Analysis of niflumic acid prepared by rapid microwave-assisted evaporation.

Evaporative crystallization is widely applied in several industrial processes, including the pharmaceutical industry. Microwave irradiation can significantly speed up solvent evaporation in these crystallization processes, resulting in reduced particle size due to rapid crystallization. A single-mode microwave setup was used for evaporative crystallization of the model active pharmaceutical ingredient, niflumic acid, and the polymer, polyvinylpirrolidone (PVP). Production of crystals by microwave irradiation offers a modern way for drug formulation, and by reducing the particle size the dissolution rate and bioavailability of the active pharmaceutical ingredient can be enhanced. In this study, a 2.5-fold increase in the dissolution rate of the produced niflumic acid crystals was observed compared to the dissolution rate of the original drug in 120min. When niflumic acid was produced together with the PVP in the microwave system, an amorphous solid dispersion was created with particles in the nano-size range, which showed a 5-fold increase in dissolution rate in 120min compared to the dissolution of the crystalline niflumic acid samples created by the microwave irradiation in the absence of PVP.

[1]  K. Johnston,et al.  Enhanced drug dissolution using evaporative precipitation into aqueous solution. , 2002, International journal of pharmaceutics.

[2]  Norbert Radacsi,et al.  Microwave-Assisted Evaporative Crystallization of Niflumic Acid for Particle Size Reduction , 2013 .

[3]  J Kristl,et al.  Investigation of preparation parameters to improve the dissolution of poorly water-soluble meloxicam. , 2009, International journal of pharmaceutics.

[4]  L. Goodman,et al.  The Pharmacological Basis of Therapeutics , 1976 .

[5]  Jennifer B Dressman,et al.  Classification of orally administered drugs on the World Health Organization Model list of Essential Medicines according to the biopharmaceutics classification system. , 2004, European journal of pharmaceutics and biopharmaceutics : official journal of Arbeitsgemeinschaft fur Pharmazeutische Verfahrenstechnik e.V.

[6]  R. Ambrus,et al.  Physico-chemical characterization and dissolution properties of nifluminic acid-cyclodextrin-PVP ternary systems , 2011 .

[7]  Souheng Wu,et al.  Calculation of interfacial tension in polymer systems , 2007 .

[8]  Hirofumi Takeuchi,et al.  Particle design of poorly water-soluble drug substances using supercritical fluid technologies. , 2008, Advanced drug delivery reviews.

[9]  P. Sharma,et al.  EVALUATION OF ENHANCEMENT OF SOLUBILITY OF PARACETAMOL BY SOLID DISPERSION TECHNIQUE USING DIFFERENT POLYMERS CONCENTRATION , 2011 .

[10]  Michael D. Abràmoff,et al.  Image processing with ImageJ , 2004 .

[11]  Koichi Wada,et al.  Formulation design for poorly water-soluble drugs based on biopharmaceutics classification system: basic approaches and practical applications. , 2011, International journal of pharmaceutics.

[12]  C. Frances,et al.  On the use of scanning electron microscopy for the modelling of co-grinding kinetics in a tumbling ball mill , 2004 .

[13]  T. Arita,et al.  Inhibitory Effect of Polyvinylpyrrolidone on the Crystallization of Drugs , 1978 .

[14]  A. Noyes,et al.  The rate of solution of solid substances in their own solutions , 1897 .