How spherical crystallization improves direct tableting properties: a review.

Direct tableting has been renewed as a preferable process by simply mixing and compressing powder to save time and cost in comparison with granule tableting. Direct compression tableting as a technique has been successfully applied to numerous drugs on the industrial scale, although the success of any procedure, and resulting mechanical properties of tablets, is strongly affected by the quality of the crystals used. Good flowability, packability and compactability are prerequisite for drug to be prepared by direct tableting. When the mechanical properties of the drug particles are inadequate a primary granulation is necessary. The use of spherical crystallization as a technique appears to be an efficient alternative for obtaining suitable particles for direct tableting. Spherical crystallization is a particle design technique, by which crystallization and agglomeration can be carried out simultaneously in one step and which has been successfully utilized for improvement the micromeritic properties of crystalline drugs. In this review, we will discuss how the micromeritic properties of the particles such as flowability, packability and compactability can be improved by spherical crystallization technique.

[1]  L L Augsburger,et al.  Plastic flow during compression of directly compressible fillers and its effect on tablet strength. , 1977, Journal of pharmaceutical sciences.

[2]  Kimio Kawakita,et al.  Some considerations on powder compression equations , 1971 .

[3]  Toshiyuki Niwa,et al.  Parameters determining the agglomeration behaviour and the micromeritic properties of spherically agglomerated crystals prepared by the spherical crystallization technique with miscible solvent systems , 1995 .

[4]  J. Fell,et al.  Granulation and compaction of a model system. II. Stress relaxation , 1987 .

[5]  H. M. Smith,et al.  Spherical agglomeration of solids in liquid suspension , 1961 .

[6]  P. York,et al.  The compaction properties of nitrofurantoin samples crystallised from different solvents , 1991 .

[7]  P. Marchal,et al.  Relations between the properties of particles and their process of manufacture , 1996 .

[8]  Y. Kawashima,et al.  Spherical Crystallization: Direct Spherical Agglomeration of Salicylic Acid Crystals During Crystallization , 1982, Science.

[9]  J. Guyot,et al.  Ibuprofen agglomerates preparation by phase separation. , 1999, Drug development and industrial pharmacy.

[10]  Y. Kawashima,et al.  The effects of temperature on the spherical crystallization of salicylic acid , 1984 .

[11]  Y. Kawashima,et al.  Improvements in flowability and compressibility of pharmaceutical crystals for direct tabletting by spherical crystallization with a two-solvent system , 1994 .

[12]  C. Martín,et al.  Preparation of spherically agglomerated crystals of the 3,5-diglucoside of cyanidin (cyanin) , 1994 .

[13]  Y. Kawashima,et al.  Direct preparation of spherically agglomerated salicylic acid crystals during crystallization. , 1984, Journal of pharmaceutical sciences.

[14]  F. Espitalier,et al.  Definition of a solvent system for spherical crystallization of salbutamol sulfate by quasi-emulsion solvent diffusion (QESD) method. , 2001, Journal of pharmaceutical sciences.

[15]  Y. Kawashima,et al.  Improved Static Compression Behaviors and Tablettabilities of Spherically Agglomerated Crystals Produced by the Spherical Crystallization Technique with a Two-Solvent System , 1995, Pharmaceutical Research.

[16]  Leila Barghi,et al.  Design of Agglomerated Crystals of Ibuprofen During Crystallization: Influence of Surfactant , 2011 .

[17]  R L Carr,et al.  EVALUATING FLOW PROPERTIES OF SOLIDS , 1965 .

[18]  A. McKenna,et al.  Effect of particle size on the compaction mechanism and tensile strength of tablets , 1982, The Journal of pharmacy and pharmacology.

[19]  G. Bolhuis,et al.  Magnesium stearate susceptibility of directly compressible materials as an indication of fragmentation properties , 1988 .

[20]  B. Shekunov,et al.  CRYSTALLIZATION PROCESSES IN PHARMACEUTICAL TECHNOLOGY AND DRUG DELIVERY DESIGN , 2000 .

[21]  M. Maghsoodi Effect of process variables on physicomechanical properties of the agglomerates obtained by spherical crystallization technique , 2011, Pharmaceutical development and technology.

[22]  Å. Rasmuson,et al.  On the mechanisms of formation of spherical agglomerates. , 2011, European journal of pharmaceutical sciences : official journal of the European Federation for Pharmaceutical Sciences.

[23]  Z. Chowhan,et al.  Manipulation of Naproxen Particle Morphology Via the Spherical Crystallization Technique to Achieve A Directly Compressible Raw Material , 1990 .

[24]  Peter R. Griffiths,et al.  Theory and Instrumentation , 2002 .

[25]  A. Paradkar,et al.  Spherical Crystallization of Celecoxib , 2002, Drug development and industrial pharmacy.

[26]  Y. Kawashima,et al.  Spherical agglomeration of aminophylline crystals during reaction in liquid by the spherical crystallization technique. , 1982 .

[27]  Å. Rasmuson,et al.  Spherical crystallization of benzoic acid. , 2008, International journal of pharmaceutics.

[28]  Kawashima Yoichi,et al.  Tabletting properties of bucillamine agglomerates prepared by the spherical crystallization technique , 1994 .

[29]  Y. Kawashima,et al.  Particle Design of Tolbutamide by the Spherical Crystallization Technique. V. Improvement of Dissolution and Bioavailability of Direct Compressed Tablets Prepared Using Tolbutamide Agglomerated Crystals , 1992 .

[30]  Hirofumi Takeuchi,et al.  Improved flowability and compactibility of spherically agglomerated crystals of ascorbic acid for direct tableting designed by spherical crystallization process , 2003 .