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

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rdf:type	skos:Concept http://linked.opendata.cz/ontology/domain/vavai/Vysledek
Description	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)
skos:prefLabel	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	P V Z
http://linked.open...avai/riv/aktivity	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
http://linked.open...vai/riv/dodaniDat	2012
http://linked.open...aciTvurceVysledku	Rárová, Lucie
http://linked.open.../riv/druhVysledku	J - Článek v odborném periodiku
http://linked.open...iv/duvernostUdaju	S - Úplné a pravdivé údaje nepodléhající ochraně podle zvláštních právních předpisů
http://linked.open...titaPredkladatele	Ústav experimentální botaniky AV ČR, v. v. i.
http://linked.open...dnocenehoVysledku	205712
http://linked.open...ai/riv/idVysledku	RIV/61389030:_____/11:00368601
http://linked.open...riv/jazykVysledku	eng - angličtina
http://linked.open.../riv/klicovaSlova	Cholic acid derivatives; Lipophilicity; Transdermal penetration enhancers; Intestinal absorption promoters; In vitro cytotoxicity (en)
http://linked.open.../riv/klicoveSlovo	Cholic acid derivatives In vitro cytotoxicity Intestinal absorption promoters Transdermal penetration enhancers Lipophilicity
http://linked.open...odStatuVydavatele	US - Spojené státy americké
http://linked.open...ontrolniKodProRIV	[05B434DFC426]
http://linked.open...i/riv/nazevZdroje	Steroids
http://linked.open...in/vavai/riv/obor	CE
http://linked.open...ichTvurcuVysledku	1 (xsd:int)
http://linked.open...cetTvurcuVysledku	12 (xsd:int)
http://linked.open...vavai/riv/projekt	Supramolecular materials based on natural phytosterols for application in biology Centre of the Region Haná for Biotechnological and Agricultural Research Modulation of cell division of normal and cancer cells by cyclin-dependent kinase inhibitors Nanoliposomes for development of recombinant vaccines and targetted immunotherapeutics
http://linked.open...UplatneniVysledku	2011
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	Mechanismy regulace růstu a vývoje rostlin na úrovni buněk, orgánů a celých organismů: fyziologické, genetické a molekulárně biologické základy Teoretické základy potravinářských a biochemických technologií
issn	0039-128X
number of pages	16 (xsd:int)
http://bibframe.org/vocab/doi	10.1016/j.steroids.2011.04.014

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