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

Result code in 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>

Result on the web

<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>

Result language

angličtina

Original language name

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

Original language description

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

Czech name

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Czech description

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Type

J_SC - Article in a specialist periodical, which is included in the SCOPUS database

CEP classification

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OECD FORD branch

20401 - Chemical engineering (plants, products)

Project

<a href="/en/project/GX19-26127X" target="_blank" >GX19-26127X: The robotic nano-pharmacist: Next-generation manufacturing processes for personalised therapeutic agents</a><br>

Continuities

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

Publication year

2019

Confidentiality

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

Name of the periodical

Chemical Engineering Journal

ISSN

1385-8947

e-ISSN

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Volume of the periodical

Neuveden

Issue of the periodical within the volume

09.12.2019

Country of publishing house

CH - SWITZERLAND

Number of pages

8

Pages from-to

1-8

UT code for WoS article

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EID of the result in the Scopus database

2-s2.0-85076861881