Evaluation of amorphous solid dispersion properties using thermal analysis techniques.

doi:10.1016/J.ADDR.2011.07.009

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Evaluation of amorphous solid dispersion properties using thermal analysis techniques.

Journal Article•DOI•

Evaluation of amorphous solid dispersion properties using thermal analysis techniques.

Jared A. Baird¹, Lynne S. Taylor¹•Institutions (1)

Purdue University¹

01 Apr 2012-Advanced Drug Delivery Reviews (Adv Drug Deliv Rev)-Vol. 64, Iss: 5, pp 396-421

TL;DR: Although differential scanning calorimetry is the most widely used thermal analytical technique applied to the characterization of amorphous solid dispersions, there are many established and emerging techniques which have been shown to provide useful information.

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About: This article is published in Advanced Drug Delivery Reviews.The article was published on 2012-04-01. It has received 399 citations till now. The article focuses on the topics: Analytical technique & Amorphous solid.

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Journal Article•DOI•

Strategies to Address Low Drug Solubility in Discovery and Development

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Hywel David Williams¹, Natalie L. Trevaskis, Susan A. Charman, Ravi Mysore Shanker², William N. Charman, Colin W. Pouton, Christopher J.H. Porter - Show less +3 more•Institutions (2)

Monash University¹, Pfizer²

01 Jan 2013-Pharmacological Reviews

TL;DR: The article provides an integrated and contemporary discussion of current approaches to solubility and dissolution enhancement but has been deliberately structured as a series of stand-alone sections to allow also directed access to a specific technology where required.

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Abstract: Drugs with low water solubility are predisposed to low and variable oral bioavailability and, therefore, to variability in clinical response. Despite significant efforts to "design in" acceptable developability properties (including aqueous solubility) during lead optimization, approximately 40% of currently marketed compounds and most current drug development candidates remain poorly water-soluble. The fact that so many drug candidates of this type are advanced into development and clinical assessment is testament to an increasingly sophisticated understanding of the approaches that can be taken to promote apparent solubility in the gastrointestinal tract and to support drug exposure after oral administration. Here we provide a detailed commentary on the major challenges to the progression of a poorly water-soluble lead or development candidate and review the approaches and strategies that can be taken to facilitate compound progression. In particular, we address the fundamental principles that underpin the use of strategies, including pH adjustment and salt-form selection, polymorphs, cocrystals, cosolvents, surfactants, cyclodextrins, particle size reduction, amorphous solid dispersions, and lipid-based formulations. In each case, the theoretical basis for utility is described along with a detailed review of recent advances in the field. The article provides an integrated and contemporary discussion of current approaches to solubility and dissolution enhancement but has been deliberately structured as a series of stand-alone sections to allow also directed access to a specific technology (e.g., solid dispersions, lipid-based formulations, or salt forms) where required.

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1,201 citations

Cites background or methods from "Evaluation of amorphous solid dispe..."

...However, drugpolymer miscibility at elevated temperatures (i.e., temperatures around the Tg) is not necessarily predictive of miscibility at lower (storage) temperatures (Qi and Craig, 2010; Qian et al., 2010a,b; Baird and Taylor, 2012)....
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...In contrast, predicted Tg values that are consistent with experimental values are usually indicative of good mixing, although this is not always the case (Marsac et al., 2009; Baird and Taylor, 2012)....
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...Tg may be determined experimentally using DSC or other calorimetric methods (Royall et al., 1998; Weuts et al., 2003; Baird and Taylor, 2012)....
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...Others have also suggested that increases in configurational entropy may be used to provide an indication of increased stability of amorphous materials (Zhou et al., 2008; Graeser et al., 2009; Baird and Taylor, 2012)....
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...Further details of the techniques that can be used to detect phaseseparated drug within solid dispersions are provided in two recent reviews (Qi and Craig, 2010; Baird and Taylor, 2012)....
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Journal Article•DOI•

Polymeric Amorphous Solid Dispersions: A Review of Amorphization, Crystallization, Stabilization, Solid-State Characterization, and Aqueous Solubilization of Biopharmaceutical Classification System Class II Drugs

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Shrawan Baghel¹, Helen Cathcart¹, Niall J. O’Reilly¹•Institutions (1)

Waterford Institute of Technology¹

01 Sep 2016-Journal of Pharmaceutical Sciences

TL;DR: This review attempts to address the critical molecular and thermodynamic aspects governing the physicochemical properties of amorphous solid dispersion systems and potential advantage of polymers as inert, hydrophilic, pharmaceutical carrier matrices.

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680 citations

Journal Article•DOI•

Current trends and future perspectives of solid dispersions containing poorly water-soluble drugs.

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Chau Le-Ngoc Vo¹, Chulhun Park¹, Beom-Jin Lee¹•Institutions (1)

Ajou University¹

01 Nov 2013-European Journal of Pharmaceutics and Biopharmaceutics

TL;DR: Critical aspects and recent advances in formulation, preparation and characterization of solid dispersions as well as in-depth pharmaceutical solutions to overcome some problems and issues that limit the development and marketability of solid dispersion products are reviewed.

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510 citations

Journal Article•DOI•

Recent advances in co-amorphous drug formulations

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Swapnil J. Dengale¹, Holger Grohganz², Thomas Rades², Korbinian Löbmann²•Institutions (2)

Manipal University¹, University of Copenhagen²

01 May 2016-Advanced Drug Delivery Reviews

TL;DR: This study investigates co-amorphous formulations from the viewpoint of solid dispersions, describes their formation and mechanism of stabilization, study their impact on dissolution and in vivo performance and briefly outline the future potentials.

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327 citations

Journal Article•DOI•

Pharmaceutical solvates, hydrates and amorphous forms: A special emphasis on cocrystals

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Anne Marie Healy¹, Zelalem Ayenew Worku¹, Dinesh Kumar¹, Atif Madi¹•Institutions (1)

Trinity College, Dublin¹

01 Aug 2017-Advanced Drug Delivery Reviews

TL;DR: The fundamental characteristics and trends observed for pharmaceutical hydrates, solvates and amorphous forms are presented, with special emphasis, on pharmaceutical Hydrates with single and two‐component (i.e. cocrystal) host molecules.

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228 citations

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References

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Journal Article•DOI•

Experimental and computational approaches to estimate solubility and permeability in drug discovery and development settings

[...]

Christopher A. Lipinski¹, Franco Lombardo¹, Beryl W. Dominy¹, Paul J. Feeney¹•Institutions (1)

Pfizer¹

15 Jan 1997-Advanced Drug Delivery Reviews

TL;DR: Experimental and computational approaches to estimate solubility and permeability in discovery and development settings are described in this article, where the rule of 5 is used to predict poor absorption or permeability when there are more than 5 H-bond donors, 10 Hbond acceptors, and the calculated Log P (CLogP) is greater than 5 (or MlogP > 415).

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14,026 citations

Journal Article•DOI•

The Temperature Dependence of Relaxation Mechanisms in Amorphous Polymers and Other Glass-Forming Liquids

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Malcolm L. Williams, Robert F. Landel, John D. Ferry

01 Jul 1955-Journal of the American Chemical Society

6,510 citations

Journal Article•DOI•

On the Temperature Dependence of Cooperative Relaxation Properties in Glass‐Forming Liquids

[...]

Gerold Adam, Julian H. Gibbs

01 Jul 1965-Journal of Chemical Physics

TL;DR: In this paper, a molecularkinetic theory was proposed to explain the temperature dependence of relaxation behavior in glass-forming liquids in terms of the temperature variation of the size of the cooperatively rearranging region.

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Abstract: A molecular‐kinetic theory, which explains the temperature dependence of relaxation behavior in glass‐forming liquids in terms of the temperature variation of the size of the cooperatively rearranging region, is presented. The size of this cooperatively rearranging region is shown to be determined by configuration restrictions in these glass‐forming liquids and is expressed in terms of their configurational entropy. The result of the theory is a relation practically coinciding with the empirical WLF equation. Application of the theory to viscosimetric experiments permits evaluation of the ratio of the kinetic glass temperature Tg (derived from usual ``quasistatic'' experiments) to the equilibrium second‐order transition temperature T2 (indicated by either statistical‐mechanical theory or extrapolations of experimental data) as well as the hindrance‐free energy per molecule. These parameters have been evaluated for fifteen substances, the experimental data for which were available. Hindrance‐free energies ...

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5,037 citations

"Evaluation of amorphous solid dispe..." refers background in this paper

...The most common models to describe structural relaxation are the Adam–Gibbs–Vogel [97] (AGV), Vogel– Tammann–Fulcher [98] (VTF), Adam–Gibbs [99] (AG), and Williams Landell Ferry [100] (WLF) equations....
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Journal Article•DOI•

Non-symmetrical dielectric relaxation behaviour arising from a simple empirical decay function

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Graham Williams, David C. Watts

01 Jan 1970-Transactions of The Faraday Society

TL;DR: In this article, the empirical dielectric decay function γ(t)= exp −(t/τ 0)β was transformed analytically to give the frequency dependent complex dielectrics constant if β is chosen to be 0.50 in the range log(ωτ0) > −0.5.

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Abstract: The empirical dielectric decay function γ(t)= exp –(t/τ0)β may be transformed analytically to give the frequency dependent complex dielectric constant if β is chosen to be 0.50. The resulting dielectric constant and dielectric loss curves are non-symmetrical about the logarithm of the frequency of maximum loss, and are intermediate between the Cole-Cole and Davidson-Cole empirical relations. Using a short extrapolation procedure, good agreement is obtained between the empirical representation and the experimental curves for the α relaxation in polyethyl acrylate. It is suggested that the present representation would have a general application to the α relaxations in other polymers. The Hamon approximation, with a small applied correction, is valid for the present function with β= 0.50 in the range log(ωτ0) > –0.5, but cannot be used at lower frequencies.

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3,675 citations

"Evaluation of amorphous solid dispe..." refers methods in this paper

...can be modeled using the Kohlrausch–Williams–Watts [113] (KWW) or stretched exponential equation:...
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...These non-exponential relaxation phenomena can be modeled using the Kohlrausch–Williams–Watts [113] (KWW) or stretched exponential equation: φ tð Þ = exp − t τKWW β ð6Þ where φ(t) is the extent of relaxation at time t, τKWW is the average relaxation time constant, and β is a parameter varying between 0 and 1 that accounts for the degree of non-exponentiality in the relaxation dynamics....
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Journal Article•DOI•

Improving drug solubility for oral delivery using solid dispersions.

[...]

Christian Leuner¹, Jennifer B. Dressman¹•Institutions (1)

Goethe University Frankfurt¹

03 Jul 2000-European Journal of Pharmaceutics and Biopharmaceutics

TL;DR: The historical background and definitions of the various systems including eutectic mixtures, solid dispersions and solid solutions, as well as the production, the different carriers and the methods used for the characterization of solid dispersion are outlined.

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2,695 citations

"Evaluation of amorphous solid dispe..." refers background in this paper

...In amorphous one phase blends (sometimes termed amorphous solid solutions) the drug-carrier interactions are significant, resulting in completemiscibility of the two components, forming a onephase systemwhich is homogeneous at themolecular level [10,11]....
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