Abstract：
:Intestinal transport of the type III phosphodiesterase inhibitor cilostazol was characterized to evaluate the influence of secretory transporter. Intestinal absorption of cilostazol measured by the in situ closed loop method, showed regional differences, with high permeability in the upper part of the small intestine. Intestinal secretory transport of cilostazol at the ileum was tended to be decreased by the increase of tested concentration of cilostazol from 10 to 20 microM when evaluated by means of a Ussing-type chamber method with mounted rat intestinal tissues. Transcellular transport of cilostazol in the basolateral-to-apical direction in LLC-GA5-COL150 cells, which overexpress P-glycoprotein, was higher than that in parental LLC-PK1 cells. In addition, cilostazol reduced the basolateral-to-apical transport and increased the accumulation of [(3)H]daunomycin in LLC-GA5-COL150 cells. Accordingly, cilostazol was demonstrated to be transported by P-glycoprotein, while cilostazol is not likely to cause induction of the expression level of P-glycoprotein by the same manner with rifampin. Apical-to-basolateral transport of cilostazol in Caco-2 cells was increased in a low concentration range, followed by a decrease with further increase of the concentration, while the permeability coefficient of cilostazol was above 1 x 10(-6) cm/s at any concentration. Initial uptake of [(14)C]cilostazol by Caco-2 cells was temperature dependent and was reduced in the presence of unlabeled cilostazol, suggesting that apical uptake is also mediated by a transporter(s). In conclusion, intestinal absorption of cilostazol, which has a high absorptive permeability, may not be significantly hampered by efflux transporters, such as P-glycoprotein.
journal_name
J Pharm Scijournal_title
Journal of pharmaceutical sciencesauthors
Toyobuku H,Tamai I,Ueno K,Tsuji Adoi
10.1002/jps.10490subject
Has Abstractpub_date
2003-11-01 00:00:00pages
2249-59issue
11eissn
0022-3549issn
1520-6017pii
S0022-3549(16)31351-Xjournal_volume
92pub_type
杂志文章abstract：:The degradation kinetics and mechanism of a potent new cephalosporin, cefotaxime sodium, in aqueous solution were investigated at pH 0-10 at 25 degrees and an ionic strength of 0.5. The degradation rates were determined by high-pressure liquid chromatography and were observed to follow pseudo first-order kinetics with...
journal_title：Journal of pharmaceutical sciences
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更新日期：2004-02-01 00:00:00
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journal_title：Journal of pharmaceutical sciences
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doi：10.1002/jps.2600761206
更新日期：1987-12-01 00:00:00
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更新日期：1995-02-01 00:00:00
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更新日期：2008-01-01 00:00:00
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更新日期：2004-02-01 00:00:00
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pub_type： 杂志文章
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更新日期：2014-02-01 00:00:00
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journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1002/jps.2600690134
更新日期：1980-01-01 00:00:00
abstract：:Taxanes such as paclitaxel (Taxol) and docetaxel (Taxotere) are promising agents for use against ovarian cancer and other malignancies. Recently, SB-T-1011, a semisynthetic taxane, has been prepared from 14-hydroxy-10-deacetylbaccatin III. SB-T-1011 shows similar or greater in vitro cytostatic activity than paclitaxel...
journal_title：Journal of pharmaceutical sciences
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