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dc.contributor.authorYang, J
dc.contributor.authorZhou, L
dc.contributor.authorWang, J
dc.contributor.authorWang, C
dc.contributor.authorDavey, AK
dc.date.accessioned2017-05-03T14:05:56Z
dc.date.available2017-05-03T14:05:56Z
dc.date.issued2008
dc.date.modified2011-08-30T06:21:46Z
dc.identifier.issn0032-0943
dc.identifier.doi10.1055/s-2008-1081328
dc.identifier.urihttp://hdl.handle.net/10072/40479
dc.description.abstractThe 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 ᠰ.31 cm/min and 0.35 ᠰ.33 min-1, while those for GA were 5.73 ᠰ.11 cm/min and 1.53 ᠰ.05 min-1, respectively. The hepatic extraction ratios of unbound GZ and GA in the IPL were 0.22 ᠰ.01 and 0.44 ᠰ.15, respectively. Seven hours after intra-portal 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.
dc.description.peerreviewedYes
dc.description.publicationstatusYes
dc.languageEnglish
dc.language.isoeng
dc.publisherGeorg Thieme Verlag
dc.publisher.placeGermany
dc.relation.ispartofstudentpublicationN
dc.relation.ispartofpagefrom1351
dc.relation.ispartofpageto1356
dc.relation.ispartofissue11
dc.relation.ispartofjournalPlanta Medica
dc.relation.ispartofvolume74
dc.rights.retentionY
dc.subject.fieldofresearchPlant biology
dc.subject.fieldofresearchTraditional, complementary and integrative medicine
dc.subject.fieldofresearchPharmacology and pharmaceutical sciences
dc.subject.fieldofresearchBasic pharmacology
dc.subject.fieldofresearchcode3108
dc.subject.fieldofresearchcode4208
dc.subject.fieldofresearchcode3214
dc.subject.fieldofresearchcode321401
dc.titleThe disposition of diammonium glycyrrhizinate and glycyrrhetinic acid in the isolated perfused rat intestine and liver
dc.typeJournal article
dc.type.descriptionC1 - Articles
dc.type.codeC - Journal Articles
gro.date.issued2008
gro.hasfulltextNo Full Text
gro.griffith.authorDavey, Andrew


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