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
  • [1] A new method to determine drug-polymer solubility through enthalpy of melting and mixing
    Meiland, Peter
    Larsen, Bjarke Strom
    Knopp, Matthias Manne
    Tho, Ingunn
    Rades, Thomas
    INTERNATIONAL JOURNAL OF PHARMACEUTICS, 2022, 629
  • [2] Automation Potential of a New, Rapid, Microscopy-Based Method for Screening Drug-Polymer Solubility
    Alhijjaj, Muqdad
    Belton, Peter
    Fabian, Laszlo
    Reading, Mike
    Qi, Sheng
    ACS OMEGA, 2020, 5 (20): : 11402 - 11410
  • [3] A new method to determine drug-polymer solubility through enthalpy of melting and mixing (vol 629, 122391, 2022)
    Meiland, Peter
    Larsen, Bjarke Strom
    Knopp, Matthias Manne
    Tho, Ingunn
    Rades, Thomas
    INTERNATIONAL JOURNAL OF PHARMACEUTICS, 2024, 662
  • [4] Prediction of drug solubility in an acrylate adhesive based on the drug-polymer interaction parameter and drug solubility in acetonitrile
    Li, JW
    Masso, JJ
    Guertin, JA
    JOURNAL OF CONTROLLED RELEASE, 2002, 83 (02) : 211 - 221
  • [5] Theoretical and practical approaches for prediction of drug-polymer miscibility and solubility
    Marsac, Patrick J.
    Shamblin, Sheri L.
    Taylor, Lynne S.
    PHARMACEUTICAL RESEARCH, 2006, 23 (10) : 2417 - 2426
  • [6] Comparative Study of Different Methods for the Prediction of Drug-Polymer Solubility
    Knopp, Matthias Manne
    Tajber, Lidia
    Tian, Yiwei
    Olesen, Niels Erik
    Jones, David S.
    Kozyra, Agnieszka
    Lobmann, Korbinian
    Paluch, Krzysztof
    Brennan, Claire Marie
    Holm, Rene
    Healy, Anne Marie
    Andrews, Gavin P.
    Rades, Thomas
    MOLECULAR PHARMACEUTICS, 2015, 12 (09) : 3408 - 3419
  • [7] Analytical and Computational Methods for the Determination of Drug-Polymer Solubility and Miscibility
    Thakore, Samarth D.
    Akhtar, Junia
    Jain, Ranjna
    Paudel, Amrit
    Bansal, Arvind K.
    MOLECULAR PHARMACEUTICS, 2021, 18 (08) : 2835 - 2866
  • [8] Influence of PVP/VA copolymer composition on drug-polymer solubility
    Rask, Malte Bille
    Knopp, Matthias Manne
    Olesen, Niels Erik
    Holm, Rene
    Rades, Thomas
    EUROPEAN JOURNAL OF PHARMACEUTICAL SCIENCES, 2016, 85 : 10 - 17
  • [9] Drug-Polymer Solubility Determination: A New Thermodynamic Model Free from Lattice Theory Assumptions
    Almeida e Sousa, Luis
    Domotor, Kata J.
    Paiva, Mafalda
    Cacela, Constanca
    PHARMACEUTICAL RESEARCH, 2019, 36 (12)
  • [10] Effect of drug-polymer interactions on the aqueous solubility of milled solid dispersions
    Al-Obaidi, Hisham
    Lawrence, M. Jayne
    Shah, Sonal
    Moghul, Henna
    Al-Saden, Noor
    Bari, Fiza
    INTERNATIONAL JOURNAL OF PHARMACEUTICS, 2013, 446 (1-2) : 100 - 105