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The step-wise dissolution method: An efficient DSC-based protocol for verification of predicted API-polymer compatibility

The result's identifiers

  • Result code in IS VaVaI

    <a href="https://www.isvavai.cz/riv?ss=detail&h=RIV%2F60461373%3A22340%2F23%3A43928104" target="_blank" >RIV/60461373:22340/23:43928104 - isvavai.cz</a>

  • Result on the web

    <a href="https://www.sciencedirect.com/science/article/pii/S0378517323010256?via%3Dihub" target="_blank" >https://www.sciencedirect.com/science/article/pii/S0378517323010256?via%3Dihub</a>

  • DOI - Digital Object Identifier

    <a href="http://dx.doi.org/10.1016/j.ijpharm.2023.123604" target="_blank" >10.1016/j.ijpharm.2023.123604</a>

Alternative languages

  • Result language

    angličtina

  • Original language name

    The step-wise dissolution method: An efficient DSC-based protocol for verification of predicted API-polymer compatibility

  • Original language description

    The development of an amorphous solid dispersion (ASD) is a promising strategy for improving the low bioavailability of many poorly water-soluble active pharmaceutical ingredients (APIs). The construction of a temperature-composition (T-C) phase diagram for an API-polymer combination is imperative as it can provide critical information that is essential for formulating stable ASDs. However, the currently followed differential scanning calorimetry (DSC)-based strategies for API solubility determination in a polymer at elevated temperatures are inefficient and, on occasions, unreliable, which may lead to an inaccurate prediction at lower temperatures of interest (i.e., T = 25 degrees C). Recently, we proposed a novel DSC-based protocol called the &quot;step-wise dissolution&quot; (S-WD) method, which is both cost-and time-effective. The objective of this study was to test the applicability of the S-WD method regarding expeditious verification of the purely-predicted API-polymer compatibility via the perturbed chain-statistical associating fluid theory (PC-SAFT) equation of state (EOS). Fifteen API-polymer T-C phase diagrams were reliably constructed, with three distinct API-polymer case types being identified regarding the approach used for the S-WD method. Overall, the PC-SAFT EOS provided satisfactory qualitative descriptions of the API-polymer compatibility, but not necessarily accurate quantitative predictions of the API solubility in the polymer at T = 25 degrees C. The S-WD method was subsequently modified and an optimal protocol was proposed, which can significantly reduce the required experimental effort.

  • Czech name

  • Czech description

Classification

  • Type

    J<sub>imp</sub> - Article in a specialist periodical, which is included in the Web of Science database

  • CEP classification

  • OECD FORD branch

    10403 - Physical chemistry

Result continuities

  • Project

    <a href="/en/project/GA22-07164S" target="_blank" >GA22-07164S: Rational design of drug delivery systems based on tailored biodegradable polymers using an iterative in silico and experimental approach</a><br>

  • Continuities

    P - Projekt vyzkumu a vyvoje financovany z verejnych zdroju (s odkazem do CEP)

Others

  • Publication year

    2023

  • Confidentiality

    S - Úplné a pravdivé údaje o projektu nepodléhají ochraně podle zvláštních právních předpisů

Data specific for result type

  • Name of the periodical

    INTERNATIONAL JOURNAL OF PHARMACEUTICS

  • ISSN

    0378-5173

  • e-ISSN

    1873-3476

  • Volume of the periodical

    648

  • Issue of the periodical within the volume

    prosinec 2023

  • Country of publishing house

    US - UNITED STATES

  • Number of pages

    14

  • Pages from-to

    123604

  • UT code for WoS article

    001125162800001

  • EID of the result in the Scopus database

    2-s2.0-85178174698