Abstract:
:The intestinal lymphatic absorption of cyclosporin A (CyA) following oral administration of 6.5 +/- 0.6 and 25.2 +/- 1.4 mg kg-1 doses of the drug dissolved in an olive oil solution was studied using a thoracic duct-cannulated rat model. Cumulative lymph samples were collected for up to 114 h post-dosing and assayed by liquid scintillation counting. In this study, the estimated amount of lymphatically absorbed CyA was 0.35 +/- 0.13 and 0.47 +/- 0.29 per cent of the respective doses. In terms of the overall oral bioavailability of CyA (Fpo) by all absorptive mechanisms, the intestinal lymphatics accounted for the absorption of approximately 2 per cent of the total amount of absorbed drug. Fpo was 21.3 +/- 2.5 per cent. The results of this study suggested that lipophilicity alone was not the only factor governing intestinal lymphatic drug absorption. An explanation for the low level of lymphatic CyA absorption is presented. In addition, some reasons for the low overall oral bioavailability of CyA are discussed.
journal_name
Biopharm Drug Disposjournal_title
Biopharmaceutics & drug dispositionauthors
Ueda CT,Lemaire M,Gsell G,Nussbaumer Kdoi
10.1002/bdd.2510040203subject
Has Abstractpub_date
1983-04-01 00:00:00pages
113-24issue
2eissn
0142-2782issn
1099-081Xjournal_volume
4pub_type
杂志文章abstract::A high-performance liquid chromatographic method was developed to determine stobadin pharmacokinetics in dog and man. The relative bioavailability of stobadin dipalmitate compared with dihydrochloride was 46.4 per cent in dog. In man peak serum concentrations ranged from 12 to 289 ng ml-1 after a single oral dose of s...
journal_title:Biopharmaceutics & drug disposition
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journal_title:Biopharmaceutics & drug disposition
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journal_title:Biopharmaceutics & drug disposition
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journal_title:Biopharmaceutics & drug disposition
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journal_title:Biopharmaceutics & drug disposition
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journal_title:Biopharmaceutics & drug disposition
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journal_title:Biopharmaceutics & drug disposition
pub_type: 临床试验,杂志文章,随机对照试验
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journal_title:Biopharmaceutics & drug disposition
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journal_title:Biopharmaceutics & drug disposition
pub_type: 杂志文章
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journal_title:Biopharmaceutics & drug disposition
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journal_title:Biopharmaceutics & drug disposition
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journal_title:Biopharmaceutics & drug disposition
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journal_title:Biopharmaceutics & drug disposition
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更新日期:2012-12-01 00:00:00
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journal_title:Biopharmaceutics & drug disposition
pub_type: 杂志文章,评审
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更新日期:2010-10-01 00:00:00
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journal_title:Biopharmaceutics & drug disposition
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journal_title:Biopharmaceutics & drug disposition
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journal_title:Biopharmaceutics & drug disposition
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journal_title:Biopharmaceutics & drug disposition
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journal_title:Biopharmaceutics & drug disposition
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journal_title:Biopharmaceutics & drug disposition
pub_type: 临床试验,杂志文章,随机对照试验
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journal_title:Biopharmaceutics & drug disposition
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journal_title:Biopharmaceutics & drug disposition
pub_type: 临床试验,杂志文章,随机对照试验
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更新日期:1987-01-01 00:00:00
abstract::Telaprevir, a chronic hepatitis C virus (HCV) protease inhibitor, is known to be a cytochrome P450 (CYP) 3A4/5 substrate and inhibitor. In the present study, the in vitro inhibitory effect of telaprevir on the metabolism of tacrolimus in human liver microsomes was investigated using 13-O-demethyltacrolimus (M-I) as a ...
journal_title:Biopharmaceutics & drug disposition
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更新日期:2014-12-01 00:00:00
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journal_title:Biopharmaceutics & drug disposition
pub_type: 临床试验,杂志文章,随机对照试验
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journal_title:Biopharmaceutics & drug disposition
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journal_title:Biopharmaceutics & drug disposition
pub_type: 杂志文章
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更新日期:2016-07-01 00:00:00
abstract::We present a novel method for performing pharmacokinetic and metabolism studies on macromolecules that offers advantages over the existing techniques of radiolabeling, immunoassay or bioassays. Our strategy uses macromolecules with stable isotopes uniformly distributed throughout the structure. The stable isotope enri...
journal_title:Biopharmaceutics & drug disposition
pub_type: 杂志文章
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更新日期:1998-10-01 00:00:00
abstract::MDL 26479 is a new drug undergoing clinical evaluation for the treatment of depression and for memory loss associated with Alzheimer's disease. As part of a dose tolerance trial, the single- (SD) and multiple-dose (MD) pharmacokinetics of MDL 26479 were evaluated in healthy male volunteers. SDs ranging from 2 to 465 m...
journal_title:Biopharmaceutics & drug disposition
pub_type: 临床试验,杂志文章,随机对照试验
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更新日期:1997-05-01 00:00:00