PMID- 17377959
OWN - NLM
STAT- MEDLINE
DCOM- 20070628
LR  - 20131121
IS  - 0142-2782 (Print)
IS  - 0142-2782 (Linking)
VI  - 28
IP  - 4
DP  - 2007 May
TI  - Liquid chromatographic-mass spectrometry analysis and pharmacokinetic studies of 
      a novel rabeprazole formulation, sterile powder for injection, in dogs and rats.
PG  - 177-86
AB  - Rabeprazole is among the most potent proton pump inhibitors (PPI) identified to 
      date and it has been demonstrated that it is effective in such diseases as 
      gastroesophageal reflux disease (GERD), duodenal ulcer and gastric ulcer. There 
      is currently interest in developing a new formulation: rabeprazole sterile powder 
      for injection (RSPI). This investigation was conducted to evaluate the 
      preclinical pharmacokinetics of RSPI in rats and at the same time a comparative 
      study was carried out in dogs between RSPI and Pariet tablets using liquid 
      chromatographic-mass spectrometry analysis. The liquid chromatographic-mass 
      spectrometry method was first conducted and validated as being specific, and 
      having accuracy, precision, sensitivity and a satisfactory recovery. After 
      intravenous administration of RSPI (i.v.: 2, 6 and 18 mg/kg) to rats, no 
      significant dose-dependency was found in the CL (4.20-5.72 l/h/kg), V(area) (d) 
      (0.94-1.32 l/kg), dose-normalized AUC (197.20-245.82 microg/l*h based on 1 mg/kg) 
      and t(1/2) (p>0.05). In the dog, a randomized, open-label, crossover experiment 
      was carried out to show that the mean area under the plasma concentration-time 
      curve (AUC(0-infinity)) after i.v. administration of RSPI was at least four times 
      larger than that following oral administration of Pariet tablet at an equivalent 
      dose but the elimination half-life of these two formulation was similar (p>0.05). 
      The results showed that the pharmacokinetics of RSPI was linear (r(2) = 0.98) in 
      the dose range 2-18 mg/kg and the RSPI had a much higher AUC(0-infinity) and 
      similar t(1/2) values compared with the enteric-coated tablet.
CI  - Copyright (c) 2007 John Wiley & Sons, Ltd.
FAU - Shao, Feng
AU  - Shao F
AD  - Key Laboratory of Drug Metabolism and Pharmacokinetics, China Pharmaceutical 
      University, Nanjing, 210009, Jiangsu Province, China.
FAU - Sun, Jianguo
AU  - Sun J
FAU - Wang, Guangji
AU  - Wang G
FAU - Xie, Haitang
AU  - Xie H
FAU - Zhu, Xiaoyan
AU  - Zhu X
FAU - Zhang, Jingwei
AU  - Zhang J
LA  - eng
PT  - Journal Article
PT  - Research Support, Non-U.S. Gov't
PL  - England
TA  - Biopharm Drug Dispos
JT  - Biopharmaceutics & drug disposition
JID - 7911226
RN  - 0 (2-Pyridinylmethylsulfinylbenzimidazoles)
RN  - 0 (Anti-Ulcer Agents)
RN  - 0 (Powders)
RN  - 0 (Proton Pump Inhibitors)
RN  - 32828355LL (Rabeprazole)
SB  - IM
MH  - 2-Pyridinylmethylsulfinylbenzimidazoles/blood/*pharmacokinetics
MH  - Animals
MH  - Anti-Ulcer Agents/blood/*pharmacokinetics
MH  - Chemistry, Pharmaceutical
MH  - Chromatography, Liquid
MH  - Dogs
MH  - Female
MH  - Half-Life
MH  - Injections, Intravenous
MH  - Male
MH  - Mass Spectrometry
MH  - Metabolic Clearance Rate
MH  - Powders
MH  - Proton Pump Inhibitors
MH  - Rabeprazole
MH  - Rats
MH  - Rats, Sprague-Dawley
MH  - Species Specificity
MH  - Tissue Distribution
EDAT- 2007/03/23 09:00
MHDA- 2007/06/29 09:00
CRDT- 2007/03/23 09:00
PHST- 2007/03/23 09:00 [pubmed]
PHST- 2007/06/29 09:00 [medline]
PHST- 2007/03/23 09:00 [entrez]
AID - 10.1002/bdd.543 [doi]
PST - ppublish
SO  - Biopharm Drug Dispos. 2007 May;28(4):177-86. doi: 10.1002/bdd.543.