Drug amorphisation by fluid bed hot-melt impregnation of mesoporous silica carriers

Kód výsledku v IS VaVaI

<a href="https://www.isvavai.cz/riv?ss=detail&h=RIV%2F60461373%3A22340%2F19%3A43919146" target="_blank" >RIV/60461373:22340/19:43919146 - isvavai.cz</a>

Výsledek na webu

<a href="https://doi.org/10.1016/j.cej.2019.123754" target="_blank" >https://doi.org/10.1016/j.cej.2019.123754</a>

DOI - Digital Object Identifier

<a href="http://dx.doi.org/10.1016/j.cej.2019.123754" target="_blank" >10.1016/j.cej.2019.123754</a>

Jazyk výsledku

angličtina

Název v původním jazyce

Drug amorphisation by fluid bed hot-melt impregnation of mesoporous silica carriers

Popis výsledku v původním jazyce

Amorphisation using mesoporous inorganic carriers represents an emerging formulation strategy for the dissolution rate enhancement of poorly water-soluble Active Pharmaceutical Ingredients (APIs). This approach employs API loading to a porous carrier, which stabilises the amorphous form and prevents recrystallisation due to spatial confinement in the mesopores. In this work, we utilise recently discovered silica particles with a unique pore structure that contain well-connected macropores for rapid capillary transport of the molten API, alongside mesopores for efficient drug amorphisation. We demonstrate that these particles enable efficient drug loading by a solvent-free process, namely hot-melt impregnation in a fluidised bed reactor. By controlling the process temperature and therefore the melt-in rate of the API, we show that the co-fluidisation of the API source crystals and silica carrier particles is possible without wall build-up or agglomeration. Using ibuprofen as a model API, we systematically investigate the effect of drug loading (30–50% w/w) and process conditions (heating time, process temperature) on the physico-chemical and dissolution properties of the product. The amorphous content of the silica particles after drug loading was established by DSC and XRPD and the chemical stability was confirmed by FTIR spectroscopy. More than a five-fold dissolution rate enhancement compared to crystalline API was achieved by fluid bed amorphisation

Název v anglickém jazyce

Drug amorphisation by fluid bed hot-melt impregnation of mesoporous silica carriers

Popis výsledku anglicky

Amorphisation using mesoporous inorganic carriers represents an emerging formulation strategy for the dissolution rate enhancement of poorly water-soluble Active Pharmaceutical Ingredients (APIs). This approach employs API loading to a porous carrier, which stabilises the amorphous form and prevents recrystallisation due to spatial confinement in the mesopores. In this work, we utilise recently discovered silica particles with a unique pore structure that contain well-connected macropores for rapid capillary transport of the molten API, alongside mesopores for efficient drug amorphisation. We demonstrate that these particles enable efficient drug loading by a solvent-free process, namely hot-melt impregnation in a fluidised bed reactor. By controlling the process temperature and therefore the melt-in rate of the API, we show that the co-fluidisation of the API source crystals and silica carrier particles is possible without wall build-up or agglomeration. Using ibuprofen as a model API, we systematically investigate the effect of drug loading (30–50% w/w) and process conditions (heating time, process temperature) on the physico-chemical and dissolution properties of the product. The amorphous content of the silica particles after drug loading was established by DSC and XRPD and the chemical stability was confirmed by FTIR spectroscopy. More than a five-fold dissolution rate enhancement compared to crystalline API was achieved by fluid bed amorphisation

Druh

J_SC - Článek v periodiku v databázi SCOPUS

CEP obor

—

OECD FORD obor

20401 - Chemical engineering (plants, products)

Projekt

<a href="/cs/project/GX19-26127X" target="_blank" >GX19-26127X: Robotický nano-lékárník: Výrobní procesy budoucnosti pro personalisovaná terapeutika</a><br>

Návaznosti

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

Rok uplatnění

2019

Kód důvěrnosti údajů

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

Název periodika

Chemical Engineering Journal

ISSN

1385-8947

e-ISSN

—

Svazek periodika

Neuveden

Číslo periodika v rámci svazku

09.12.2019

Stát vydavatele periodika

CH - Švýcarská konfederace

Počet stran výsledku

8

Strana od-do

1-8

Kód UT WoS článku

—

EID výsledku v databázi Scopus

2-s2.0-85076861881