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Predicate | Object |
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rdf:type | |
lifeskim:mentions | |
pubmed:issue |
10
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pubmed:dateCreated |
1992-3-16
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pubmed:abstractText |
The in vitro transdermal absorption of five calcium channel antagonists (nifedipine, nitrendipine, nicardipine, felodipine, and nimodipine) was studied using the skin of hairless rats as a membrane. The aim of this study was to determine the penetration parameters [permeability constant (Kp), lag time (T1, and flux (J)] as measures of the intrinsic transdermal permeabilities of these drugs, in order to predict the potential capacity of these drugs to be formulated in a therapeutical transdermal system (TTS). Reliable prediction of Kp values, using K'w (extrapolated capacity factor in 100% water) and P (n-octanol-water partition coefficient) values as independent variables in the parabolic, bilinear, and hyperbolic functions, were assayed. Nicardipine showed a higher mean transdermal penetration (Kp; 4.9 x 10(-3) cm.h-1) value than the other dihydropyridines. Nifedipine showed the shortest mean T1 value (5.1 h). The permeability rate constants of the calcium channel antagonists assayed can be predicted from their n-octanol-water partition coefficients, using the parabolic function (r = 0.984, p less than 0.01). Nicardipine would be the most suitable candidate for formulation in a TTS design.
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pubmed:language |
eng
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pubmed:journal | |
pubmed:citationSubset |
IM
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pubmed:chemical | |
pubmed:status |
MEDLINE
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pubmed:month |
Oct
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pubmed:issn |
0022-3549
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pubmed:author | |
pubmed:issnType |
Print
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pubmed:volume |
80
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
931-4
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pubmed:dateRevised |
2008-11-21
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pubmed:meshHeading |
pubmed-meshheading:1784001-Administration, Cutaneous,
pubmed-meshheading:1784001-Animals,
pubmed-meshheading:1784001-Calcium Channel Blockers,
pubmed-meshheading:1784001-Chemistry, Physical,
pubmed-meshheading:1784001-Chromatography, High Pressure Liquid,
pubmed-meshheading:1784001-Male,
pubmed-meshheading:1784001-Physicochemical Phenomena,
pubmed-meshheading:1784001-Rats,
pubmed-meshheading:1784001-Skin Absorption,
pubmed-meshheading:1784001-Solubility,
pubmed-meshheading:1784001-Spectrophotometry, Ultraviolet
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pubmed:year |
1991
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pubmed:articleTitle |
A comparative in vitro study of transdermal absorption of a series of calcium channel antagonists.
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pubmed:affiliation |
Department of Pharmacy, University of Barcelona, Spain.
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pubmed:publicationType |
Journal Article,
Comparative Study,
In Vitro,
Research Support, Non-U.S. Gov't
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