Abstract：
:Recently a new in vivo approach in man, using a regional intestinal perfusion technique, has been developed. The perfusion tube consists of a multichannel tube with two inflatable balloons, which are placed 10 cm apart. The tube is introduced orally and the time required for insertion and positioning of the tube is approximately 1 hr. In the present study eight healthy subjects were perfused in the proximal jejunum on three separate occasions. The first two perfusion experiments used the same flow rate, 3 ml/min, and the third experiment used 6 ml/min. Phenazone (antipyrine) was chosen as the model drug. The recovery of PEG 4000 in the outlet intestinal perfusate was complete in experiments 1 and 2, but slightly lower (90%) when the higher flow rate was used. The mean (+/- SD) fraction of phenazone absorbed calculated from perfusion data was 51 +/- 12% (3 ml/min), 64 +/- 19% (3 ml/min), and 42 +/- 27% (6 ml/min) for the three experiments, respectively. The mean fraction absorbed estimated by deconvolution of the plasma data was 47 +/- 16%, 51 +/- 19%, and 38 +/- 26%, respectively. The effective permeability of phenazone was 5.3 +/- 2.5, 11 +/- 6.8, and 11 +/- 12 (x 10(4) cm/sec, respectively. We have shown that it was possible to establish a tight intestinal segment which behaved as a well-mixed compartment. The low perfusion rate of 3 ml/min was preferred, since it resulted in the lowest variability in absorption.(ABSTRACT TRUNCATED AT 250 WORDS)
journal_name
Pharm Resjournal_title
Pharmaceutical researchauthors
Lennernäs H,Ahrenstedt O,Hällgren R,Knutson L,Ryde M,Paalzow LKdoi
10.1023/a:1015888813741subject
Has Abstractpub_date
1992-10-01 00:00:00pages
1243-51issue
10eissn
0724-8741issn
1573-904Xjournal_volume
9pub_type
杂志文章abstract：:We report the chemical and enzymatic hydrolysis of two hydrophobic prodrugs of ganciclovir (3 = dipropionate ester; 4 = diadamantoate ester). Both prodrugs undergo hydrolysis showing a pH dependence of kobs = kH+aH+ + ko + kHO-aHO- and a pH of maximum stability near pH 5. Only 4 exhibited a shelf life (t90) greater th...
journal_title：Pharmaceutical research
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更新日期：1991-11-01 00:00:00
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journal_title：Pharmaceutical research
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journal_title：Pharmaceutical research
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pub_type： 杂志文章,评审
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更新日期：2008-03-01 00:00:00
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更新日期：2016-03-01 00:00:00
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journal_title：Pharmaceutical research
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更新日期：2009-04-01 00:00:00
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journal_title：Pharmaceutical research
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journal_title：Pharmaceutical research
pub_type： 杂志文章
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更新日期：2012-10-01 00:00:00
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journal_title：Pharmaceutical research
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更新日期：1998-03-01 00:00:00
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更新日期：2011-04-01 00:00:00
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journal_title：Pharmaceutical research
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更新日期：2005-06-01 00:00:00
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更新日期：2005-08-01 00:00:00
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更新日期：2020-01-07 00:00:00
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更新日期：2016-10-01 00:00:00
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journal_title：Pharmaceutical research
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更新日期：2007-01-01 00:00:00
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journal_title：Pharmaceutical research
pub_type： 杂志文章,评审
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更新日期：2014-11-01 00:00:00
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journal_title：Pharmaceutical research
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doi：10.1023/a:1016216611809
更新日期：1995-12-01 00:00:00
