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000281842 1001_ $$0P:(DE-HGF)0$$aKhoshakhlagh, Pooneh$$b0
000281842 245__ $$aFasted-State Simulated Intestinal Fluid 'FaSSIF-C', a Cholesterol Containing Intestinal Model Medium for In Vitro Drug Delivery Development
000281842 260__ $$aNew York, NY$$bWiley$$c2015
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000281842 520__ $$aA set of biorelevant media "fasted-state simulated intestinal fluid with cholesterol (FaSSIF-C)" for the in vitro study of intestinal drug dissolution in the duodenum was developed. These contain cholesterol at the same levels as in human bile: the cholesterol content of FaSSIF-7C is equivalent to healthy female, FaSSIF-10C to healthy male persons, and FaSSIF-13C to several disease cases that lead to gallstones. The fluids were studied in three aspects: biocompatibility, intestinal nanostructure, and solubilizing power of hydrophobic drugs of the BCS class II. The biocompatibility study showed no toxic effects in a Caco-2 cell system. The drug-solubilizing capacity toward Fenofibrate, Danazol, Griseofulvin, and Carbamazepine was assessed as example. It varied with the cholesterol content widely from a fourfold improvement to a twofold reduction. The nanostructure study by dynamic light scattering and small-angle neutron scattering indicated vesicles as the main component of FaSSIF-C in equilibrium (> 1 h), but at high cholesterol content, larger particles were observed as a minor contribution. The neutron experiments indicated the presence of complex micelle-vesicle mixtures, even after 1 h development of fed-state bile model to FaSSIF. The results indicate that cholesterol affects some drugs in solubilization and particle size in intestinal model fluids.
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000281842 7001_ $$0P:(DE-HGF)0$$aJohnson, Raphael$$b1
000281842 7001_ $$0P:(DE-HGF)0$$aLangguth, Peter$$b2
000281842 7001_ $$0P:(DE-HGF)0$$aNawroth, Thomas$$b3$$eCorresponding author
000281842 7001_ $$0P:(DE-HGF)0$$aSchmueser, Lars$$b4
000281842 7001_ $$0P:(DE-HGF)0$$aHellmann, Nadja$$b5
000281842 7001_ $$0P:(DE-HGF)0$$aDecker, Heinz$$b6
000281842 7001_ $$0P:(DE-Juel1)145431$$aSzekely, Noemi$$b7
000281842 773__ $$0PERI:(DE-600)1491821-3$$a10.1002/jps.24470$$gVol. 104, no. 7, p. 2213 - 2224$$n7$$p2213 - 2224$$tJournal of pharmaceutical sciences$$v104$$x0022-3549$$y2015
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