Biorelevant dissolution of poorly soluble weak acids studied by UV imaging reveals ranges of fractal-like kinetics

Niederquell, Andreas; Kuentz, Martin

doi:10.1016/j.ijpharm.2013.12.049

Cited by 38 publications

(28 citation statements)

References 51 publications

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“…To this end, it is beneficial to combine standard USP-type dissolution tests with chemically specific, spectroscopic imaging-based analytical approaches such as attenuated total reflection-Fourier transform infrared (ATR-FTIR) spectroscopic imaging (21–24), magnetic resonance imaging (MRI) (25,26), UV imaging (27,28) and Raman imaging (29,30). These techniques allow the visualization of dynamic physico-chemical processes within a tablet under dissolution conditions, making it possible to elucidate phenomena that could not be easily identifiable from the USP release curve.…”

Section: Introductionmentioning

confidence: 99%

The Combined Use of Imaging Approaches to Assess Drug Release from Multicomponent Solid Dispersions

et al. 2016

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PurposeImaging methods were used as tools to provide an understanding of phenomena that occur during dissolution experiments, and ultimately to select the best ratio of two polymers in a matrix in terms of enhancement of the dissolution rate and prevention of crystallization during dissolution.MethodsMagnetic resonance imaging, ATR-FTIR spectroscopic imaging and Raman mapping have been used to study the release mechanism of a poorly water soluble drug, aprepitant, from multicomponent amorphous solid dispersions. Solid dispersions were prepared based on the combination of two selected polymers - Soluplus, as a solubilizer, and PVP, as a dissolution enhancer. Formulations were prepared in a ratio of Soluplus:PVP 1:10, 1:5, 1:3, and 1:1, in order to obtain favorable properties of the polymer carrier.ResultsThe crystallization of aprepitant during dissolution has occurred to a varying degree in the polymer ratios 1:10, 1:5, and 1:3, but the increasing presence of Soluplus in the formulation delayed the onset of crystallization. The Soluplus:PVP 1:1 solid dispersion proved to be the best matrix studied, combining the abilities of both polymers in a synergistic manner.ConclusionsAprepitant dissolution rate has been significantly enhanced. This study highlights the benefits of combining imaging methods in order to understand the release process.Electronic supplementary materialThe online version of this article (doi:10.1007/s11095-016-2018-x) contains supplementary material, which is available to authorized users.

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Section: Introductionmentioning

confidence: 99%

The Combined Use of Imaging Approaches to Assess Drug Release from Multicomponent Solid Dispersions

et al. 2016

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“…Decreasing intrinsic dissolution rates over time can be also observed for pure drugs due to heterogeneity effects on the samples surface (Niederquell and Kuentz, 2014). The solid dispersions in this study provide an even more complex situation because the hydration layer on the surface and the moving dissolution medium in the cell provide a dynamically evolving multiphase system.…”

Section: Uv Imaging Of Drug Dissolutionmentioning

confidence: 81%

Amorphous drug dispersions with mono- and diacyl lecithin: On molecular categorization of their feasibility and UV dissolution imaging

Gautschi

Hoogevest

Kuentz

2015

International Journal of Pharmaceutics

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“…The reviewed publications showed that different grades of water were used as media to determine the solubility of drug substance: double-distilled water (6)(7)(8); double deionized water (9), Milli-Q® purified water (10), 18.2 MΩ.cm/ 0.22 μm (11); Milli-Q®ultrapure water, conductivity less than 0.1 μS cm (12,13); ultrapure water Elix® Millipore (14); distilled water (5,15-21) deionized water (22)(23)(24)(25)(26); distilled, deionized, and filtered water (27); purified water (28)(29)(30)(31)(32)(33)(34)(35)(36); demineralized water (37). The type of water was not specified in 19 of 51 studies (37%) (38)(39)(40)(41)(42)(43)(44)(45)(46)(47)(48)(49)(50)(51)(52)(53)(54)(55)(56).…”

Section: Watermentioning

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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Biorelevant dissolution of poorly soluble weak acids studied by UV imaging reveals ranges of fractal-like kinetics

Cited by 38 publications

References 51 publications

The Combined Use of Imaging Approaches to Assess Drug Release from Multicomponent Solid Dispersions

The Combined Use of Imaging Approaches to Assess Drug Release from Multicomponent Solid Dispersions

Amorphous drug dispersions with mono- and diacyl lecithin: On molecular categorization of their feasibility and UV dissolution imaging

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

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