Simulation of fasting gastric conditions and its importance for the in vivo dissolution of lipophilic compounds

Vertzoni, Maria; Dressman, Jennifer B.; Butler, James; Hempenstall, John

doi:10.1016/j.ejpb.2005.03.002

Cited by 335 publications

(215 citation statements)

References 26 publications

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“…To evaluate gastric stability, a fluid simulating conditions in the stomach in the fasted state (FaSSGF) was used by preparing a solution of NaCl (30 mM), pepsin (0.1 mg/ml), sodium taurocholate (80 mM) and lecithin (20 mM), at pH 1.6 by addition of HCl (Vertzoni et al, 2005).…”

Section: Drug Release Studiesmentioning

confidence: 99%

Galactosylated polymeric carriers for liver targeting of sorafenib

Craparo

Sardo

Serio

et al. 2014

International Journal of Pharmaceutics

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Section: Drug Release Studiesmentioning

confidence: 99%

Galactosylated polymeric carriers for liver targeting of sorafenib

Craparo

Sardo

Serio

et al. 2014

International Journal of Pharmaceutics

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“…Polyoxyethyleneglycol dodecyl ether, commercially known as Brij 35, was used in some studies as surfactant for dissolution testing (95). The hydrophobic segment of this surfactant is of similar size and structure as the one of polysorbate, but Brij 35 has an unbranched hydrophilic PEO chain and has a single long-chain fatty acid.…”

Section: Surfactantsmentioning

confidence: 99%

Evolution of Choice of Solubility and Dissolution Media After Two Decades of Biopharmaceutical Classification System

Bou‐Chacra

Melo

Morales

et al. 2017

AAPS J

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Abstract.The introduction of the biopharmaceutics drug classification system (Biopharmaceutics Classification System (BCS)), in 1995, provided a simple way to describe the biopharmaceutics behavior of a drug. Solubility and permeability are among the major parameters, which determine the fraction dose absorbed of a drug substance and consequently its chances to be bioavailable. The purpose of this review is to summarize the evolution of the media used for determining solubility and dissolution and how this can be used in modern drug development. Over the years, physiologically adapted media and buffers were introduced with the intention to better predict the in vivo solubility and dissolution of drug substances. Water, buffer solutions, compendial media, micellar solubilization media, and biorelevant media are reviewed. At this time point, there is no universal medium available which can be used to predict every drug substance's solubility or a drug product's in vivo dissolution behavior. However, there have been many improvements and additions made to media to optimize their in vivo predictability; for example, the current phosphate concentrations in buffers seem to be too high to correlate with the carbonate buffer concentrations in vivo. Biorelevant media were updated to correlate them better with the composition of human intestinal fluids. The BCS was introduced into regulatory sciences as a scientific risk management tool to waive bioequivalence studies under certain conditions. Today's different guidance documents define the dose-solubility ratio differently. As shown for amoxicillin, this can cause more confusion than certainty for globally operating companies. Harmonization of BCS guidelines is highly desirable.

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“…The volume was set as the smallest amount which enables the performance of the dissolution testing in USP II [2]. To simulate the fasted state, the volume of media in the range of 250-300 ml (stomach) or 300-500 ml (duodenum) is recommended [8], but the volume reduction was not feasible. Despite the volume reduction, sink conditions were maintained in medium PPT20 regarding on our solubility data of CC.…”

Section: Dissolution Studiesmentioning

confidence: 99%