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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]

Biosimilars

Biosimilarity of HX575 (human recombinant epoetin alfa) and epoetin beta after multiple subcutaneous administration

F. Sörgel, U. Thyroff-Friesinger, A. Vetter, B. Vens-Cappell and M. Kinzig

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Volume 47 p. 391 - 401

Abstract

F. Sörgel¹, U. Thyroff-Friesinger², A. Vetter², B. Vens-Cappell³ and M. Kinzig¹

¹IBMP-Institute for Biomedical and Pharmaceutical Research, Nürnberg-Heroldsberg, ²Clinical Research, Hexal AG, Holzkirchen, and ³Scope International, Hamburg, Germany
Objective: To compare the steady-state pharmacokinetics and pharmacodynamics following multiple subcutaneous administration of a new erythropoiesis stimulating agent (HX575, Binocrit^®, Sandoz GmbH, Holzkirchen, Germany) with that of epoetin beta (NeoRecormon^®, Roche Ltd., Welwyn Garden City, UK). Methods: An open, randomized, parallel group study was conducted in 80 healthy adult males. Subjects were randomized to multiple subcutaneous doses of 100 IU/kg body weight of HX575 or epoetin beta three-times-weekly for 4 weeks. Serum epoetin concentrations were measured using an enzyme-linked immunosorbent assay (ELISA) and pharmacokinetic parameters for the two treatments were compared. The time course and area under the effect curve ratios of hematological characteristics were used as surrogate parameters for efficacy evaluation. Results: The pharmacokinetic profiles after multiple doses were similar for both treatments. HX575 was bioequivalent to epoetin beta with respect to the rate and extent of exposure of exogenous epoetin, as indicated by the ratios (90% confidence intervals) of AUC_tau (96.1 (86.4 – 106.9)) and C_max,ss (98.5 (85.2 – 113.9)). The hematological profiles of both treatments were similar as determined from the population mean curves and the AUEC_Hb ratio (90% confidence interval] (99.2 (97.7 – 100.7)), the primary endpoint of this study. Study medication was well tolerated with no clinically relevant differences between safety profiles of the treatments. Anti-epoetin antibodies were not detected at any time. Conclusions: HX575 and epoetin beta were bioequivalent with respect to their steady-state pharmacokinetic profile and pharmacodynamic action. These results support the conclusion that HX575 and epoetin beta will be equally efficacious and may be interchangeable as therapy.Correspondence to:
Prof. F. Sörgel
Department of Research
IBMP-Institute for Biomedical and Pharmaceutical Research
Paul-Ehrlich-Straße 19
90562 Nürnberg-Heroldsberg, Germany
Email: [email protected]

Extended Abstracts

Biomarker response on exposure to sunitinib and its primary metabolite (SU12662) in metastatic colorectal cancer patients

F. Kanefendt, A. Lindauer, M. Kinzig, D. Strumberg, M.E. Scheulen, K. Mross, R. Fischer, B. Moritz, F. Sörgel and U. Jaehde

Volume 49 p. 88 - 90

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