A Promising New Method to Estimate Drug-Polymer Solubility at Room Temperature

被引:29
|
作者
Knopp, Matthias Manne [1 ,2 ]
Gannon, Natasha [2 ]
Porsch, Ilona [2 ]
Rask, Malte Bille [1 ,3 ]
Olesen, Niels Erik [1 ]
Langguth, Peter [2 ]
Holm, Rene [1 ,3 ]
Rades, Thomas [3 ]
机构
[1] H Lundbeck & Co AS, Pharmaceut Sci & CMC Biol, DK-2500 Valby, Denmark
[2] Johannes Gutenberg Univ Mainz, Inst Pharm & Biochem, D-55128 Mainz, Germany
[3] Univ Copenhagen, Dept Pharm, DK-2100 Copenhagen, Denmark
关键词
solubility; polymers; poorly soluble drugs; Flory-Huggins; shake-flask method; amorphous solid dispersion; solubility enhancement; thermal analysis; CRYSTALLINE DRUGS; MISCIBILITY; PREDICTION; MATRICES; PVP/VA;
D O I
10.1016/j.xphs.2016.02.017
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
The established methods to predict drug-polymer solubility at room temperature either rely on extrapolation over a long temperature range or are limited by the availability of a liquid analogue of the polymer. To overcome these issues, this work investigated a new methodology where the drug-polymer solubility is estimated from the solubility of the drug in a solution of the polymer at room temperature using the shake-flask method. Thus, the new polymer in solution method does not rely on temperature extrapolations and only requires the polymer and a solvent, in which the polymer is soluble, that does not affect the molecular structure of the drug and polymer relative to that in the solid state. Consequently, as this method has the potential to provide fast and precise estimates of drug-polymer solubility at room temperature, we encourage the scientific community to further investigate this principle both fundamentally and practically. (c) 2016 American Pharmacists Association((R)). Published by Elsevier Inc. All rights reserved.
引用
收藏
页码:2621 / 2624
页数:4
相关论文
共 50 条
  • [31] Simultaneous XRD-DSC identifies correct drug-polymer solubility and miscibility for enantiotropic solid forms
    Bookwala, Mustafa
    Shi, Jiawanjun
    Buckner, Ira S.
    Bates, Simon
    Wildfong, Peter L. D.
    JOURNAL OF PHARMACEUTICAL SCIENCES, 2025, 114 (01) : 416 - 423
  • [32] Estimation of Drug-Polymer Miscibility and Solubility in Amorphous Solid Dispersions Using Experimentally Determined Interaction Parameters
    Marsac, Patrick J.
    Li, Tonglei
    Taylor, Lynne S.
    PHARMACEUTICAL RESEARCH, 2009, 26 (01) : 139 - 151
  • [33] Multivariate Analysis of Solubility Parameters for Drug-Polymer Miscibility Assessment in Preparing Raloxifene Hydrochloride Amorphous Solid Dispersions
    Moreira, Guilherme G.
    Taveira, Stephania F.
    Martins, Felipe T.
    Wagner, Karl G.
    Marreto, Ricardo N.
    AAPS PHARMSCITECH, 2024, 25 (05):
  • [34] A thermal analysis method to predict the complete phase diagram of drug-polymer solid dispersions
    Lin, Dexi
    Huang, Yanbin
    INTERNATIONAL JOURNAL OF PHARMACEUTICS, 2010, 399 (1-2) : 109 - 115
  • [35] Investigation of the Dependence of the Flory-Huggins Interaction Parameter on Temperature and Composition in a Drug-Polymer System
    Potter, Catherine B.
    Davis, Mark T.
    Albadarin, Ahmad B.
    Walker, Gavin M.
    MOLECULAR PHARMACEUTICS, 2018, 15 (11) : 5327 - 5335
  • [36] Synthesis of ceramic-polymer-drug biocomposites at room temperature
    Vallet-Regi, M
    Gordo, M
    Ragel, CV
    Cabanas, MV
    San Roman, J
    SOLID STATE IONICS, 1997, 101 : 887 - 892
  • [37] Synthesis of ceramic-polymer-drug biocomposites at room temperature
    Vallet-Regi, M.
    Gordo, M.
    Ragel, C.V.
    Cabanas, M.V.
    San Roman, J.
    Solid State Ionics, 1997, 101-103 (pt 2): : 887 - 892
  • [38] The Peculiar Behavior of the Glass Transition Temperature of Amorphous Drug-Polymer Films Coated on Inert Sugar Spheres
    Dereymaker, Aswin
    Van den Mooter, Guy
    JOURNAL OF PHARMACEUTICAL SCIENCES, 2015, 104 (05) : 1759 - 1766
  • [39] Drug-Polymer Electrostatic Complexes as New Structuring Agents for the Formation of Drug-Loaded Ordered Mesoporous Silica
    Molina, Emilie
    Warnant, Jerome
    Mathonnat, Melody
    Bathfield, Mael
    In, Martin
    Laurencin, Danielle
    Jerome, Christine
    Lacroix-Desmazes, Patrick
    Marcotte, Nathalie
    Gerardin, Corine
    LANGMUIR, 2015, 31 (47) : 12839 - 12844
  • [40] Prediction of drug-polymer miscibility through the use of solubility parameter based flory-huggins interaction parameter and the experimental validation: PEG as model polymer
    Thakral, Seema
    Thakral, Naveen K.
    JOURNAL OF PHARMACEUTICAL SCIENCES, 2013, 102 (07) : 2254 - 2263