Pharmacokinetics of ibuprofen sodium dihydrate and gastrointestinal tolerability of short-term treatment with a novel, rapidly absorbed formulation

Sörgel, Fritz; Fuhr, Uwe; Vulović, Maja; Siegmund, M; Maares, J.; Jetter, Alexander; Kinzig‐Schippers, Martina; Tomalik-Scharte, Dorota; Szymański, Jacek; Goeser, Tobias; Toex, Ulrich; Scheidel, B; Lehmacher, Walter

doi:10.5414/cpp43140

Cited by 24 publications

(16 citation statements)

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“…The favorable safety profile of IBU Na described in this analysis is consistent with that seen in clinical studies of other IBU Na formulations [19][20][21][22][23]. In those studies, AEs associated with IBU Na were typically mild to moderate and did not result in treatment discontinuation.…”

Section: Discussionsupporting

confidence: 82%

Safety of a novel formulation of ibuprofen sodium compared with standard ibuprofen and placebo

Jayawardena

Leyva

Kellstein

2014

Postgraduate Medicine

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Section: Discussionsupporting

confidence: 82%

Safety of a novel formulation of ibuprofen sodium compared with standard ibuprofen and placebo

Jayawardena

Leyva

Kellstein

2014

Postgraduate Medicine

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“…Previous studies have demonstrated that the median time to meaningful pain relief for ibuprofen arginate was half that of the standard ibuprofen [6,13,14]. Because the T max for sodium ibuprofen in this study (median: 35 min) was found to be similar to ibuprofen arginate (mean: 33.6 min) [9], it can be expected that sodium ibuprofen would induce analgesic effects with a similar onset of action as ibuprofen arginate. Such a formulation would be a valuable addition to the OTC choice currently available to individuals with acute pain.…”

Section: Discussionmentioning

confidence: 58%

“…This is likely to be due to faster dissolution and more rapid availability of ibuprofen particles for absorption, as suggested by Sorgel et al . [9]. …”

Section: Discussionmentioning

confidence: 99%

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Bioavailability of ibuprofen following oral administration of standard ibuprofen, sodium ibuprofen or ibuprofen acid incorporating poloxamer in healthy volunteers

Dewland¹,

Reader

Berry

2009

BMC Clin Pharmacol

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BackgroundThe aim of this study was to compare the pharmacokinetic properties of sodium ibuprofen and ibuprofen acid incorporating poloxamer with standard ibuprofen acid tablets.MethodsTwenty-two healthy volunteers were enrolled into this randomised, single-dose, 3-way crossover, open-label, single-centre, pharmacokinetic study. After 14 hours' fasting, participants received a single dose of 2 × 200 mg ibuprofen acid tablets (standard ibuprofen), 2 × 256 mg ibuprofen sodium dihydrate tablets (sodium ibuprofen; each equivalent to 200 mg ibuprofen acid) and 2 × 200 mg ibuprofen acid incorporating 60 mg poloxamer 407 (ibuprofen/poloxamer). A washout period of 2-7 days separated consecutive dosing days. On each of the 3 treatment days, blood samples were collected post dose for pharmacokinetic analyses and any adverse events recorded. Plasma concentration of ibuprofen was assessed using a liquid chromatographic-mass spectrometry procedure in negative ion mode. A standard statistical ANOVA model, appropriate for bioequivalence studies, was used and ratios of 90% confidence intervals (CIs) were calculated.ResultsTmax for sodium ibuprofen was less than half that of standard ibuprofen (median 35 min vs 90 min, respectively; P = 0.0002) and Cmax was significantly higher (41.47 μg/mL vs 31.88 μg/mL; ratio test/reference = 130.06%, 90% CI 118.86-142.32%). Ibuprofen/poloxamer was bioequivalent to the standard ibuprofen formulation, despite its Tmax being on average 20 minutes shorter than standard ibuprofen (median 75 mins vs 90 mins, respectively; P = 0.1913), as the ratio of test/reference = 110.48% (CI 100.96-120.89%), which fell within the 80-125% limit of the CPMP and FDA guidelines for bioequivalence. The overall extent of absorption was similar for the three formulations, which were all well tolerated.ConclusionIn terms of Tmax, ibuprofen formulated as a sodium salt was absorbed twice as quickly as from standard ibuprofen acid. The addition of poloxamer to ibuprofen acid did not significantly affect absorption.

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“…IBU is a carboxylic acid that does not rapidly dissolve in an acidic aqueous environment such as that of the stomach [ 3 ]. In vitro investigations have shown a significantly faster rate of dissolution for IBU Na compared with standard IBU tablets at acidic pH levels [ 13 ]. The current findings demonstrate that these novel IBU Na tablets, which have a thin-film coating and are manufactured using a patent-pending process, provide faster absorption with a more rapid attainment of peak IBU plasma concentrations compared with standard IBU tablets.…”

Section: Discussionmentioning

confidence: 99%

Ibuprofen Sodium Is Absorbed Faster than Standard Ibuprofen Tablets: Results of Two Open-Label, Randomized, Crossover Pharmacokinetic Studies

et al. 2014

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BackgroundA novel ibuprofen (IBU) formulation, Advil® Film-Coated Tablets (IBUNa), was developed.ObjectivePharmacokinetic comparison of IBUNa versus other IBU formulations.Study DesignTwo randomized, single-dose, open-label, five-way crossover pharmacokinetic studies.SettingInpatient research clinic.SubjectsSeventy-one healthy adult volunteers.InterventionStudy 1: In three periods, fasted subjects received 400-mg IBU dose equivalents as IBUNa 2 × 256 mg, Advil® Liqui-Gels® (IBULG) 2 × 200 mg, and Motrin® IB (IBUMot) 2 × 200 mg tablets. In two periods following a high-fat breakfast, subjects received 400-mg IBU dose equivalents as IBUNa 2 × 256 mg and IBULG 2 × 200 mg. Study 2: In five study periods, fasted subjects received 400-mg IBU dose equivalents as IBUNa 2 × 256 mg, Advil® FastGel® (IBUFG) 2 × 200 mg, Nurofen® (IBUNur) 2 × 200 mg, Advil® (IBUAdv) 2 × 200 mg, and Nurofen® Express containing IBU lysinate (IBULys) 2 × 342 mg.Main Outcome MeasureLog-transformed area under the plasma concentration versus time curve to last observable concentration (AUCL) and maximum plasma concentration (Cmax) were the primary pharmacokinetic parameters; time to maximum measured plasma concentration (Tmax) was analyzed post hoc.ResultsIBUNa was bioequivalent to IBULG (fasted and fed) and IBUFG and IBULys (fasted) for rate (Cmax) and extent (AUCL) of IBU absorption. After fasting, AUCL was bioequivalent for IBUNa and IBUMot, IBUAdv, and IBUNur, but Cmax occurred significantly earlier with IBUNa. After fasting, median IBUNaTmax was comparable to that for IBULG, IBUFG, and IBULys, but was much shorter than that for IBUMot, IBUNur, and IBUAdv. Food slowed absorption of IBUNa and IBULG similarly. All treatments were tolerated similarly.ConclusionIBUNa is absorbed faster but to a similar extent as standard IBU formulations.

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Pharmacokinetics of ibuprofen sodium dihydrate and gastrointestinal tolerability of short-term treatment with a novel, rapidly absorbed formulation

Cited by 24 publications

References 0 publications

Safety of a novel formulation of ibuprofen sodium compared with standard ibuprofen and placebo

Safety of a novel formulation of ibuprofen sodium compared with standard ibuprofen and placebo

Bioavailability of ibuprofen following oral administration of standard ibuprofen, sodium ibuprofen or ibuprofen acid incorporating poloxamer in healthy volunteers

Ibuprofen Sodium Is Absorbed Faster than Standard Ibuprofen Tablets: Results of Two Open-Label, Randomized, Crossover Pharmacokinetic Studies

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