epsilon-Aminocaproic acid esters as transdermal penetration enhancing agents
Jazyk angličtina Země Spojené státy americké Médium print
Typ dokumentu srovnávací studie, časopisecké články
PubMed
8378243
DOI
10.1023/a:1018914806761
Knihovny.cz E-zdroje
- MeSH
- aminokapronáty * MeSH
- aplikace kožní MeSH
- azepiny farmakologie MeSH
- chemická stimulace MeSH
- činčila MeSH
- dráždivé látky toxicita MeSH
- indikátory a reagencie MeSH
- kožní absorpce účinky léků MeSH
- králíci MeSH
- kyselina 6-aminokapronová chemická syntéza farmakologie toxicita MeSH
- LD50 MeSH
- lidé MeSH
- myši MeSH
- rozpustnost MeSH
- techniky in vitro MeSH
- theofylin farmakokinetika MeSH
- zvířata MeSH
- Check Tag
- králíci MeSH
- lidé MeSH
- mužské pohlaví MeSH
- myši MeSH
- ženské pohlaví MeSH
- zvířata MeSH
- Publikační typ
- časopisecké články MeSH
- srovnávací studie MeSH
- Názvy látek
- aminokapronáty * MeSH
- azepiny MeSH
- dodecyl 6-aminocaproate MeSH Prohlížeč
- dráždivé látky MeSH
- indikátory a reagencie MeSH
- kyselina 6-aminokapronová MeSH
- laurocapram MeSH Prohlížeč
- octyl 6-aminocaproate MeSH Prohlížeč
- theofylin MeSH
The synthesis of epsilon-aminocaproic acid esters is described. Two representative members from a group of five of the 1-alkyl homologues synthetized as flexible analogues of 1-alkylazacyclohepatanone derivatives were evaluated in vitro for their effectiveness on the transport of theophylline through the excised human cadaver skin in comparison with Azone. The 1-octyl- and 1-dodecyl-epsilon-aminocaproic acid esters (OCEAC and DDEAC) show excellent penetration enhancement. Donor samples contained 2.5% theophylline and 1% enhancers tested in three different vehicles. Fluxes of theophylline were increased with OCEAC about 19 times from olive oil, 45 times from water, and about 38 times from water-propylene glycol (3:2) vehicle toward controls (with DDEAC about 17, 39, and 35 times, respectively) and they were markedly higher than Azone under the given conditions. Acute LD50's (i.p. in mice) of OCEAC (DDEAC) were 245 mg/kg (352 mg/kg), with a slightly lower toxicity than Azone. OCEAC and DDEAC did not exhibit acute dermal irritation in vivo on rabbits at a 5% concentration in white petrolatum.
Zobrazit více v PubMed
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