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Overcoming drug impurity challenges in amorphous solid dispersion with rational development of biorelevant dissolution-permeation methodHuzjak, Tilen, 1995- ...Hot-melt extrusion is often used to prepare amorphous solid dispersion to overcome low drug solubility and enhance bio-performance of the formulation. Due to the uniqueness of each drug - polymer ... combination and its physico-chemical properties, setting the appropriate HME barrel temperature, feed rate and screw speed ensures drug amorphization, absence of residual crystallinity, absence of water, and a suitable drug release profile. In this research, samples with BCS II/IV model drug and PVP/VA polymer were prepared to evaluate the impact of HME process parameters, incoming drug form (anhydrous vs. hydrate), and drug supplier (i.e., impurity profile), on biorelevant drug release. This study provides a relationship between observed in vitro supersaturation and precipitation behavior of amorphous solid dispersion formulation with in vivo results, on patients, by using the acceptor profile of side-by-side dissolution-permeation apparatus. An in vitro dissolution method, in small volumes, in an apparatus with paddles and dissolution-permeation side-by-side method was developed on the MicroFlux™ apparatus to assess if the differences observed in vitro bears relevance to the bioequivalence outcome in vivo. The former was used to guide the generic drug product development due to high discriminatory strength, while the latter was biorelevant, due to the inclusion of the second compartment assuring absorptive environment to capture the impact of supersaturation and subsequent precipitation on bioavailability. Bio-relevancy of the in vitro method was confirmed with the in vivo dog study and clinical study on patients, and an in vitro - in vivo correlation was established. For the investigated BCS II/IV drug, this research highlights the importance of considering supersaturation and formation of colloidal species during amorphous solid dispersion release testing to assure product quality, safety and efficacy.Source: European Journal of Pharmaceutical Sciences. - ISSN 0928-0987 (Vol. 192, 2024, 12 str.)Type of material - article, component part ; adult, seriousPublish date - 2024Language - englishCOBISS.SI-ID - 188116227
Author
Huzjak, Tilen, 1995- |
Jakasanovski, Ognen |
Berginc, Katja, 1980- |
Puž, Vid |
Zajc-Kreft, Katarina |
Jeraj, Žiga |
Janković, Biljana, 1982-
Topics
Farmacevtske oblike |
Topnost |
biorelevant dissolution-permeation |
hot-melt extrusion |
In vitro – in vivo correlation |
liquid-liquid phase separation |
solid dispersion |
supersaturation |
biorelevantno raztapljanje-prepustnost |
ekstrudiranje z vročim taljenjem |
in vitro – in vivo korelacija |
ločevanje tekoče-tekoče faze |
trdna disperzija |
prenasičenost
Author | Huzjak, Tilen, 1995- ... |
Title | Overcoming drug impurity challenges in amorphous solid dispersion with rational development of biorelevant dissolution-permeation method |
Publication date | |
COBISS.SI-ID | 188116227 |
Publication version in repository | Publisher's version |
Publication licence | Creative Commons Attribution-NoDerivatives 4.0 International |
Embargo | Immediate publication for public |
Project(s) from which the publication was funded
Title | Acronym | Project ID | Funder |
---|---|---|---|
Lek | Lek MA-16430-2020 | ||
Farmacevtska tehnologija: od dostavnih sistemov učinkovin do terapijskih izidov zdravil pri otrocih in starostnikih | P1-0189-2018 |
Javna agencija za znanstvenoraziskovalno in inovacijsko dejavnost Republike Slovenije |
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https://www.sciencedirect.com/science/article/pii/S0928098723002841 |
https://repozitorij.uni-lj.si/IzpisGradiva.php?id=155631 |
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Database name | Field | Year |
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Links to authors' personal bibliographies | Links to information on researchers in the SICRIS system |
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Huzjak, Tilen, 1995- | 56114 |
Jakasanovski, Ognen | |
Berginc, Katja, 1980- | 25492 |
Puž, Vid | 35337 |
Zajc-Kreft, Katarina | 13309 |
Jeraj, Žiga | |
Janković, Biljana, 1982- | 34670 |
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