Rapid determination of drug solubilization versus supersaturation in natural and digested lipids
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Autor:innen
Autor:in (Körperschaft)
Publikationsdatum
2016
Typ der Arbeit
Studiengang
Sammlung
Typ
01A - Beitrag in wissenschaftlicher Zeitschrift
Herausgeber:innen
Herausgeber:in (Körperschaft)
Betreuer:in
Übergeordnetes Werk
International Journal of Pharmaceutics
Themenheft
DOI der Originalpublikation
Link
Reihe / Serie
Reihennummer
Jahrgang / Band
513
Ausgabe / Nummer
1-2
Seiten / Dauer
164-174
Patentnummer
Verlag / Herausgebende Institution
Elsevier
Verlagsort / Veranstaltungsort
Auflage
Version
Programmiersprache
Abtretungsempfänger:in
Praxispartner:in/Auftraggeber:in
Zusammenfassung
Lipid-based formulations (LBFs) represent one of the successful formulation approaches that enable oral delivery of poorly water-sol. drugs. This work presents a simple equil. approach based on soly. in lipids and their corresponding digestion media to est. a max. drug supersatn. ratio (SRmax). This value of drug concn. normalized by the soly. in the aq. digestion phase indicates the propensity for drug pptn. A set of 16 structurally diverse drugs was first measured for their soly. in tricaprin and tricaprylin and results were compared to an empirical model based on mol. predictors. In the next step, digestion media were either prepd. by in vitro lipolysis or by assembling a compn. to mimic the endpoint of digestion. It was found that drug soly. in the pure lipids mainly was related to the m.p. in that increased values resulted in reduced soly. The soly. values measured in the lipolysis media correlated well with those obtained from assembled digestion media. Interestingly, the solubilization upon digestion was typically higher when using tricaprin than tricaprylin in spite of that the latter oil (as pure excipient) generally was a more potent solvent. This work suggests that a simplified digestion screen can be used to facilitate evaluation of formulations during early development. Estn. of SRmax provides an early risk assessment of drug pptn. for LBFs. The method is easily scaled down to the microtiter plate format and can be used for selecting candidate formulations that merit further evaluation in more complex and dynamic in vitro tests.
Schlagwörter
Biological digestion, Drug delivery systems, Risk assessment
Fachgebiet (DDC)
Veranstaltung
Startdatum der Ausstellung
Enddatum der Ausstellung
Startdatum der Konferenz
Enddatum der Konferenz
Datum der letzten Prüfung
ISBN
ISSN
0378-5173
1873-3476
1873-3476
Sprache
Englisch
Während FHNW Zugehörigkeit erstellt
Ja
Publikationsstatus
Veröffentlicht
Begutachtung
Peer-Review der ganzen Publikation
Open Access-Status
Lizenz
Zitation
GAUTSCHI, Nicolas, Christel BERGSTROEM und Martin KUENTZ, 2016. Rapid determination of drug solubilization versus supersaturation in natural and digested lipids. International Journal of Pharmaceutics. 2016. Bd. 513, Nr. 1-2, S. 164–174. DOI 10.1016/j.ijpharm.2016.09.015. Verfügbar unter: http://hdl.handle.net/11654/23689