2010
DOI: 10.1007/s11095-010-0111-0
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Multivariate Data Analysis of Factors Affecting the In Vitro Dissolution Rate and the Apparent Solubility for a Model Basic Drug Substance in Aqueous Media

Abstract: The miniaturized rotating disk equipment was suitable to use, in conjunction with the chemometric analyses, in the evaluation of the factors affecting the in vitro dissolution rate. The apparent solubility was found to be influenced by the same factors as G.

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Cited by 4 publications
(4 citation statements)
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“…IOAC models also possess significant advantages over Ussing chamber models based on animal tissue that are both labor and resource intensive . It is also noteworthy that direct kinetic comparisons of transport variables such as permeability coefficients under complex human intestinal in vivo environments are rare. , Technique mimicking intestinal perfusions, such as IOAC microfluidic models, have the potential to enable direct in vitro investigation of single parameters such as intestinal permeability, absorption, biliary secretion and efflux; without the complex influences of metabolism, pH changes, dissolution and intestinal mobility that are experienced in vivo. It is well-established that the physicochemical properties of drugs such as molecular weight, log P , log D , polar surface area, and hydrogen bonding, are directly related to their overall intestinal absorption potential. , Suggesting microfluidic IOAC models have a significant role to play in the future to study the intestinal permeability of newly developed drugs and biomolecules other than those in the existing well-characterized chemical space, such as lipophilic conjugated prodrugs, as well as to better define the relationship between physiochemical properties and intestinal permeability. , …”
Section: Resultsmentioning
confidence: 99%
See 1 more Smart Citation
“…IOAC models also possess significant advantages over Ussing chamber models based on animal tissue that are both labor and resource intensive . It is also noteworthy that direct kinetic comparisons of transport variables such as permeability coefficients under complex human intestinal in vivo environments are rare. , Technique mimicking intestinal perfusions, such as IOAC microfluidic models, have the potential to enable direct in vitro investigation of single parameters such as intestinal permeability, absorption, biliary secretion and efflux; without the complex influences of metabolism, pH changes, dissolution and intestinal mobility that are experienced in vivo. It is well-established that the physicochemical properties of drugs such as molecular weight, log P , log D , polar surface area, and hydrogen bonding, are directly related to their overall intestinal absorption potential. , Suggesting microfluidic IOAC models have a significant role to play in the future to study the intestinal permeability of newly developed drugs and biomolecules other than those in the existing well-characterized chemical space, such as lipophilic conjugated prodrugs, as well as to better define the relationship between physiochemical properties and intestinal permeability. , …”
Section: Resultsmentioning
confidence: 99%
“…54,55 Suggesting microfluidic IOAC models have a significant role to play in the future to study the intestinal permeability of newly developed drugs and biomolecules other than those in the existing well-characterized chemical space, such as lipophilic conjugated prodrugs, as well as to better define the relationship between physiochemical properties and intestinal permeability. 56,57 Permeability Coefficient of Lipophilic SN38 Prodrugs. Toward the development of oral SN38-based chemotherapy with efficient oral absorption, we have recently developed novel lipophilic SN38 prodrugs.…”
Section: Acs Biomaterials Science and Engineeringmentioning
confidence: 99%
“…Solubility evaluation is very important for the pharmaceutical product design, because the drug solubility affects the drug efficacy directly, as well as its future developments and formulation optimizations, influencing the pharmacokinetic properties, such as release, transport, and absorption. …”
Section: Introductionmentioning
confidence: 99%
“…are used for the evaluation of the data) and statistical methods (like ANOVA and multivariate statistics) (Costa and Sousa Lobo, 2001;Ruiz and Volonte, 2014;Yuksel, 2000). Multivariate approaches have been used to assess the impact of formulation composition and manufacturing method on dissolution (Andersson et al, 2007;Huang et al, 2009;Kaul et al, 2011;Maggio et al, 2009;Nagarwal et al, 2009;Ring et al, 2011), to compare dissolution profiles of various pharmaceutical dosage forms (Adams et al, 2002(Adams et al, , 2001Enăchescu, 2010;Huang et al, 2011;Maggio et al, 2008), to quantify the drug release during dissolution (Hernandez et al, 2016), to develop in vitro dissolution methods for pure substance or several formulation types (Eaton et al, 2007;Fish et al, 2009;Graffner et al, 1996;Persson et al, 2010;Petruševska et al, 2015), and to define the in vivo predictive in vitro dissolution set-up based on the modification of the polarity of the dissolution medium with the use of ethanol (Abuzarur-Aloul et al, 1998a, 1998b. In vitro dissolution profiles can be used to predict the in vivo behaviour of a formulation by developing an in vitro-in vivo correlation (IVIVC).…”
Section: Introductionmentioning
confidence: 99%