Abstract：
:A characterization and optimization of the in vitro transdermal iontophoretic transport of 5-hydroxy-2-(N,N,-di-n-propylamino)tetralin (5-OH-DPAT) is presented. The utility of acetaminophen as a marker of electroosmotic flow was studied as well. The following parameters of iontophoretic transport of 5-OH-DPAT were examined: drug donor concentration, electroosmotic contribution, influence of co-ions, current density, and composition of the acceptor phase. The steady-state flux (Flux(ss)) of acetaminophen was linearly correlated with the donor concentration and co-iontophoresis of acetaminophen did not influence the iontophoretic flux of 5-OH-DPAT, indicating that acetaminophen is an excellent marker of electroosmotic flow. Lowering the Na(+) concentration from 78 to 10 mM in the donor phase, resulted in a 2.5-fold enhancement of the Flux(ss). The Flux(ss) showed a nonlinear relation with the drug donor concentration and an excellent linear correlation with the current density. Reducing the pH of the acceptor phase from 7.4 to 6.2 resulted in a dramatic decrease of the Flux(ss) of 5-OH-DPAT, explained by a reduced electroosmotic flow and an increased counter-ion flow. Optimization of the conditions resulted in a maximum Flux(ss) of 5-OH-DPAT of 1.0 micromol x cm(-2) h(-1) demonstrating the potential of the iontophoretic delivery of this dopamine agonist for the symptomatic treatment of Parkinson's disease.
journal_name
J Pharm Scijournal_title
Journal of pharmaceutical sciencesauthors
Ackaert OW,Van Smeden J,De Graan J,Dijkstra D,Danhof M,Bouwstra JAdoi
10.1002/jps.21833subject
Has Abstractpub_date
2010-01-01 00:00:00pages
275-85issue
1eissn
0022-3549issn
1520-6017pii
S0022-3549(16)30337-9journal_volume
99pub_type
杂志文章abstract：:The effect of micellar sodium lauryl sulfate on the rate of cupric-ion-promoted hydrolysis of some dicarboxylic acid hemiesters was investigated at pH 5, ionic strength 0.1 M, and 40, 45, and 50 degrees. The rate of cupric-ion-promoted hydrolysis of sodium n-decyloxalate in the micellar phase is about 50 times as fast...
journal_title：Journal of pharmaceutical sciences
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更新日期：1993-05-01 00:00:00
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journal_title：Journal of pharmaceutical sciences
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doi：10.1002/jps.23709
更新日期：2013-11-01 00:00:00
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journal_title：Journal of pharmaceutical sciences
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doi：10.1002/jps.10038
更新日期：2002-02-01 00:00:00
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更新日期：1990-08-01 00:00:00
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journal_title：Journal of pharmaceutical sciences
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abstract：:Solubilization of nonpolar drugs constitutes one of the most important tasks in parenteral formulations design. This study investigates and assesses the solubility enhancement of Fluasterone by various techniques including cosolvency, micellization, and complexation. Of the solubilizing agents used, the modified beta-...
journal_title：Journal of pharmaceutical sciences
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journal_title：Journal of pharmaceutical sciences
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更新日期：1975-08-01 00:00:00
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journal_title：Journal of pharmaceutical sciences
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doi：10.1002/jps.2600670106
更新日期：1978-01-01 00:00:00
abstract：:The plasma concentrations and urinary excretions of bisoprolol enantiomers in four Japanese male healthy volunteers after a single oral administration of 20 mg of racemic bisoprolol were evaluated. The AUC(infinity) and elimination half-life of (S)-(-)-bisoprolol were slightly larger than those of (R)-(+)-bisoprolol i...
journal_title：Journal of pharmaceutical sciences
pub_type： 临床试验,杂志文章
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更新日期：1998-03-01 00:00:00
