Development of a rapidly dispersing tablet of a poorly wettable compound: formulation DOE and mechanistic study of effect of formulation excipients on wetting of celecoxib

International Journal of Pharmaceutics
Xiaorong HeDavid C Sperry

Abstract

Celecoxib has extremely poor aqueous wettability and dispersibility. A dispersibility method was developed to study the effects of formulation excipients and processing methods on wetting of celecoxib. In this method, a tablet or powder was placed in water and the turbidity of the resulting "dynamic" suspension was measured. Higher turbidity values reflect better dispersibility. Results show that wet granulation facilitates better drug dispersion than does dry granulation or direct compression. Results from a screening formulation statistical design of experiments (DOE) show that sodium lauryl sulfate (SLS), an anionic surfactant, gives higher celecoxib dispersibility than polysorbate 80, a neutral surfactant. Polyplasdone XL as a disintegrant results in better celecoxib dispersibility than sodium starch glycolate. The binder Kollidon 30 leads to better dispersibility, but slower disintegration than Kollidon 12. Jet-milling celecoxib with excipients not only improves dispersibility of the drug but also the ease of material handling. The method of microcrystalline cellulose addition does not significantly impact tablet properties. The effect of critical formulation variables on the wettability of celecoxib was further examined i...Continue Reading

Citations

Oct 16, 2012·Journal of Pharmacy & Bioallied Sciences·Bhumika PatelDeepali Swarnkar
Aug 11, 2016·Journal of Pharmaceutical Sciences·Parind Mahendrakumar DesaiPaul Wan Sia Heng
Jan 25, 2013·Drug Development and Industrial Pharmacy·Johnny Edward Aguilar-DíazJosé Ramón Ticó
Mar 25, 2010·European Journal of Pharmaceutics and Biopharmaceutics : Official Journal of Arbeitsgemeinschaft Für Pharmazeutische Verfahrenstechnik E.V·Farhan AlHusbanAfzal R Mohammed
Mar 17, 2010·European Journal of Pharmaceutical Sciences : Official Journal of the European Federation for Pharmaceutical Sciences·Vibha PuriArvind K Bansal
Feb 9, 2019·Carbohydrate Polymers·Maria Terezinha FrançaHellen Karine Stulzer

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