Agglomeration of celecoxib by quasi-emulsion solvent diffusion method without stabilizer: effect of good solvent

Aim: The aim of the present research is to investigate the feasibility of agglomeration of crystals by the quasi-emulsion solvent diffusion method without using a stabilizer. Method: Two solvent systems comprising a solvent and an antisolvent (water) were used to prepare celecoxib agglomerates. To t...

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Bibliographic Details
Published in:Pharmaceutical development and technology 2018-11, Vol.23 (10), p.1037-1046
Main Authors: Maghsoodi, Maryam, Nokhodchi, Ali
Format: Article
Language:English
Subjects:
Anti-Inflammatory Agents, Non-Steroidal - chemical synthesis
Celecoxib
Celecoxib - chemical synthesis
Chemistry, Pharmaceutical - methods
Emulsions
Excipients
good solvent
Particle Size
quasi-emulsion solvent diffusion method
Solubility
Solvents - chemical synthesis
X-Ray Diffraction - methods
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Summary:Aim: The aim of the present research is to investigate the feasibility of agglomeration of crystals by the quasi-emulsion solvent diffusion method without using a stabilizer. Method: Two solvent systems comprising a solvent and an antisolvent (water) were used to prepare celecoxib agglomerates. To this end, seven solvents including propanol, methyl acetate, methyl ethyl ketone, butanol, ethyl acetate, isopropyl acetate, and pentanol were examined. The agglomerates were evaluated by micromeritic properties (e.g., size, density, flowability), yield, drug physical state, friability, and dissolution behavior. Results: In the present study the clear trend was observed experimentally in the agglomerate properties as a function of physical properties of the solvent such as miscibility with water. Solvents with high water miscibility (25% v/v) resulted in sticky and hollow particles, while solvents with low water miscibility (3%v/v) led to the formation of agglomerates with low strength. However, the agglomerates made from the solvents with intermediate water miscibility (10% v/v), may reflect a greater integrity of the agglomerates regarding yield and strength. Conclusion: Results of this study offer a useful starting point for a conceptual framework to guide the selection of solvent systems for the quasi-emulsion solvent diffusion method without using a stabilizer.
ISSN:1083-7450
1097-9867
DOI:10.1080/10837450.2016.1270965