Influence of the intermediate digestion phases of common formulation lipids on the absorption of a poorly water‐soluble drug

The influence of different model intestinal phases (modelled on those likely to be produced in vivo after the digestion of commonly used formulation lipids) on the absorption profile of cinnarizine has been studied. Combinations of C8, C12, or C18:1 fatty acid and monoglyceride and simulated endogen...

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Veröffentlicht in:Journal of pharmaceutical sciences 2005-03, Vol.94 (3), p.481-492
Hauptverfasser: Kossena, Greg A., Charman, William N., Boyd, Ben J., Porter, Christopher J.H.
Format: Artikel
Sprache:eng
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Zusammenfassung:The influence of different model intestinal phases (modelled on those likely to be produced in vivo after the digestion of commonly used formulation lipids) on the absorption profile of cinnarizine has been studied. Combinations of C8, C12, or C18:1 fatty acid and monoglyceride and simulated endogenous intestinal fluid were formulated to provide examples of liquid (L1), lamellar (Lα), and cubic (C) liquid crystalline phases. Phases containing cinnarizine were dosed intraduodenally and absorption was assessed in an anesthetized rat model. Bile duct ligation was performed to inhibit the effects of digestion/dilution on the phase structure. Absorption from the Lα phases (C8 and C12 lipids) was statistically higher (p 
ISSN:0022-3549
1520-6017
DOI:10.1002/jps.20260