-dosed groups. Renal findings after 2 wk of exposure included increased interstitial ground substance, tubular dilatation, and tubulointerstitial nephritis; in the 13-wk study, cortical tubular atrophy and interstitial fibrosis were also observed. These studies identify the kidney as the target organ of naproxen sodium in cynomolgus monkeys.

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Section: Introductionmentioning

confidence: 99%

Renal Changes Associated with Naproxen Sodium Administration in Cynomolgus Monkeys

Leach¹,

Frank²,

Berardi³

et al. 1999

Toxicol Pathol

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“…Previous studies suggested that higher BA and faster absorption may correspond to improved clinical benefit. 3,34) Furthermore, in addition to the in vivo animal experiments, our preliminary in vitro human cadaver skin permeation studies indicated that the MNs were feasible to deliver sufficient SS across the skin for treatment of migraine by increasing the diameter of the array up to 2 cm (data not shown). Therefore, although further practical verifications are needed, these findings demonstrated that the novel sodium hyaluronate MN delivery system was an excellent candidate for delivering SS to migraine patients, while avoiding the pain associated with use of hypodermic needles.…”

Section: Discussionmentioning

confidence: 99%

Improvement of Transdermal Delivery of Sumatriptan Succinate Using a Novel Self-dissolving Microneedle Array Fabricated from Sodium Hyaluronate in Rats

Quan

Kamiyama

et al. 2015

Biological & Pharmaceutical Bulletin

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The purpose of the present study was to develop an alternative transdermal formulation containing sumatriptan succinate (SS) for the treatment of migraine. Novel self-dissolving SS-loaded microneedle arrays (MNs) were fabricated from sodium hyaluronate and their efficacy for transdermal delivery of SS was characterized. The resulting MNs maintained their skin piercing abilities for at least 30 min after being placed at a high relative humidity of 75%. Rapid release of SS from the MNs was also observed in vitro. Optical coherence tomography images demonstrated that MNs were able to successfully pierce into rat skin without any bending or cracking, and needles were completely dissolved within 1 h. MNs significantly increased transepidermal water loss; however, skin barrier function gradually recovered to control levels within 24 h, in contrast to the skin damage observed after tape stripping treatment. These findings indicated that the micropores created by MNs quickly resealed, and that the skin damage was reversible. Furthermore, a dosedependent plasma concentration of SS was obtained after transdermal delivery using SS-loaded MNs in rats. Absorption of SS delivered by MNs was similar to that observed after subcutaneous injection and was associated with high bioavailability (ca. 90%), which was much higher than that produced by oral administration. These findings suggested that application of SS-loaded MNs to the skin provided an effective alternative approach to enhance the transdermal delivery of SS without serious skin damage, and would be likely to improve patient compliance.

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“…Naproxen ( Fig.1) chemically designated as [(S)-6-methoxy-alpha-methyl-2-naphthaleneacetic acid] is non-steroidal anti-inflammatory medicine that demonstrates both antipyretic and analgesic behavior [1][2][3][4]. It can be used for the remedy of various diseases, such as rheumatoid arthritis, juvenile rheumatoid arthritis, ankylosing spondylitis, osteoarthritis, primary dysmenorrheal and acute gout [5].…”

Section: -Introductionmentioning

confidence: 99%

Development and Validation of Liquid Chromatographic Method for Naproxen and Esomeprazole in Binary Combination

Razzaq

Ashfaq

Khan

et al. 2012

J. Chil. Chem. Soc.

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The present study reports the development and validation of a simple, economic and sensitive HPLC method for the concurrent determination of naproxen and esomeprazole in pharmaceutical formulations. Isocratic chromatography was performed with C-18 column and mixture of phosphate buffer (pH 6.1) and acetonitrile in ratio of (40:60, v/v) at 1.5 mlmin -1. The eluents were monitored at 302 nm using UV detector. The method was isocratic in the range of 9.38 to 300 µgml -1 for naproxen and 0.5 to 16 µgml -1 for esomeprazole. Validation of the method was performed by testing parameters like linearity, accuracy, precision, robustness, specificity, LOD and LOQ values. In the specificity the drugs were subjected to forced degradation studies like acidic, basic, oxidative and thermal stresses. Both the analytes were separated within three minutes. As the method separates the degradation products produced during forced degradation studies from the active analytes so it can be used not only for regular determination of naproxen and esomeprazole but also for their stability studies.Key words: HPLC, acetonitrile, isocratic, specificity, forced degradation study.e-mail: ashfaqchemist@hotmail.com 1-INTRODUCTIONNaproxen (Fig.1) chemically designated as [(S)-6-methoxy-alpha-methyl-2-naphthaleneacetic acid] is non-steroidal anti-inflammatory medicine that demonstrates both antipyretic and analgesic behavior [1][2][3][4]. It can be used for the remedy of various diseases, such as rheumatoid arthritis, juvenile rheumatoid arthritis, ankylosing spondylitis, osteoarthritis, primary dysmenorrheal and acute gout [5]. After taken orally, naproxen is partially metabolized to its 6-O-desmethylated active metabolite. Both the drug and its metabolite are then excreted through urine either as unchanged or in conjugation with sulphate or glucoronic acid [6][7][8].A careful literature survey did not reveal any single analytical technique for the determination of naproxen and esomeprazole simultaneously. Therefore, attempts were made to develop and validate an isocratic reverse phase HPLC method to determine both drugs simultaneously. We are currently engaged in binary combination analysis of different classes of drugs in synthetic mixtures and in pharmaceutical formulations [30][31][32][33][34][35][36][37][38][39]. The present work is therefore, aimed to attain the optimum chromatographic conditions for the determination of naproxen and esomeprazole simultaneously.We describe in this paper a simple, cheap, sensitive and validated HPLC method with run time less than 3 minutes for the determination of naproxen and esomeprazole simultaneously in pharmaceutical formulations. The developed method can be applied to routine quality control analysis of drugs and for other analytical purposes. 2-EXPERIMENTAL Chemicals and ReagentsReference standards of both naproxen and esomeprazole with claimed percentage purity of 99.62 and 99.71 % respectively were kindly gifted by Schazoo Zaka Laboratories (Lahore, Pakistan). Acetonitrile (chromatography grad...

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Bioavailability of naproxen sodium and its relationship to clinical analgesic effects.

Cited by 85 publications

References 16 publications

Renal Changes Associated with Naproxen Sodium Administration in Cynomolgus Monkeys

Renal Changes Associated with Naproxen Sodium Administration in Cynomolgus Monkeys

Improvement of Transdermal Delivery of Sumatriptan Succinate Using a Novel Self-dissolving Microneedle Array Fabricated from Sodium Hyaluronate in Rats

Development and Validation of Liquid Chromatographic Method for Naproxen and Esomeprazole in Binary Combination

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