Please use this identifier to cite or link to this item: http://hdl.handle.net/20.500.11889/5312
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dc.contributor.authorLi, Ming
dc.contributor.authorSi, Luqin
dc.contributor.authorPan, Hongping
dc.contributor.authorRabba, Abdullah K.
dc.contributor.authorYan, Fang
dc.contributor.authorQiu, Jun
dc.contributor.authorLi, Gao
dc.date.accessioned2018-01-08T06:10:59Z
dc.date.available2018-01-08T06:10:59Z
dc.date.issued2011
dc.identifier.urihttp://hdl.handle.net/20.500.11889/5312
dc.description.abstractIn rats we examined the effects of some common excipients on the intestinal absorption of ganciclovir (GCV), a BCS-III drug and substrate of P-gp, by assessing its in vitro transfer from mucosa to serosa and in situ transepithelial permeation. In vitro, all selected excipients (concentration range 0.1–1% [w/v]) could increase the transport amount of GCV in the everted gut sac model. Whereas enhancement by F-68 demonstrated regional differences like verapamil, PEG-400, Tween-80 and EL-35 exhibited no regional differences. In situ studies were performed by an improved perfusion model, single-pass perfusion with whole small intestine, to determine more accurately the permeability of lipophobic compounds. The permeability of GCV was significantly increased by all excipients. The effects of EL-35 and F-68 were dose-dependent but those of PEG-400 and Tween-80 were not. The results suggest that enhancements of intestinal absorption of GCV by these excipients are probably due to inhibition of P-gp mediated drug efflux. It could be deduced from their different properties that both blocking binding sites of P-gp and altering membrane fluidity were involved in their P-gp-inhibition. The former mechanism might be involved for F-68, while the latter one might account for the effects of PEG-400, Tween-80 and EL-35.en_US
dc.language.isoen_USen_US
dc.subjectExcipientsen_US
dc.subjectGanciclovir - Absorption and adsorptionen_US
dc.subjectIntestinal absorptionen_US
dc.subjectP-glycoprotein - Absorption and adsorptionen_US
dc.subjectPerfusion (Physiology)en_US
dc.titleExcipients enhance intestinal absorption of ganciclovir by P-gp inhibition : assessed in vitro by everted gut sac and in situ by improved intestinal perfusionen_US
dc.typeArticleen_US
newfileds.departmentPharmacy - Nursing and Health Professionsen_US
newfileds.item-access-typeopen_accessen_US
newfileds.thesis-prognoneen_US
newfileds.general-subjectHuman Biology, Medicine and Health Sciences | الطب والعلوم الطبيةen_US
item.grantfulltextopen-
item.languageiso639-1other-
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