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Combinative Particle Size Reduction Technologies for the Production of Drug Nanocrystals.

Salazar J, Müller RH, Möschwitzer JP - J Pharm (Cairo) (2014)

Bottom Line: These processes were developed to improve the particle size reduction effectiveness of the standard techniques.The combinative processes lead in general to improved particle size reduction effectiveness.The combinative particle size reduction technologies are very useful formulation tools, and they will continue acquiring importance for the production of drug nanocrystals.

View Article: PubMed Central - PubMed

Affiliation: Institute of Pharmacy, Department of Pharmaceutics, Biopharmaceutics and NutriCosmetics, Freie Universität Berlin, Kelchstraße 31, 12169 Berlin, Germany.

ABSTRACT
Nanosizing is a suitable method to enhance the dissolution rate and therefore the bioavailability of poorly soluble drugs. The success of the particle size reduction processes depends on critical factors such as the employed technology, equipment, and drug physicochemical properties. High pressure homogenization and wet bead milling are standard comminution techniques that have been already employed to successfully formulate poorly soluble drugs and bring them to market. However, these techniques have limitations in their particle size reduction performance, such as long production times and the necessity of employing a micronized drug as the starting material. This review article discusses the development of combinative methods, such as the NANOEDGE, H 96, H 69, H 42, and CT technologies. These processes were developed to improve the particle size reduction effectiveness of the standard techniques. These novel technologies can combine bottom-up and/or top-down techniques in a two-step process. The combinative processes lead in general to improved particle size reduction effectiveness. Faster production of drug nanocrystals and smaller final mean particle sizes are among the main advantages. The combinative particle size reduction technologies are very useful formulation tools, and they will continue acquiring importance for the production of drug nanocrystals.

No MeSH data available.


Particle size reduction performance of standard and combinative technologies. Six levels: premilling (1), 1 HPH cycle at 1500 bar/1 hour of WBM (2), 5 cycles/2 hours (3), 10 cycles/4 hours (4), 15 cycles/8 hours (5), and 20 cycles/24 hours (6).
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fig2: Particle size reduction performance of standard and combinative technologies. Six levels: premilling (1), 1 HPH cycle at 1500 bar/1 hour of WBM (2), 5 cycles/2 hours (3), 10 cycles/4 hours (4), 15 cycles/8 hours (5), and 20 cycles/24 hours (6).

Mentions: The particle size reduction performances of standard and selected combinative processes with glibenclamide as a model compound are compared in Figure 2. The graphic description shows the superior particle size reduction effectiveness of the combinative technologies regarding the process length to achieve a nanosuspension and the smallest final mean particle size. The HPH and WBM standard techniques achieved a final mean particle size of 772 nm and 191 nm at the end of their respective processes (after 20 cycles of HPH and 24 hours of WBM). However, these processes presented a slower particle size reduction progress than the combinative methods.


Combinative Particle Size Reduction Technologies for the Production of Drug Nanocrystals.

Salazar J, Müller RH, Möschwitzer JP - J Pharm (Cairo) (2014)

Particle size reduction performance of standard and combinative technologies. Six levels: premilling (1), 1 HPH cycle at 1500 bar/1 hour of WBM (2), 5 cycles/2 hours (3), 10 cycles/4 hours (4), 15 cycles/8 hours (5), and 20 cycles/24 hours (6).
© Copyright Policy - open-access
Related In: Results  -  Collection

Show All Figures
getmorefigures.php?uid=PMC4590828&req=5

fig2: Particle size reduction performance of standard and combinative technologies. Six levels: premilling (1), 1 HPH cycle at 1500 bar/1 hour of WBM (2), 5 cycles/2 hours (3), 10 cycles/4 hours (4), 15 cycles/8 hours (5), and 20 cycles/24 hours (6).
Mentions: The particle size reduction performances of standard and selected combinative processes with glibenclamide as a model compound are compared in Figure 2. The graphic description shows the superior particle size reduction effectiveness of the combinative technologies regarding the process length to achieve a nanosuspension and the smallest final mean particle size. The HPH and WBM standard techniques achieved a final mean particle size of 772 nm and 191 nm at the end of their respective processes (after 20 cycles of HPH and 24 hours of WBM). However, these processes presented a slower particle size reduction progress than the combinative methods.

Bottom Line: These processes were developed to improve the particle size reduction effectiveness of the standard techniques.The combinative processes lead in general to improved particle size reduction effectiveness.The combinative particle size reduction technologies are very useful formulation tools, and they will continue acquiring importance for the production of drug nanocrystals.

View Article: PubMed Central - PubMed

Affiliation: Institute of Pharmacy, Department of Pharmaceutics, Biopharmaceutics and NutriCosmetics, Freie Universität Berlin, Kelchstraße 31, 12169 Berlin, Germany.

ABSTRACT
Nanosizing is a suitable method to enhance the dissolution rate and therefore the bioavailability of poorly soluble drugs. The success of the particle size reduction processes depends on critical factors such as the employed technology, equipment, and drug physicochemical properties. High pressure homogenization and wet bead milling are standard comminution techniques that have been already employed to successfully formulate poorly soluble drugs and bring them to market. However, these techniques have limitations in their particle size reduction performance, such as long production times and the necessity of employing a micronized drug as the starting material. This review article discusses the development of combinative methods, such as the NANOEDGE, H 96, H 69, H 42, and CT technologies. These processes were developed to improve the particle size reduction effectiveness of the standard techniques. These novel technologies can combine bottom-up and/or top-down techniques in a two-step process. The combinative processes lead in general to improved particle size reduction effectiveness. Faster production of drug nanocrystals and smaller final mean particle sizes are among the main advantages. The combinative particle size reduction technologies are very useful formulation tools, and they will continue acquiring importance for the production of drug nanocrystals.

No MeSH data available.