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Pharmacokinetics

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

F. Sörgel, U. Fuhr, M. Minic, M. Siegmund, J. Maares, A. Jetter, M. Kinzig- Schippers, D. Tomalik-Scharte, J. Szymanski, T. Goeser, U. Toex, B. Scheidel and W. Lehmacher

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Volume 43 p. 140 - 149

Abstract

F. Sörgel¹, U. Fuhr², M. Minic³, M. Siegmund⁴, J. Maares⁴, A. Jetter², M. Kinzig- Schippers², D. Tomalik-Scharte², J. Szymanski², T. Goeser⁵, U. Toex⁵, B. Scheidel¹ and W. Lehmacher⁶

¹Institute for Biomedical and Pharmaceutical Research, Nuremberg-Heroldsberg, ²University of Cologne, Department of Pharmacology, Clinical Pharmacology, Cologne, Germany, ³F. Hoffmann-La Roche Ltd., Basel, ⁴Roche Consumer Health Ltd., Kaiseraugst, Switzerland, ⁵University of Cologne, Department of Gastroenterology and ⁶University of Cologne, Department of Medical Statistics, Cologne, Germany
Objective: This paper describes four studies investigating the dissolution, plasma pharmacokinetics and safety of a novel, fast-acting ibuprofen formulation, ibuprofen sodium dihydrate. Material and Method: Four separate studies investigated: the in vitro dissolution rates of ibuprofen sodium dihydrate (at pH 1.2, 3.5 and 7.2); the bioavailability of ibuprofen sodium dihydrate (in two pharmacokinetic studies; combined n = 38) compared with conventional ibuprofen, ibuprofen lysinate, ibuprofen arginate and ibuprofen liquagels (all 2 × 200 mg ibuprofen); and the gastroduodenal tolerance of ibuprofen sodium dihydrate and ibuprofen arginate (both 2 × 200 mg ibuprofen t.i.d.) in an endoscopy safety study, where endoscopy was performed at baseline and at the end of each treatment period using a five-point scale to assess the integrity of the gastric and duodenal mucosa. Results: Ibuprofen sodium dihydrate dissolved significantly more rapidly at pH 1.2, 3.5 and 7.2 than conventional ibuprofen, ibuprofen lysinate and ibuprofen liquagels. Ibuprofen sodium dihydrate had similar C_max to ibuprofen lysinate and ibuprofen liquagels and significantly higher C_max than conventional ibuprofen (p = 0.002). The mean plasma concentration for ibuprofen sodium dihydrate was significantly higher than for conventional ibuprofen (p = 0.028) 10 minutes post-dose and the t_max for ibuprofen sodium dihydrate was reached significantly earlier than for conventional ibuprofen (p = 0.018). All three formulations were bioequivalent according to the acceptable boundaries (90% confidence intervals). No statistically significant difference was observed between the ibuprofen formulations in terms of adverse events and specifically with respect to hemorrhagic scores; 41 (46.0%) adverse events (AEs) occurred after administration of ibuprofen sodium dihydrate, and 46 (52.9%) after ibuprofen arginate. One occurrence of an invasive ulcer was observed after administration of ibuprofen arginate. Conclusions: The new formulation of ibuprofen sodium dihydrate dissolves quickly in vitro, has the same extent of absorption as other fast-acting ibuprofen formulations, and is absorbed into plasma more rapidly than conventional ibuprofen. In addition, the present studies suggest that the tolerability and safety profile of ibuprofen sodium dihydrate is comparable to existing ibuprofen formulations.Correspondence to:
Prof. Dr. F. Sörgel; Institute for Biomedical and Pharmaceutical Research, Paul-Ehrlich-Straße 19,
90562 Nürnberg-Heroldsberg, Germany
Email: [email protected]

Therapeutics

Ibuprofen sodium dihydrate, an ibuprofen formulation with improved absorption characteristics, provides faster and greater pain relief than ibuprofen acid

P. Schleier, A. Prochnau, A.M. Schmidt-Westhausen, H. Peters, J. Becker, T. Latz, J. Jackowski, E.U. Peters, G.E. Romanos, B. Zahn, J. Lüdemann, J. Maares and B. Petersen

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Volume 45 p. 89 - 97

Abstract

P. Schleier, A. Prochnau, A.M. Schmidt-Westhausen, H. Peters, J. Becker, T. Latz, J. Jackowski, E.U. Peters, G.E. Romanos, B. Zahn, J. Lüdemann, J. Maares and B. Petersen

¹Department of Maxillofacial Surgery/Plastic Surgery, Friedrich Schiller University, Jena, ²Department of Oral Surgery and Dental Radiology, Charité Universitätsmedizin Berlin, ³Department of Oral Surgery and Central Admittance, University Clinic of Düsseldorf, ⁴Department of Oral Surgery, School of Dental Medicine, University of Witten/Herdecke, ⁵Department of Oral Surgery and Implantology, University of Frankfurt am Main, Germany, ⁶Bayer Consumer Care AG, Basle, Switzerland, and ⁷Schlossweg ³, Grenzach-Wyhlen, Germany
Objective: The objective of this 6-hour study was to compare rate of pain relief, analgesic efficacy and tolerability of a novel ibuprofen formulation, ibuprofen sodium dihydrate, with that of ibuprofen acid in subjects with postoperative dental pain. Material and methods: The test formulation of ibuprofen sodium dihydrate (256 mg sodium salt) and the reference product both contain 200 mg ibuprofen. Subjects with moderate-to-severe pain after extraction of third molars were randomized to receive two tablets of either ibuprofen sodium dihydrate (198 subjects) or ibuprofen (198 subjects) in this double-blind, multicenter trial. Pain was measured using traditional descriptor scales and onset of analgesia assessed using the stopwatch method. Results: Median time to substantial pain relief occurred 14 minutes earlier in the ibuprofen sodium dihydrate group (p < 0.001). The first sign of pain relief, an increase in relief and time until the pain was half gone occurred significantly earlier and faster in the ibuprofen sodium dihydrate-treated patients (p < 0.02 – 0.00003). Corresponding numbers needed to treat were in the range 5 – 11. Reduction in pain intensity was evident within 5 minutes (p < 0.01) in the ibuprofen sodium dihydrate group compared to 15 minutes in the ibuprofen group. Pain intensity was reduced to half after 30 and 57 minutes in the ibuprofen sodium dihydrate and ibuprofen groups, respectively (p < 0.025). The overall analgesic efficacy in terms of summed pain intensity differences (SPID), total pain relief (TOTPAR) and remedication times in the two groups were similar. Both treatments were well tolerated and no serious events occurred. Conclusion: Ibuprofen sodium dihydrate provides faster and more efficacious pain relief during the first hour after intake when compared to a conventional ibuprofen acid formulation. The tolerability profiles are similar.Correspondence to:
B. Petersen; Bayer Consumer Care AG, Peter Merian-Straße 84, Postbox, 4002 Basel, Switzerland
Email: [email protected]

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