In vitro kinetics of amiodarone and its major metabolite in two human liver cell models after acute and repeated treatments
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- 作者：Giuliana Pomponioa ; e ; 1 ; Camille C. Savaryb ; 1 ; Cé ; line Parmentierc ; 1 ; Frederic Boisd ; 1 ; André ; Guillouzob ; Luca Romanellie ; Lysiane Richertc ; f ; Emma Di Consiglioa ; emma.diconsiglio@iss.it" class="auth_mail" title="E-mail the corresponding author ; Emanuela Testaia
- 关键词：AMI ; amiodarone ; MDEA ; mono-N-desethylamiodarone ; DDEA ; di-N-desethylamiodarone ; PHH ; primary human hepatocytes ; CYP ; cytochrome P450 ; DMSO ; dimetylsulfoxide ; MeOH ; methanol ; HMM ; Hepatocyte Maintenance Medium ; FCS ; fetal calf serum ; SW ; sandwich ; d0 ; day 0 ; d13 ; day 13 ; TP ; time point ; LOD ; limit of detection ; ADR ; adverse drug reactions ; PBPK ; Physiologically Based Pharmacokinetic models ; PBBK ; physiologically based biokinetic models
- 刊名：Toxicology in Vitro
- 出版年：2015
- 出版时间：25 December 2015
- 年：2015
- 卷：30
- 期：1
- 页码：36-51
- 全文大小：3104 K
文摘
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Amiodarone biokinetics was studied and modelled in two human liver cells after acute and repeated treatment.
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Amiodarone bioavailability was influenced by abiotic processes.
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It is rapidly uptaken and efficiently metabolised to MDEA in HepaRG and in PHH.
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MDEA accumulated into the cells much more than the parent over time, especially in HepaRG.
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The treatment induced phospholipidosis in HepaRG.