Abstract：
PURPOSE:The aim of this study is to investigate the effects of 50% ethyl acetate extracts of grapefruit juice (GFJ) and orange juice (OJ) on the transport activity of P-glycoprotein (P-gp) in the rat small intestine. METHODS:The efflux of P-gp substrates from rat everted sac in the absence or presence of verapamil, GFJ, OJ or erythromycin was measured. Rhodamine123, fexofenadine and saquinavir were used as P-gp substrates. P-gp expression levels in the rat jejunum and ileum were determined by Western blot analysis. RESULTS:The efflux of rhodamine123 from the everted sac increased from the apex of the jejunum to the low ileum and the expression of P-gp in the ileum was 2.31-fold higher than that in the jejunum. Verapamil and the 50% GFJ and OJ extracts inhibited the efflux from the intestine of all three drugs tested. Erythromycin decreased the efflux of rhodaminel23 and fexofenadine, but did not affect the efflux of saquinavir in the intestine. CONCLUSIONS:GFJ and OJ extracts inhibited the efflux of P-gp substrates from the small intestine. Therefore, they may enhance the oral bioavailability of P-gp substrates by increasing absorption in the small intestine.
journal_name
Pharm Resjournal_title
Pharmaceutical researchauthors
Tian R,Koyabu N,Takanaga H,Matsuo H,Ohtani H,Sawada Ydoi
10.1023/a:1016100715125subject
Has Abstractpub_date
2002-06-01 00:00:00pages
802-9issue
6eissn
0724-8741issn
1573-904Xjournal_volume
19pub_type
杂志文章abstract：PURPOSE:This study aimed to characterize the transepithelial transport of miltefosine (HePC), the first orally effective drug against visceral leishmaniasis, across the intestinal barrier to further understand its oral absorption mechanism. MATERIALS AND METHODS:Caco-2 cell monolayers were used as an in vitro model of...
journal_title：Pharmaceutical research
pub_type： 杂志文章
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更新日期：2007-03-01 00:00:00
abstract：PURPOSE:The intratumoral heterogeneity observed in breast cancer (BC), in particular with regard to cell surface receptor expression, can hinder the success of many targeted cancer therapies. The development of novel therapeutic agents that target more than one receptor can overcome this inherent property of tumors and...
journal_title：Pharmaceutical research
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journal_title：Pharmaceutical research
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doi：10.1023/A:1016356926714
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abstract：:The molecular environment of sucrose and mineral oil within sucrose and mineral oil solid state emulsions was investigated by NMR techniques. The 13C and 1H chemical shifts of sucrose and mineral oil to those observed in solid state emulsions (comprised of sucrose and mineral oil) were equivalent, indicating that the ...
journal_title：Pharmaceutical research
pub_type： 杂志文章
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journal_title：Pharmaceutical research
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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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journal_title：Pharmaceutical research
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更新日期：2015-05-01 00:00:00
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更新日期：2005-01-01 00:00:00
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journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1023/a:1022202926073
更新日期：2003-01-01 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
doi：10.1023/a:1016462205267
更新日期：2002-07-01 00:00:00
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journal_title：Pharmaceutical research
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journal_title：Pharmaceutical research
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abstract：PURPOSE:Interferon beta is commonly used as therapeutic in the first line of therapy for multiple sclerosis. However, depending on the product, it induces an antibody response in up to 60% of patients. This study evaluated the impact of therapy related factors like dose, route of administration and administration frequ...
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更新日期：2013-06-01 00:00:00
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journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1023/a:1018979703726
更新日期：1994-12-01 00:00:00
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更新日期：2009-07-01 00:00:00
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更新日期：2020-09-28 00:00:00
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更新日期：2014-06-01 00:00:00
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更新日期：2019-08-14 00:00:00
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abstract：:A number of substituted phthalimide, 1, 8-naphthalimide, succinimide and glutarimide derivatives demonstrated significant hypolipidemic activity at 20 mg/kg/ day, I.P. after 16 days dosing. The N-(n-pentyl) succinimide proved to be the most potent analogue of the new compounds, lowering serum triglyceride levels 51 % ...
journal_title：Pharmaceutical research
pub_type： 杂志文章
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更新日期：1984-11-01 00:00:00
abstract：PURPOSE:The in vitro inhibitory effect of Docetaxel (DTX) and Everolimus (EVR) alone and together in poly(ethylene glycol)-block-poly(D,L-lactic acid) (PEG-b-PLA) nanocarriers on angiogenic processes and acute toxicity in mice was evaluated. METHODS:PEG-b-PLA DTX and/or EVR nanocarriers were characterized for size, dr...
journal_title：Pharmaceutical research
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更新日期：2014-03-01 00:00:00
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journal_title：Pharmaceutical research
pub_type： 杂志文章
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更新日期：1999-01-01 00:00:00
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journal_title：Pharmaceutical research
pub_type： 杂志文章
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更新日期：1985-09-01 00:00:00
abstract：:The technique of Affinity capillary electrophoresis (ACE) is a useful tool to characterize complexation and partition equilibria. A wide range of applications in pharmaceutics has been presented: the determination of pKA values, of association constants between drugs and cyclodextrins or amphiphilic compounds as well ...
journal_title：Pharmaceutical research
pub_type： 杂志文章,评审
doi：
更新日期：1999-11-01 00:00:00
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journal_title：Pharmaceutical research
pub_type： 杂志文章
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更新日期：2010-12-01 00:00:00
