Navigation überspringen
Universitätsbibliothek Heidelberg
Status: Bibliographieeintrag

Verfügbarkeit
Standort: ---
Exemplare: ---
heiBIB
 Online-Ressource
Verfasst von:Buckley, Stephen Timothy [VerfasserIn]   i
 Frank, Kerstin J. [VerfasserIn]   i
 Fricker, Gert [VerfasserIn]   i
 Brandl, Martin [VerfasserIn]   i
Titel:Biopharmaceutical classification of poorly soluble drugs with respect to "enabling formulations"
Verf.angabe:Stephen Timothy Buckley, Kerstin Julia Frank, Gert Fricker, Martin Brandl
E-Jahr:2013
Jahr:11 April 2013
Umfang:9 S.
Fussnoten:Gesehen am 26.11.2020
Titel Quelle:Enthalten in: European journal of pharmaceutical sciences
Ort Quelle:New York, NY [u.a.] : Elsevier, 1993
Jahr Quelle:2013
Band/Heft Quelle:50(2013), 1, Seite 8-16
ISSN Quelle:1879-0720
Abstract:The large number of drug candidates with poor dissolution characteristics seen in the past decade, has fostered interest in so-called "enabling formulations", i.e., formulations which shall make such drugs bio-available. Development of enabling formulations is currently being guided by the following (simplified) hypothesis: If a poorly soluble drug (BCS class II drug) can be transferred into a solubilized state, one can achieve an absorption profile close to that of a soluble drug (BCS class I drug). Thus, formulation development typically endeavors to achieve the most robust solubility enhancement. Here we critically review both common in vitro approaches and experimental data available in literature pertaining to the solubility and permeability of poorly soluble drugs from enabling formulations, and discuss their interplay. Recent in vitro data indicate, that commonly employed surfactants as well as endogenous surfactants present in the intestine, although enhancing drug solubility, mostly hamper drug permeation. Mechanistic studies demonstrate a direct correlation between passive transcellular diffusion and the concentration of molecularly dissolved drug. The latter may be reduced due to partitioning into micelles or other solubilizing carriers, but enhanced in supersaturating formulations. We conclude thus that biopharmaceutical assessment approaches that rely on the amount of molecularly dissolved drug should guide us towards successful enabling formulations.
DOI:doi:10.1016/j.ejps.2013.04.002
URL:Bitte beachten Sie: Dies ist ein Bibliographieeintrag. Ein Volltextzugriff für Mitglieder der Universität besteht hier nur, falls für die entsprechende Zeitschrift/den entsprechenden Sammelband ein Abonnement besteht oder es sich um einen OpenAccess-Titel handelt.

DOI: https://doi.org/10.1016/j.ejps.2013.04.002
Datenträger:Online-Ressource
Sprache:eng
Sach-SW:Absorption
 active pharmaceutical ingredient
 amorphous solid dispersion
 API
 ASD
 BCRP
 BCS
 Bile Acids and Salts
 Biological Availability
 Biopharmaceutical Classification Scheme
 Biopharmaceutics
 breast cancer resistant protein
 Chemistry, Pharmaceutical
 CMC
 critical micelle concentration
 CsA
 cyclosporin A
 Excipients
 FaSSIF
 fasted state simulated intestinal fluid
 fed state simulated intestinal fluid
 FeSSIF
 Gastrointestinal
 GI
 Hank’s buffered salt solution
 HBSS
 Micelle
 MRP
 multidrug resistance-related protein
 p-Glycoprotein
 p-GP
 Permeability
 Pharmaceutical Preparations
 Phospholipids
 self nanoemulsifying drug delivery system
 SNEDDS
 Solubility
 Solubilization
 SSDS
 supersaturating drug delivery systems
 Surface-Active Agents
 TEER
 transepithelial electrical resistance
K10plus-PPN:1741217202
Verknüpfungen:→ Zeitschrift

Permanenter Link auf diesen Titel (bookmarkfähig):  https://katalog.ub.uni-heidelberg.de/titel/68666027   QR-Code
zum Seitenanfang