Comparison of the Solubility and Dissolution of Drugs in FastedState Biorelevant Media (FaSSIF and FaSSIF-V2)

Leigh, Mathew; Kloefer, Bastian; Schaich, Michael

doi:10.14227/dt200313p44

Cited by 20 publications

(10 citation statements)

References 8 publications

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“…Biorelevant media such as FaSSIF (Fasted Stated Simulated Intestinal Fluid) are commonly used to more accurately mimic in vivo conditions, resulting in better predictions overall [9]. These media have frequently been used to mimic human intestinal fluids for greater biorelevance in solubility and dissolution experiments [3,10,11].…”

Section: Solubility and Dissolutionmentioning

confidence: 99%

An interlaboratory investigation of intrinsic dissolution rate determination using surface dissolution

Etherson

Dunn

Pamelund

et al. 2020

European Journal of Pharmaceutics and Biopharmaceutics

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The purpose of this study was to conduct an interlaboratory ring-study, with six partners (academic and industrial), investigating the measurement of intrinsic dissolution rate (IDR) using surface dissolution imaging (SDI) equipment. Measurement of IDR is important in pharmaceutical research as it provides characterising information on drugs and their formulations. This work allowed us to assess the SDI's interlaboratory performance for measuring IDR using a defined standard operating procedure (see supporting information) and six drugs assigned as low (tadalafil, bromocriptine mesylate), medium (carvedilol, indomethacin) and high (ibuprofen, valsartan) solubility compounds. Fasted State Simulated Intestinal Fluid (FaSSIF) and blank FaSSIF (without sodium taurocholate and lecithin) (pH 6.5) were used as media. Using the standardised protocol an IDR value was obtained for all compounds and the results show that the overall IDR rank order matched the solubility rank order. Interlaboratory variability was also examined and it was observed that the variability for lower solubility compounds was higher, coefficient of variation > 50%, than for intermediate and high solubility compounds, with the exception of indomethacin in FaSSIF medium. Inter laboratory variability is a useful descriptor for understanding the robustness of the protocol and the system variability. On comparison to another published small-scale IDR study the rank ordering with respect to dissolution rate is identical except for the high solubility compounds. This results indicates that the SDI robustly measures IDR however, no recommendation on the use of one small scale method over the other is made.

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Section: Solubility and Dissolutionmentioning

confidence: 99%

An interlaboratory investigation of intrinsic dissolution rate determination using surface dissolution

Etherson

Dunn

Pamelund

et al. 2020

European Journal of Pharmaceutics and Biopharmaceutics

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“…These demonstrated a benefit over conventional dissolution media regarding the solubility and dissolution of poorly soluble APIs. However, the impact on absorption of dissolved API has not been considered [5] or in other words: as absorption is not part of the experimental model, the fraction absorbed in vivo can only be correlated with the fraction dissolved in an aqueous phase; the important partitioning step into a second lipophilic phase is missing.…”

Section: Introductionmentioning

confidence: 99%

Evolution of a mini-scale biphasic dissolution model: Impact of model parameters on partitioning of dissolved API and modelling of in vivo-relevant kinetics

Locher

Borghardt

Frank

et al. 2016

European Journal of Pharmaceutics and Biopharmaceutics

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“…A precursor of biorelevant media was investigated by Macheras, Koupparis, and Tsaprounis in 1986 (82) (88). The difference between FeSSIF and FeSSIF-V2 is that the second-generation medium includes two digestion components: glyceryl monooleate and sodium oleate.…”

Section: Biorelevant Mediamentioning

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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Comparison of the Solubility and Dissolution of Drugs in FastedState Biorelevant Media (FaSSIF and FaSSIF-V2)

Cited by 20 publications

References 8 publications

An interlaboratory investigation of intrinsic dissolution rate determination using surface dissolution

An interlaboratory investigation of intrinsic dissolution rate determination using surface dissolution

Evolution of a mini-scale biphasic dissolution model: Impact of model parameters on partitioning of dissolved API and modelling of in vivo-relevant kinetics

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

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