About: Investigation of new acyloxy derivatives of cholic acid and their esters as drug absorption modifiers     Goto   Sponge   NotDistinct   Permalink

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  • Skin penetration enhancers are used in the formulation of transdermal delivery systems for drugs that are otherwise not sufficiently skin-permeable. Intestinal absorption promoters/enhancers are used as excipients in oral formulations of poorly oral-bioavailable drugs. Series of fourteen acyloxy derivatives of 5 beta-cholic acid as potential drug absorption modifiers was generated by multistep synthesis. The synthesis of all newly prepared compounds is presented here. Structure confirmation of all generated compounds was accomplished by (1)H NMR, (13)C NMR, IR and MS spectroscopy methods. All the prepared compounds were analyzed using RP-TLC, and their lipophilicity (R(M)) was determined. The hydrophobicity (log P) and solubility (logS) of the studied compounds were also calculated using two commercially available programs. All the target compounds were tested for their in vitro transdermal penetration activity and as potential intestinal absorption enhancers.
  • Skin penetration enhancers are used in the formulation of transdermal delivery systems for drugs that are otherwise not sufficiently skin-permeable. Intestinal absorption promoters/enhancers are used as excipients in oral formulations of poorly oral-bioavailable drugs. Series of fourteen acyloxy derivatives of 5 beta-cholic acid as potential drug absorption modifiers was generated by multistep synthesis. The synthesis of all newly prepared compounds is presented here. Structure confirmation of all generated compounds was accomplished by (1)H NMR, (13)C NMR, IR and MS spectroscopy methods. All the prepared compounds were analyzed using RP-TLC, and their lipophilicity (R(M)) was determined. The hydrophobicity (log P) and solubility (logS) of the studied compounds were also calculated using two commercially available programs. All the target compounds were tested for their in vitro transdermal penetration activity and as potential intestinal absorption enhancers. (en)
Title
  • Investigation of new acyloxy derivatives of cholic acid and their esters as drug absorption modifiers
  • Investigation of new acyloxy derivatives of cholic acid and their esters as drug absorption modifiers (en)
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  • Investigation of new acyloxy derivatives of cholic acid and their esters as drug absorption modifiers
  • Investigation of new acyloxy derivatives of cholic acid and their esters as drug absorption modifiers (en)
skos:notation
  • RIV/61389030:_____/11:00368601!RIV12-AV0-61389030
http://linked.open...avai/riv/aktivita
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  • P(2B06024), P(ED0007/01/01), P(GA301/08/1649), P(GAP304/10/1951), V, Z(AV0Z50380511), Z(MSM6046137305)
http://linked.open...iv/cisloPeriodika
  • 10-11
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  • 205712
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  • RIV/61389030:_____/11:00368601
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  • Cholic acid derivatives; Lipophilicity; Transdermal penetration enhancers; Intestinal absorption promoters; In vitro cytotoxicity (en)
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  • US - Spojené státy americké
http://linked.open...ontrolniKodProRIV
  • [05B434DFC426]
http://linked.open...i/riv/nazevZdroje
  • Steroids
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http://linked.open...v/svazekPeriodika
  • 76
http://linked.open...iv/tvurceVysledku
  • Drašar, P.
  • Král, V.
  • Dvořáková, L.
  • Dohnal, J.
  • Jampílek, J.
  • Mandelová, Z.
  • Mrozek, L.
  • Opatřilová, R.
  • Paleta, O.
  • Plaček, L.
  • Rárová, Lucie
  • Řezáčová, A.
http://linked.open...ain/vavai/riv/wos
  • 000294074700019
http://linked.open...n/vavai/riv/zamer
issn
  • 0039-128X
number of pages
http://bibframe.org/vocab/doi
  • 10.1016/j.steroids.2011.04.014
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