Microstructure based simulation of the disintegration and dissolution of immediate release pharmaceutical tablets

Result code in IS VaVaI

<a href="https://www.isvavai.cz/riv?ss=detail&h=RIV%2F60461373%3A22340%2F21%3A43922318" target="_blank" >RIV/60461373:22340/21:43922318 - isvavai.cz</a>

Result on the web

<a href="https://doi.org/10.1016/j.powtec.2020.08.093" target="_blank" >https://doi.org/10.1016/j.powtec.2020.08.093</a>

DOI - Digital Object Identifier

<a href="http://dx.doi.org/10.1016/j.powtec.2020.08.093" target="_blank" >10.1016/j.powtec.2020.08.093</a>

Result language

angličtina

Original language name

Microstructure based simulation of the disintegration and dissolution of immediate release pharmaceutical tablets

Original language description

The design of pharmaceutical tablets involves the determination of formulation parameters that define the tablet composition and internal microstructure. These parameters must be chosen so that the release of an active pharmaceutical ingredient (API) from the tablet follows a prescribed dissolution curve. In the case of immediate release formulations, the dissolution process typically consists of tablet disintegration, followed by the dissolution of the disintegration fragments. In order to find the appropriate values of formulation parameters, numerous experiments are typically required. In the present work, we propose a computational methodology for in silico design of tablet formulations with the aim of reducing the amount experimental work required during tablet design. The methodology is based on the coupling of two modelling approaches: (i) tablet fragmentation triggered by the swelling of the disintegrant is simulated by the discrete element method (DEM), and (ii) the dissolution of the resulting population of disintegration fragments is simulated using a finite volume gridbased model. The final API release curve is then obtained by the superposition of dissolution curves originating from the individual disintegration fragments. Using directly compressed tablets containing ibuprofen as the API and croscarmellose sodium as the disintegrant, the model was validated against experimental data. The fragment size distribution was evaluated by static light scattering and the dissolution profiles were obtained by a standard dissolution apparatus with UV/Vis spectroscopic detection. We demonstrate that the computational methodology is able to quantitatively predict the effect of disintegrant content and API primary particle size on the fragment size distribution and the final dissolution profiles, and is therefore useful as a tool for computerassisted tablet formulation design. (C) 2020 Elsevier B.V. All rights reserved.

Czech name

—

Czech description

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Type

J_imp - Article in a specialist periodical, which is included in the Web of Science database

CEP classification

—

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

2021

Confidentiality

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

Name of the periodical

Powder Technology

ISSN

0032-5910

e-ISSN

—

Volume of the periodical

377

Issue of the periodical within the volume

2 January 2021

Country of publishing house

US - UNITED STATES

Number of pages

12

Pages from-to

257-268

UT code for WoS article

000598624300011

EID of the result in the Scopus database

2-s2.0-85090750689