Effects of polymers on the crystallinity of nanonized meloxicam during a co-grinding process

Crystallinity changes of MX in the samples made with different polymers. [Display omitted] •Polymers were used to reduce the grinding energy during co-grinding process to produce nanoparticles.•PEG did not have a significant effect on the crystallinity of meloxicam but the PVP decreased it drastical...

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Veröffentlicht in:European polymer journal 2013-09, Vol.49 (9), p.2426-2432
Hauptverfasser: Mártha, Csaba, Kürti, Levente, Farkas, Gabriella, Jójárt-Laczkovich, Orsolya, Szalontai, Balázs, Glässer, Erik, Deli, Mária A., Szabó-Révész, Piroska
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container_end_page 2432
container_issue 9
container_start_page 2426
container_title European polymer journal
container_volume 49
creator Mártha, Csaba
Kürti, Levente
Farkas, Gabriella
Jójárt-Laczkovich, Orsolya
Szalontai, Balázs
Glässer, Erik
Deli, Mária A.
Szabó-Révész, Piroska
description Crystallinity changes of MX in the samples made with different polymers. [Display omitted] •Polymers were used to reduce the grinding energy during co-grinding process to produce nanoparticles.•PEG did not have a significant effect on the crystallinity of meloxicam but the PVP decreased it drastically.•Weak secondary bonding between meloxicam and the PVP was found by FT-IR.•SEM images confirmed the major particle size decrease and the differences in crystal habit of meloxicam. Particle size reduction to the submicron region in a grinding process demands a high energy input. This grinding energy requirement can be reduced by means of a suitable additive, e.g. polymer, and performing a co-grinding process. Although these excipients promote attainment of the nanoparticle size range, they can also decrease the crystallinity of the active pharmaceutical ingredient. Different types of polymers have different abilities to amorphize the active material. To demonstrate the amorphization effects of different polymers, meloxicam (MX) as a model drug was subjected to co-grinding in the presence of one or other of four different polymers (PEG 6000, PEG 20,000, PVP C30 and PVP K25) and the products were investigated by XRPD, FT-IR and SEM. Although the PEG materials slightly melted and covered the MX particles during the grinding, they did not cause any changes in crystallinity. The PVP polymers softened and covered the MX particles, but drastically reduced the crystallinity of the drug. FT-IR revealed a weak secondary bonding between MX and the PVP polymer chain.
doi_str_mv 10.1016/j.eurpolymj.2013.03.006
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[Display omitted] •Polymers were used to reduce the grinding energy during co-grinding process to produce nanoparticles.•PEG did not have a significant effect on the crystallinity of meloxicam but the PVP decreased it drastically.•Weak secondary bonding between meloxicam and the PVP was found by FT-IR.•SEM images confirmed the major particle size decrease and the differences in crystal habit of meloxicam. Particle size reduction to the submicron region in a grinding process demands a high energy input. This grinding energy requirement can be reduced by means of a suitable additive, e.g. polymer, and performing a co-grinding process. Although these excipients promote attainment of the nanoparticle size range, they can also decrease the crystallinity of the active pharmaceutical ingredient. Different types of polymers have different abilities to amorphize the active material. To demonstrate the amorphization effects of different polymers, meloxicam (MX) as a model drug was subjected to co-grinding in the presence of one or other of four different polymers (PEG 6000, PEG 20,000, PVP C30 and PVP K25) and the products were investigated by XRPD, FT-IR and SEM. Although the PEG materials slightly melted and covered the MX particles during the grinding, they did not cause any changes in crystallinity. The PVP polymers softened and covered the MX particles, but drastically reduced the crystallinity of the drug. 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[Display omitted] •Polymers were used to reduce the grinding energy during co-grinding process to produce nanoparticles.•PEG did not have a significant effect on the crystallinity of meloxicam but the PVP decreased it drastically.•Weak secondary bonding between meloxicam and the PVP was found by FT-IR.•SEM images confirmed the major particle size decrease and the differences in crystal habit of meloxicam. Particle size reduction to the submicron region in a grinding process demands a high energy input. This grinding energy requirement can be reduced by means of a suitable additive, e.g. polymer, and performing a co-grinding process. Although these excipients promote attainment of the nanoparticle size range, they can also decrease the crystallinity of the active pharmaceutical ingredient. Different types of polymers have different abilities to amorphize the active material. To demonstrate the amorphization effects of different polymers, meloxicam (MX) as a model drug was subjected to co-grinding in the presence of one or other of four different polymers (PEG 6000, PEG 20,000, PVP C30 and PVP K25) and the products were investigated by XRPD, FT-IR and SEM. Although the PEG materials slightly melted and covered the MX particles during the grinding, they did not cause any changes in crystallinity. The PVP polymers softened and covered the MX particles, but drastically reduced the crystallinity of the drug. 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subjects Amorphization
Bonding
Co-grinding
Comminution
Covering
Crystallinity
Drugs
Ingredients
Meloxicam
Nanostructure
Polyethylene glycol
Polymers
Polyvinylpyrrolidone
title Effects of polymers on the crystallinity of nanonized meloxicam during a co-grinding process
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