Dissolution Media Simulating Conditions in the Proximal Human Gastrointestinal Tract: An Update

Jantratid, Ekarat; Janssen, Niels; Reppas, Christos; Dressman, Jennifer B.

doi:10.1007/s11095-008-9569-4

Cited by 664 publications

(524 citation statements)

References 77 publications

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“…Preparation of FaB, FeB, FaSSIF, FeSSIF was done according to the procedure described by Jantratid and coworkers (Jantratid et al, 2008). Table 1 provides the composition of the different media and Table 2 gives an overview of the physicochemical and biopharmaceutical properties of employed model drugs and the marker calcein.…”

Section: Permeation Studies Using the Pvpabiomimetic Modelmentioning

confidence: 99%

“…The bile salt sodium taurocholate, present in both FaSSIF and FeSSIF in different concentrations, is known to interact with the membrane lipids at low concentrations (Jantratid et al, 2008;Schubert et al, 1986). PB pH 6.2, FaB and FeB, which do not contain the bile salt, were therefore included to compare the barrier integrity and further evaluate any possible interaction of FaSSIF and FeSSIF with the PVPAbiomimetic barrier.…”

Section: Barrier Integrity In the Presence Of Fassif And Fessifmentioning

confidence: 99%

“…The bile salt, sodium taurocholate, is present in FaSSIF and FeSSIF in concentrations of 3 mM and 10 mM, respectively (Jantratid et al, 2008). The interaction between sodium taurocholate and unilamellar vesicles has earlier been studied and according to Schubert and co-workers low bile salt concentration appears to bind to the vesicles and interact with several membrane lipids, and particularly with lecithin (Schubert et al, 1986;Schubert and Schmidt, 1988 (Fischer et al, 2012).…”

Section: Loss Of Sodium Taurocholate From the Donormentioning

confidence: 99%

“…The bile salt concentration and the amount of lecithin, primarily phosphatidylcholine, are known to be important factors in the intestinal fluid affecting the drugs' solubility as well as permeability (Dahan and Miller, 2012;Jantratid et al, 2008). The intestinal solubility remains as one of the most important parameters in order to achieve the desired systemic drug concentration.…”

Section: Influence Of Fassif and Fessif On Permeability Of Drugsmentioning

confidence: 99%

“…It is known that drugs from different classes might be affected differently in the presence of biorelevant fluids and also the presence of certain components in the GI fluid such as lecithin and bile salt (sodium taurocholate) might have a large impact on the solubility and permeability of poorly soluble compounds (Bergstrom et al, 2014;Dahan and Miller, 2012). Among the biorelevant media, FaSSIF and FeSSIF, first introduced in 1998 by Dressman and co-workers and later modified to better predict in vivo behavior of drugs, are the most utilized fluids originally applied as dissolution medium and later employed as medium in the permeability screening (Galia et al, 1998;Jantratid et al, 2008). FaSSIF has previously been shown to be compatible with the original PVPAo-barriers consisting of egg phospholipids (Fischer et al, 2012) However, the more challenging FeSSIF has never been tested in any of the PVPA models.…”

Section: Introductionmentioning

confidence: 99%

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Biomimetic PVPA in vitro model for estimation of the intestinal drug permeability using fasted and fed state simulated intestinal fluids

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2015

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Section: Permeation Studies Using the Pvpabiomimetic Modelmentioning

confidence: 99%

Section: Barrier Integrity In the Presence Of Fassif And Fessifmentioning

confidence: 99%

Section: Loss Of Sodium Taurocholate From the Donormentioning

confidence: 99%

Section: Influence Of Fassif and Fessif On Permeability Of Drugsmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

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Biomimetic PVPA in vitro model for estimation of the intestinal drug permeability using fasted and fed state simulated intestinal fluids

Naderkhani

Vasskog

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2015

European Journal of Pharmaceutical Sciences

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Physicochemical Characterization and Oral Dosage Form Design and Selection

Dening

Amidon

et al. 2021

Burger's Medicinal Chemistry and Drug Discovery

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In order to initiate formulation development activities – that is the identification of a “marketable” product – important physical and chemical properties (physicochemical properties) as well as permeability properties need to be determined. Evaluation of these properties early in the discovery process can help discovery teams select which templates to pursue as well as identify the most promising leads. This information is also valuable “downstream” as decisions regarding dosage form design are being made. The focus of this article will be on the physicochemical properties that are most important in the evaluation of discovery leads and that provide the information needed as dosage form development is initiated and progresses. It will become apparent that the most appropriate dosage forms that make sense to consider are dictated by both the physicochemical and biopharmaceutical properties of the drug molecule. Throughout this article, there will be an emphasis on the tools and principles that will help the medicinal chemist during the drug discovery process, with particular emphasis on oral dosage forms.

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Solubility and Dissolution Considerations for Amorphous Solid Dispersions

Ilevbare¹,

Xu²,

John³

et al. 2015

Pharmaceutical Sciences Encyclopedia

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This chapter presents differences between dispersions, amorphous materials, and crystalline forms, and discusses the impact of excipient selection, especially polymers. It provides guidance for solubility and dissolution testing of amorphous dispersions. Crystalline solids are mostly used in pharmaceutical drug formulations because of their physical and chemical stabilities. Amorphous solids are commonly described as condensed phases that lack the long‐range translational order typical of a crystalline solid, although the molecules may have short‐range order. The success of amorphous solids as a supersaturating dosage form depends on the choice of processing conditions to yield a pure amorphous solid with no or minimal crystallization of the amorphous drug during storage and upon dosing. The use of amorphous solid dispersions has become a well‐known strategy for inhibiting crystallization, as the amorphous solid dispersions can have increased physical stability over neat amorphous material.

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Dissolution Media Simulating Conditions in the Proximal Human Gastrointestinal Tract: An Update

Abstract: The updated dissolution media can be used to predict formulation performance and food effects in vivo. These media are more physiologically relevant and show better physical stability than their corresponding predecessors.

Cited by 664 publications

References 77 publications

Biomimetic PVPA in vitro model for estimation of the intestinal drug permeability using fasted and fed state simulated intestinal fluids

Biomimetic PVPA in vitro model for estimation of the intestinal drug permeability using fasted and fed state simulated intestinal fluids

Physicochemical Characterization and Oral Dosage Form Design and Selection

Solubility and Dissolution Considerations for Amorphous Solid Dispersions

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