PMID- 15792398
OWN - NLM
STAT- MEDLINE
DCOM- 20050614
LR  - 20190608
IS  - 0946-1965 (Print)
IS  - 0946-1965 (Linking)
VI  - 43
IP  - 3
DP  - 2005 Mar
TI  - Pharmacokinetics of ibuprofen sodium dihydrate and gastrointestinal tolerability 
      of short-term treatment with a novel, rapidly absorbed formulation.
PG  - 140-9
AB  - 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 x 200 mg 
      ibuprofen); and the gastroduodenal tolerance of ibuprofen sodium dihydrate and 
      ibuprofen arginate (both 2 x 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 Cmax 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.
FAU - Sorgel, F
AU  - Sorgel F
AD  - Institute for Biomedical and Pharmaceutical Research, Nuremberg-Heroldsberg, 
      Germany. ibmp@osn.de
FAU - Fuhr, U
AU  - Fuhr U
FAU - Minic, M
AU  - Minic M
FAU - Siegmund, M
AU  - Siegmund M
FAU - Maares, J
AU  - Maares J
FAU - Jetter, A
AU  - Jetter A
FAU - Kinzig-Schippers, M
AU  - Kinzig-Schippers M
FAU - Tomalik-Scharte, D
AU  - Tomalik-Scharte D
FAU - Szymanski, J
AU  - Szymanski J
FAU - Goeser, T
AU  - Goeser T
FAU - Toex, U
AU  - Toex U
FAU - Scheidel, B
AU  - Scheidel B
FAU - Lehmacher, W
AU  - Lehmacher W
LA  - eng
PT  - Clinical Trial
PT  - Journal Article
PT  - Randomized Controlled Trial
PL  - Germany
TA  - Int J Clin Pharmacol Ther
JT  - International journal of clinical pharmacology and therapeutics
JID - 9423309
RN  - 0 (Anti-Inflammatory Agents, Non-Steroidal)
RN  - WK2XYI10QM (Ibuprofen)
SB  - IM
MH  - Adult
MH  - Anti-Inflammatory Agents, Non-Steroidal/adverse 
      effects/*pharmacokinetics/therapeutic use
MH  - Area Under Curve
MH  - Chemistry, Pharmaceutical
MH  - Female
MH  - Gastrointestinal Tract/*metabolism
MH  - Half-Life
MH  - Humans
MH  - Ibuprofen/adverse effects/*pharmacokinetics/therapeutic use
MH  - Intestinal Absorption
MH  - Male
MH  - Middle Aged
EDAT- 2005/03/29 09:00
MHDA- 2005/06/15 09:00
CRDT- 2005/03/29 09:00
PHST- 2005/03/29 09:00 [pubmed]
PHST- 2005/06/15 09:00 [medline]
PHST- 2005/03/29 09:00 [entrez]
AID - 10.5414/cpp43140 [doi]
PST - ppublish
SO  - Int J Clin Pharmacol Ther. 2005 Mar;43(3):140-9. doi: 10.5414/cpp43140.