Ball milling and hot-melt extrusion of indomethacin-L-arginine-vinylpyrrolidone-vinyl acetate copolymer: Solid-state properties and dissolution performance
The result's identifiers
Result code in IS VaVaI
<a href="https://www.isvavai.cz/riv?ss=detail&h=RIV%2F60461373%3A22310%2F22%3A43924989" target="_blank" >RIV/60461373:22310/22:43924989 - isvavai.cz</a>
Alternative codes found
RIV/60461373:22340/22:43924989
Result on the web
<a href="https://www.sciencedirect.com/science/article/pii/S0378517321012308?via%3Dihub" target="_blank" >https://www.sciencedirect.com/science/article/pii/S0378517321012308?via%3Dihub</a>
DOI - Digital Object Identifier
<a href="http://dx.doi.org/10.1016/j.ijpharm.2021.121424" target="_blank" >10.1016/j.ijpharm.2021.121424</a>
Alternative languages
Result language
angličtina
Original language name
Ball milling and hot-melt extrusion of indomethacin-L-arginine-vinylpyrrolidone-vinyl acetate copolymer: Solid-state properties and dissolution performance
Original language description
Commonly applied approaches to enhance the dissolution properties of low water-soluble crystalline active pharmaceutical ingredients (APIs) include their amorphization by incorporation into a polymeric matrix and the formation of amorphous solid dispersions, or blending APIs with low-molecular-weight excipients and the formation of a co-amorphous system. This study focused on the preparation and characterization of binary (consisting of indomethacin (IND) and polymer - copovidone (PVP VA 64), as a carrier, or amino acid - L-arginine (ARG), as a co-former) and ternary (comprising the same API, polymer, and amino acid) formulations. Formulations were produced by ball milling (BM) and/or hot-melt extrusion (HME), and extensive physicochemical characterization was performed. Specifically, the physicochemical and solid-state properties of a model IND-ARG system incorporated into a polymeric matrix of PVP VA 64 by HME and BM as well as by combined BM/HME method together with the impact of the preparation strategy on the dissolution profiles and long-term physical stability were investigated. Ball-milled binary and ternary formulations were found to be amorphous. The residual crystals corresponding to IND-ARG salt were identified in the ternary formulations produced via HME. Despite the presence of a crystalline phase, dissolution tests showed that ternary systems prepared by HME exhibited improved IND solubility when compared to pure crystalline IND and their corresponding physical mixture. None of the binary and ternary formulations that were initially fully amorphous did undergo recrystallization during the entire period of preservation (minimum of 12 months) in dry conditions at 25 degrees C.
Czech name
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Czech description
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Classification
Type
J<sub>imp</sub> - Article in a specialist periodical, which is included in the Web of Science database
CEP classification
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OECD FORD branch
10404 - Polymer science
Result continuities
Project
<a href="/en/project/GA19-02889S" target="_blank" >GA19-02889S: Stability of amorphous solid dispersions: Predictions by SAFT equations of state and their experimental verification</a><br>
Continuities
P - Projekt vyzkumu a vyvoje financovany z verejnych zdroju (s odkazem do CEP)
Others
Publication year
2022
Confidentiality
S - Úplné a pravdivé údaje o projektu nepodléhají ochraně podle zvláštních právních předpisů
Data specific for result type
Name of the periodical
International Journal of Pharmaceutics
ISSN
0378-5173
e-ISSN
1873-3476
Volume of the periodical
613
Issue of the periodical within the volume
únor 2022
Country of publishing house
US - UNITED STATES
Number of pages
10
Pages from-to
121424
UT code for WoS article
000742653100007
EID of the result in the Scopus database
2-s2.0-85122227362