Oral bioavailability and enterohepatic recirculation of otilonium bromide in rats

@article{Shin2008OralBA,
  title={Oral bioavailability and enterohepatic recirculation of otilonium bromide in rats},
  author={Beom Soo Shin and Jung Jun Kim and John Kim and S K Hu and Han Kyung Kim and Hye Suk Lee and Sun Dong Yoo},
  journal={Archives of Pharmacal Research},
  year={2008},
  volume={31},
  pages={117-124}
}
This study was conducted to examine the oral bioavailability and the possibility of enterohepatic recirculation of otilonium bromide in rats. A sensitive LC/MS/MS assay (LLOQ 0.5 ng/mL) was developed for the determination of otilonium and applied to i.v. and oral administration studies in bile duct cannulated (BDC) and non-BDC rats. After i.v. injection to BDC rats (1 mg/kg as otilonium), average t1/2, CL, Vz and AUC were 7.9 ± 1.9 h, 8.7 ± 3.1 mL/min/kg, 5.7 ± 1.4 L/kg and 2,088 ± 676 ng·h/mL… 
Determination of the unstable drug otilonium bromide in human plasma by LC-ESI-MS and its application to a pharmacokinetic study.
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Each of the most common sources of multiple peaking is contributed by biliary secretion followed by intestinal reabsorption of a drug, a process for which the term ‘enterohepatic recycling’ has been coined.
A Mini Review on Characteristics and Analytical Methods of Otilonium Bromide.
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Otilonium bromide (OTB) is quaternary ammonium compound with action on distal GI tract as antispasmodic and is utilized in the treatment of patients influenced by Irritable inside disorder (IBS because of its particular pharmacokinetic and pharmacodynamic properties.
Development and validation of a stability-indicating RP-LC method for the simultaneous determination of otilonium bromide and its expected degradation product in bulk drug and pharmaceutical preparation
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OB is a poorly absorbed spasmolytic drug, exerting significantly greater control of the symptoms of IBS compared with placebo, suggesting that the drug could effectively be used for the long-term management of patients with IBS.
Changes in nitrergic and tachykininergic pathways in rat proximal colon in response to chronic treatment with otilonium bromide
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Otilonium bromide is used as a spasmolytic drug in the treatment of the functional bowel disorder irritable bowel syndrome but little is known about the effects of chronic administration of OB on enteric neurons, neuromuscular transmission, and interstitial cells of Cajal, key regulators of the gut function.
Colonic smooth muscle cells and colonic motility patterns as a target for irritable bowel syndrome therapy: mechanisms of action of otilonium bromide
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Otilonium bromide inhibits the main patterns of human sigmoid motility in vitro, which are spontaneous rhythmic phasic contractions, smooth muscle tone, contractions induced by stimulation of excitatory motor neurons and contraction induced by direct effect of excited neurotransmitters, thereby limiting excessive intestinal contractility and abdominal cramping.
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The aim of this study was to characterize the pharmacological effects of OB on contractile patterns in the human sigmoid colon.

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