Abstract:
PURPOSE:Highly lipophilic basic drugs, the antiestrogens AE 1 (log P = 5.82) and AE 2 (log P = 7.8) shall be delivered transdermally. METHODS:Transdermal permeation of drugs, enhancers, and solvents from various fluid formulations were characterized by in-vitro permeation studies through excised skin of hairless mice. Furthermore, differential scanning calorimetry (DSC) measurements of skin lipid phase transition temperatures were conducted. RESULTS:Transdermal flux of highly lipophilic drugs was extraordinarily enhanced by the unique permeation enhancer combination propylene glycol-lauric acid (9 + 1): steady-state fluxes of AE 1 and AE 2 were as high as 5.8 microg x cm(-2) x h(-1) and 3.2 microg x cm(-2) x h(-1), respectively. This dual enhancer formulation also resulted in a marked increase in the transdermal fluxes of the enhancers. Furthermore, skin lipid phase transition temperatures were significantly reduced by treatment with this formulation. CONCLUSION:Transdermal delivery of highly lipophilic drugs can be realized by using the permeation enhancer combination propylene glycol-lauric acid. The extraordinary permeation enhancement for highly lipophilic drugs by this formulation is due to mutual permeation enhancement of these two enhancers and their synergistic lipid-fluidising activity in the stratum corneum.
journal_name
Pharm Resjournal_title
Pharmaceutical researchauthors
Funke AP,Schiller R,Motzkus HW,Günther C,Müller RH,Lipp Rdoi
10.1023/a:1015314314796subject
Has Abstractpub_date
2002-05-01 00:00:00pages
661-8issue
5eissn
0724-8741issn
1573-904Xjournal_volume
19pub_type
杂志文章abstract:PURPOSE:To determine by pharmacokinetic (PK) means the role of erythropoietin-receptor (EPO-R) upregulation in fetuses on the elimination of erythropoietin (EPO). MATERIALS AND METHODS:Six fetal sheep were catheterized at a gestational age of 125-127 days and phlebotomized daily for 6 days. Paired tracer PK studies us...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-007-9295-3
更新日期:2007-09-01 00:00:00
abstract::Aucubin, a promising hepatoprotecting iridoid glucoside, was given intravenously (iv), orally (po), intraperitoneally (ip), and hepatoportally (pv) to rats. A linear pharmacokinetic behavior was obtained after iv administation of 400-400 mg/kg of aucubin. The half-life of aucubin in the postdistributive phase (t1/2, b...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1015821527621
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journal_title:Pharmaceutical research
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doi:10.1007/s11095-006-9056-8
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journal_title:Pharmaceutical research
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更新日期:2015-07-01 00:00:00
abstract:PURPOSE:The objective of this work is to understand the sequence specificity of HAV peptides and to improve their selectivity in regulating E-cadherin-E-cadherin interactions in the intercellular junctions. METHODS:Peptide 1 was modified using an alanine scanning method to give peptides 2-6. The ability of these pepti...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1011094025008
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journal_title:Pharmaceutical research
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更新日期:2017-11-01 00:00:00
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journal_title:Pharmaceutical research
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journal_title:Pharmaceutical research
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journal_title:Pharmaceutical research
pub_type: 杂志文章
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更新日期:2003-06-01 00:00:00
abstract:PURPOSE:To compare the adjuvanticity of polymeric particles (new-generation adjuvant) and alum (the traditional and FDA-approved adjuvant) for H5N1 influenza split vaccine, and to investigate respective action mode. METHODS:Vaccine formulations were prepared by incubating lyophilized poly(lactic acid) (PLA) microparti...
journal_title:Pharmaceutical research
pub_type: 杂志文章
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更新日期:2014-04-01 00:00:00
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journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-012-0731-7
更新日期:2012-08-01 00:00:00
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journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1018964401677
更新日期:1993-11-01 00:00:00
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journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-011-0397-6
更新日期:2011-07-01 00:00:00
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journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1018908705446
更新日期:1999-10-01 00:00:00
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journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/b:pham.0000041469.96466.12
更新日期:2004-09-01 00:00:00
abstract:PURPOSE:To evaluate the effects of several buffers and excipients on the stability of glucagon during freeze-drying and storage as dried powder formulations. METHODS:The chemical and physical stability of glucagon in freeze-dried solid formulations was evaluated by a variety of techniques including mass spectrometry (...
journal_title:Pharmaceutical research
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doi:10.1007/s11095-012-0820-7
更新日期:2012-12-01 00:00:00
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journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1015828027060
更新日期:1992-04-01 00:00:00
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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:1016212804288
更新日期:1995-03-01 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:1999-07-01 00:00:00
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更新日期:2020-04-14 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:2016-01-01 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:2013-08-01 00:00:00
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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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更新日期:2004-07-01 00:00:00
abstract::Photodegradation of solutions of metronidazole in the presence and absence of sodium urate was studied. Photodegradation appeared to follow zero-order kinetics and was found to be dependent on the pH, buffer species, sodium urate concentration, and light source. Complex formation between metronidazole and sodium urate...
journal_title:Pharmaceutical research
pub_type: 杂志文章
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更新日期:1989-01-01 00:00:00