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Improved Static Compression Behaviors and Tablettabilities of Spherically Agglomerated Crystals Produced by the Spherical Crystallization Technique with a Two-Solvent System

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Abstract

Purpose. Poorly compressible crystals of acebutolol hydrochloride were agglomerated by the spherical crystallization technique with a two-solvent system to improve the compressibility for direct tabletting. The mechanism of improvements in static compression behaviors and tablettabilities of the spherically agglomerated crystals were investigated.

Methods. The improvement of static compression behaviors of the agglomerated crystals was determined by measuring the stress relaxations and elastic recoveries of compressed powder of original and agglomerated crystals. The improved tablettability of agglomerated crystals was evaluated by the pressure transmission ratio upon compression, the ejection pressure for releasing the tablet from the die and the tablet strength, i.e., tensile strength required for breaking.

Results. The higher relaxation pressure and the lower elastic recovery of the agglomerated crystals than of the original crystals were found. The pressure transmission ratio data showed that the friction pressures of the two crystals were similar during the compression period. The ejection pressure of the agglomerated crystals was lower than that of the original crystals. The tensile strength of the tablet of agglomerated crystals was greater than that of the original crystals.

Conclusions. The compressibility and tablettability of the spherically agglomerated crystals prepared by the spherical crystallization technique were much improved due to their increased plastic property and reduced adhesive property compared to the original crystals.

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Authors and Affiliations

  1. Gifu Pharmaceutical University, Mitahora-higashi, Gifu, 502, Japan

    Yoshiaki Kawashima, Hirofumi Takeuchi, Toshiyuki Niwa & Tomoaki Hino

  2. Shenyang Pharmaceutical University, No. 103 Wenhua Road, Shenyang, China

    Fude Cui

  3. Rhone Poulenc Rorer Japan, Ltd., Roppongi 1st Building, Roppongi 1-9-9, Minato-ku, Tokyo, 107, Japan

    Katsumi Kiuchi

Authors
  1. Yoshiaki Kawashima
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  2. Fude Cui
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  3. Hirofumi Takeuchi
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  4. Toshiyuki Niwa
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  5. Tomoaki Hino
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  6. Katsumi Kiuchi
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Kawashima, Y., Cui, F., Takeuchi, H. et al. Improved Static Compression Behaviors and Tablettabilities of Spherically Agglomerated Crystals Produced by the Spherical Crystallization Technique with a Two-Solvent System. Pharm Res 12, 1040–1044 (1995). https://doi.org/10.1023/A:1016266600113

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  • DOI: https://doi.org/10.1023/A:1016266600113

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