Institutional Repository

The disposition of diammonium glycyrrhizinate and glycyrrhetinic acid in the isolated perfused rat intestine and liver

Show simple item record

dc.contributor.author Yang J. en
dc.contributor.author Zhou L. en
dc.contributor.author Wang J. en
dc.contributor.author Wang C. en
dc.contributor.author Davey A.K. en
dc.date.accessioned 2012-11-01T16:31:26Z
dc.date.available 2012-11-01T16:31:26Z
dc.date.issued 2008 en
dc.identifier.citation Planta Medica en
dc.identifier.citation 74 en
dc.identifier.citation 11 en
dc.identifier.issn 320943 en
dc.identifier.other 10.1055/s-2008-1081328 en
dc.identifier.uri http://hdl.handle.net/10500/7215
dc.description.abstract The major component of liquorice root extract, glycyrrhizinate (GZ), has been formulated as an injection for the treatment of hepatitis. If given orally, GZ has poor bioavailability and is catalysed to glycyrrhetinic acid (GA) by intestinal bacteria. GA is subsequently responsible for significant side effects. This study was conducted to clarify the relationship between GZ and GA absorption and bioavailability. GZ and GA absorption were investigated using the in situ single pass isolated perfused intestine (IPI). Hepatic disposition was investigated using isolated perfused liver (IPL) and in vivo biliary excretion models. The apparent permeability and absorption rate constants in the IPI for GZ were 0.36 ± 0.31 cm/ min and 0.35 ±0.33 min-1, while those for GA were 5.73 ± 0.11 cm/min and 1.53 ± 0.05 min -1, re spectively. The hepatic extraction ratios of unbound GZ and GA in the IPL were 0.22 ± 0.01 and 0.44 ±0.15, respectively. Seven hours after intraportal venous injection in vivo, the cumulative biliary excretion ratio for GZ was 96%. There was negligible biliary excretion of unchanged GA during the same period. It was apparent in all models used that in the absence of intestinal bacteria GZ was not metabolised to GA, or vice versa. Hence, GZ can be absorbed unchanged from the intestine provided it has sufficient time and is protected from intestinal bacteria. This opens up the possibility that the use of pharmaceutical carrier systems or similar formulation approaches may allow effective oral administration of therapeutic levels of GZ without the side effects associated with GA. © Georg Thieme Verlag KG. en
dc.language.iso en en
dc.subject Glycyrrhetinic acid; Glycyrrhizinate; Perfused intestine; Perfused liver; Pharmacokinetics; Rat diammonium glycyrrhizinate; glycyrrhetinic acid; Glycyrrhiza extract; unclassified drug; animal tissue; area under the curve; article; controlled study; drug absorption; drug bioavailability; drug disposition; drug formulation; Glycyrrhiza; high performance liquid chromatography; in vivo study; intestine flora; male; nonhuman; organ perfusion; rat; Animals; Glycyrrhetinic Acid; Glycyrrhizic Acid; Intestinal Absorption; Intestine, Small; Liver; Male; Perfusion; Rats; Rats, Sprague-Dawley; Rattus en
dc.title The disposition of diammonium glycyrrhizinate and glycyrrhetinic acid in the isolated perfused rat intestine and liver en
dc.type Article en


Files in this item

Files Size Format View

There are no files associated with this item.

This item appears in the following Collection(s)

Show simple item record

Search UnisaIR


Browse

My Account

Statistics