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

Kód výsledku v 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>

Výsledek na webu

<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>

Jazyk výsledku

angličtina

Název v původním jazyce

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

Popis výsledku v původním jazyce

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.

Název v anglickém jazyce

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

Popis výsledku anglicky

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.

Druh

J_imp - Článek v periodiku v databázi Web of Science

CEP obor

—

OECD FORD obor

10403 - Physical chemistry

Projekt

<a href="/cs/project/GA22-07164S" target="_blank" >GA22-07164S: Racionální návrh systémů pro dodávání léčiv založených na laditelných biodegradabilních polymerech: iterativní in silico a experimentální postup</a><br>

Návaznosti

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

Rok uplatnění

2023

Kód důvěrnosti údajů

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

Název periodika

INTERNATIONAL JOURNAL OF PHARMACEUTICS

ISSN

0378-5173

e-ISSN

1873-3476

Svazek periodika

648

Číslo periodika v rámci svazku

prosinec 2023

Stát vydavatele periodika

US - Spojené státy americké

Počet stran výsledku

14

Strana od-do

123604

Kód UT WoS článku

001125162800001

EID výsledku v databázi Scopus

2-s2.0-85178174698